Tag: M.W=450-500

Waugh, Stephen M. published the artcileIsolation of a proteolytically derived domain of the insulin receptor containing the major site of cross-linking/binding, Category: alcohols-buliding-blocks, the publication is Biochemistry (1989), 28(8), 3448-55, database is CAplus and MEDLINE.

Radiolabeled insulin was affinity crosslinked to purified insulin receptor with 6 sep. bifunctional N-hydroxysuccinimde esters of different lengths. Results were qual. identical for each crosslinker in that insulin was predominantly crosslinked through its B chain to the receptor’s α subunit. The maximum efficiencies of crosslinking were 10-15% for the most effective reagents, and this value was dependent upon the concentration and length of the crosslinker. In an effort to locate the crosslinking site, monoiodoinsulin was crosslinked to affinity-purified insulin receptor with disuccinimidyl suberate. Limited proteolysis of the hormone/receptor adduct with Staphylococcus aureus V8 protease, chymotrypsin, or thermolysin in an SDS-containing buffer rapidly generated a 55-kDa, insulin-labeled fragment as shown by SDS-PAGE. It was reported earlier that the 55-kDa chymotryptic fragment contained multiple internal SS bonds as evidenced by its shifting mobility on an SDS gel after dithiothreitol treatment. The 55-kDa fragment is also formed by proteolysis of the receptor in the absence of prior insulin crosslinking. This fragment was prepared in amounts sufficient for sequence anal. and was purified by passage successively over gel-permeation and reverse-phase HPLC columns. The sequence of the fragment’s N terminus corresponds to that of the N terminus of the receptor’s α subunit. This fragment also reacts with an antibody raised against a synthetic peptide corresponding to residues 242-253 of the receptor’s α subunit. On the basis of the fragment’s size, N-terminal sequence, and immunoreactivity, the results indicate that the fragment extends from the α subunit’s N terminus through the SS-rich region of this subunit, i.e., residues 155-312. These results are consistent with this region containing the insulin-binding site.

Biochemistry published new progress about 70539-42-3. 70539-42-3 belongs to alcohols-buliding-blocks, auxiliary class pyrrolidine,Ester,Amide,Inhibitor,Inhibitor, name is Bis(2,5-dioxopyrrolidin-1-yl) O,O’-ethane-1,2-diyl disuccinate, and the molecular formula is C19H21N3O3S, Category: alcohols-buliding-blocks.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Bhattacherjee, Abhishek published the artcileArgpyrimidine-tagged rutin-encapsulated biocompatible (ethylene glycol dimers) nanoparticles: Synthesis, characterization and evaluation for targeted drug delivery, Recommanded Product: Bis(2,5-dioxopyrrolidin-1-yl) O,O’-ethane-1,2-diyl disuccinate, the publication is International Journal of Pharmaceutics (Amsterdam, Netherlands) (2016), 509(1-2), 507-517, database is CAplus and MEDLINE.

Diabetes mellitus represents a major metabolic disorder affecting millions of people all over the world. Currently available therapeutic treatments are not good enough to control the long-term complications of diabetes. Active targeting via inclusion of a specific ligand on the nanoparticles provides effective therapeutic approach in different diseases. However, such specific drug delivery systems have not been explored much in diabetes due to lack of suitable biol. targets in this disorder. Our objective is to synthesize a ligand-tagged drug-loaded nanoparticle for delivery of the drug at specific sites to enhance its therapeutic efficiency in diabetic condition. The nanoparticles have been prepared by using biocompatible ethylene glycol-bis (succinic acid N-hydroxysuccinimide ester) dimers. Although advanced glycation end products (AGEs) are the root causes of diabetic complications, argpyrimidine, an AGE, possesses antioxidant and reducing activities. AGE interacts selectively with its cell surface receptors (RAGE), which are significantly increased in diabetic condition. We have selected RAGE as the target of argpyrimidine, which is tagged on the nanoparticles as a ligand. Rutin, having anti-hyperglycemic and anti-glycating activities, has been used for nanoencapsulation. Rutin-loaded argpyrimidine-tagged nanoparticles have been synthesized and characterized. We have demonstrated the drug releasing capacity and target specificity of the synthesized drug delivery system under ex vivo and in vivo conditions.

International Journal of Pharmaceutics (Amsterdam, Netherlands) published new progress about 70539-42-3. 70539-42-3 belongs to alcohols-buliding-blocks, auxiliary class pyrrolidine,Ester,Amide,Inhibitor,Inhibitor, name is Bis(2,5-dioxopyrrolidin-1-yl) O,O’-ethane-1,2-diyl disuccinate, and the molecular formula is C18H20N2O12, Recommanded Product: Bis(2,5-dioxopyrrolidin-1-yl) O,O’-ethane-1,2-diyl disuccinate.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Cui, Wen-hua published the artcileApplication of carboprost tromethamine and improved B-Lynch suture in postnatal hemorrhage of cesarean section, Application of 2-Amino-2-(hydroxymethyl)propane-1,3-diol (Z)-7-((1R,2R,3R,5S)-3,5-dihydroxy-2-((S,E)-3-hydroxy-3-methyloct-1-en-1-yl)cyclopentyl)hept-5-enoic acid, the publication is Zhongguo Fuyou Baojian (2013), 28(22), 3710-3711, database is CAplus.

The objective of this paper is to investigate carboprost tromethamine and uterine Modified B-Lynch suture in the treatment of intractable postpartum hemorrhage in cesarean. Here, 36 patients treated by general application can not stop the bleeding maternal carboprost tromethamine and modified B-Lynch suture. The results shows, 30 cases of postpartum hemorrhage were stopped, the bleeding rate was 83.33%. Carboprost tromethamine and modified B-Lynch suture in the treatment of uterine cesarean intractable postpartum hemorrhage is certainly worthy of promotion.

Zhongguo Fuyou Baojian published new progress about 58551-69-2. 58551-69-2 belongs to alcohols-buliding-blocks, auxiliary class Chiral,Alkenyl,Amine,Aliphatic cyclic hydrocarbon,Ester,Alcohol,Inhibitor,, name is 2-Amino-2-(hydroxymethyl)propane-1,3-diol (Z)-7-((1R,2R,3R,5S)-3,5-dihydroxy-2-((S,E)-3-hydroxy-3-methyloct-1-en-1-yl)cyclopentyl)hept-5-enoic acid, and the molecular formula is C25H47NO8, Application of 2-Amino-2-(hydroxymethyl)propane-1,3-diol (Z)-7-((1R,2R,3R,5S)-3,5-dihydroxy-2-((S,E)-3-hydroxy-3-methyloct-1-en-1-yl)cyclopentyl)hept-5-enoic acid.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Shi, An-Guo published the artcilePrecoupling of alpha-2B adrenergic receptors and G-proteins in transfected PC-12 cell membranes: influence of pertussis toxin and a lysine-directed cross-linker, Synthetic Route of 70539-42-3, the publication is Journal of Pharmacology and Experimental Therapeutics (1994), 271(3), 1520-7, database is CAplus and MEDLINE.

The ability of pertussis toxin (PTX) pretreatment to alter the binding of [³H]rauwolscine (RAU) to alpha-2B adrenergic receptors expressed in PC12 cells was examined PTX caused a 30% increase in the B_max for [³H]RAU and reduced its K_D, whereas in the added presence of Na⁺ and Gpp(NH)p binding was increased to 75% above the level in untreated membranes. Because all three agents act to reduce receptor/G-protein affinity, the increased binding may reflect extensive precoupling of the alpha-2B receptor. The affinity of the agonist epinephrine in displacing [³H]RAU was normally reduced by both Na⁺ and Gpp(NH)p; however, in PTX-treated membranes the effect of Gpp(NH)p was eliminated, and Na⁺ remained effective. The lysine-directed crosslinking reagent ethyleneglycol bis(succinimidyl)succinate (EGS) was utilized to cross-link precoupled receptor and G-protein. Maximal [³H]RAU binding was reduced by EGS in a time- and dose-dependent manner, and this action was reversed by prior incubation with Na⁺ and Gpp(NH)p, suggesting that EGS did indeed cross-link receptor and G-protein. RAU and epinephrine each provided protection against the effect of EGS. The inclusion of Na⁺ and Gpp(NH)p during [³H]RAU binding studies was able to restore maximal binding in EGS-treated membranes to the same level as untreated membranes. These results indicate that in the absence of Na⁺ and Gpp(NH)p at least 40% of the total alpha-2B adrenergic receptors in these membranes exist as a precoupled receptor/G-protein complex which fails to bind [³H]RAU.

Journal of Pharmacology and Experimental Therapeutics published new progress about 70539-42-3. 70539-42-3 belongs to alcohols-buliding-blocks, auxiliary class pyrrolidine,Ester,Amide,Inhibitor,Inhibitor, name is Bis(2,5-dioxopyrrolidin-1-yl) O,O’-ethane-1,2-diyl disuccinate, and the molecular formula is C25H47NO8, Synthetic Route of 70539-42-3.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Svoboda, Michal published the artcileMolecular characteristics and evidence for internalization of vasoactive intestinal peptide (VIP) receptors in the tumoral rat-pancreatic acinar cell line AR 4-2 J, Quality Control of 70539-42-3, the publication is European Journal of Biochemistry (1988), 176(3), 707-13, database is CAplus and MEDLINE.

VIP receptors were investigated in the tumoral acinar cell line AR 4-2 J derived from rat pancreas. After incubation with 20 nM dexamethasone, the binding capacity increased twofold but affinities were unchanged. External [¹²⁵I]iodo-VIP binding to intact cells reached steady state after 5 min at 37°, whereas the sequestration-internalization of the [¹²⁵I]iodo-VIP-receptor complex (tested by cold acid washing) increased progressively, reaching 75% of total binding after 1 h. This phenomenon was blocked at 4°. Further data with dexamethasone, tunicamycin, cycloheximide, low temperature, and/or phenylarsine oxide suggested a half-life of 2 days for VIP receptors and the necessity of N-glycosylation for proper translocation. For chem. [¹²⁵I]iodo-VIP crosslinking, bis[2-(succinimidooxycarbonyloxy)ethyl]sulfone gave the best yield when compared with five other bifunctional reagents. In membranes, the main specifically cross-linked peptide had M_r 66,000 under nonreducing conditions, and migrated with lower velocity (-5%) under reducing conditions. Crosslinking was suppressed by VIP, peptide His-IleNH₂ and helodermin (competitively) and also by GTP. In intact cells, the M_r of [¹²⁵I]iodo-VIP-cross-linked peptides depended on the mode of cell solubilization. After direct solubilization, the major cross-linked radioactivity migrated as a smear of M_r 130,000-180,000 but an M_r-66,000 peptide was also detectable. In contrast, the solubilization of cross-linked cells detached by mild trypsinization gave mainly the M_r-66,000 labeled peptide. This suggests that most VIP receptors in intact, attached cells were in a high-M_r complex and that mild cell treatment was sufficient to disrupt this complex.

European Journal of Biochemistry published new progress about 70539-42-3. 70539-42-3 belongs to alcohols-buliding-blocks, auxiliary class pyrrolidine,Ester,Amide,Inhibitor,Inhibitor, name is Bis(2,5-dioxopyrrolidin-1-yl) O,O’-ethane-1,2-diyl disuccinate, and the molecular formula is C6H13NO2, Quality Control of 70539-42-3.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Vaid, Arvind published the artcileA randomized controlled trial of prophylactic sublingual misoprostol versus intramuscular methyl-ergometrine versus intramuscular 15-methyl PGF2α in active management of third stage of labor, Related Products of alcohols-buliding-blocks, the publication is Archives of Gynecology and Obstetrics (2009), 280(6), 893-897, database is CAplus and MEDLINE.

Objective: To compare the efficacy and side effects of 0.2 mg methyl-ergometrine IM, 400 μg misoprostol sublingual and 125 μg 15 Me PGF2α IM in active management of third stage of labor. Method: Two hundred low risk pregnant women with induced or spontaneous labor were randomized to receive either 400 μg misoprostol sublingually or 0.2 mg methyl-ergometrine i.m. or 125 μg 15-Me PGF2α i.m., after the delivery of anterior shoulder of baby. The main outcome measures were: blood loss more than 500 mL, need for addnl. oxytoxic drug, change in Hb level and side effects due to drugs. Results: The median estimated blood loss, blood loss more than 500 mL, need for addnl. oxytocic drug and change in Hb levels were similar in all three groups. The significant side effects in the misoprostol group were shivering, pyrexia (temperature > 38°C) and vomiting, which were self-limiting. Diarrhea was significantly more in the 15 Me PGF2α group. Three women in methyl-ergometrine group underwent manual removal of placenta. One woman in misoprostol group received blood transfusion. Conclusion: Sublingual misoprostol appears to be as effective as i.m. methyl-ergometrine and i.m. 15-Me PGF2α in the prevention of postpartum hemorrhage. It can be a good alternative in resource poor setting.

Archives of Gynecology and Obstetrics published new progress about 58551-69-2. 58551-69-2 belongs to alcohols-buliding-blocks, auxiliary class Chiral,Alkenyl,Amine,Aliphatic cyclic hydrocarbon,Ester,Alcohol,Inhibitor,, name is 2-Amino-2-(hydroxymethyl)propane-1,3-diol (Z)-7-((1R,2R,3R,5S)-3,5-dihydroxy-2-((S,E)-3-hydroxy-3-methyloct-1-en-1-yl)cyclopentyl)hept-5-enoic acid, and the molecular formula is C5H7BO2S, Related Products of alcohols-buliding-blocks.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Badinga, Lokenga published the artcileCovalent coupling of bovine growth hormone to its receptor in bovine liver membranes, Safety of Bis(2,5-dioxopyrrolidin-1-yl) O,O’-ethane-1,2-diyl disuccinate, the publication is Molecular and Cellular Endocrinology (1987), 52(1-2), 85-9, database is CAplus and MEDLINE.

The structure of bovine somatotropin receptor was examined following covalent coupling of iodinated recombinant bovine growth hormone ([¹²⁵I]rbGH) to bovine liver membrane receptors using ethylene glycol bis(succinimidyl succinate). Iodinated rbGH was incorporated into a complex of estimated mol. weight (M_r) of 140,000 under reducing conditions. Excess unlabeled rbGH, but not bovine prolactin (bPRL), inhibited completely the incorporation of [¹²⁵I]rbGH into the M_r = 140,000 species. In dairy bulls, the M_r = 140,000 complex was undetectable soon after birth but became predominant at 6 mo of age. No evidence was found to support presence of bPRL receptors in steer liver membranes. Assuming a 1:1 stoichiometry of hormone binding to receptor, it appears that bGH binds to a major receptor subunit of M_r = 119,000 which does not recognize bPRL.

Molecular and Cellular Endocrinology published new progress about 70539-42-3. 70539-42-3 belongs to alcohols-buliding-blocks, auxiliary class pyrrolidine,Ester,Amide,Inhibitor,Inhibitor, name is Bis(2,5-dioxopyrrolidin-1-yl) O,O’-ethane-1,2-diyl disuccinate, and the molecular formula is C18H20N2O12, Safety of Bis(2,5-dioxopyrrolidin-1-yl) O,O’-ethane-1,2-diyl disuccinate.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Watts, Norman R. M. published the artcileAnalysis of near-neighbor contacts in bacteriophage T4 wedges and hubless baseplates by using a cleavable chemical cross-linker, Related Products of alcohols-buliding-blocks, the publication is Journal of Virology (1989), 63(6), 2427-36, database is CAplus and MEDLINE.

Although bacteriophage T4 baseplate morphogenesis has been analyzed in some detail, there is little information available on the spatial arrangement and associations of its 150 subunits. Therefore, anal. of its near-neighbor interactions by using the cleavable chem. cross-linker ethylene glycobis(succinimidylsuccinate) was carried out. The cross-linked complexes that have been identified in the one-sixth arms or wedges and also in baseplatelike structures called rings are described which consist of 6 wedges but lack the central hub, both of which are purified from T4 gene 5^–-infected cells. Thirty different complexes were identified, of which about half contain multimers of a single species and half contain 2 different species. In general, the complexes reflect and support the assembly pathway derived by Y. Kikuchi and J. King (1975 ), but broaden its scope to include such complexes as gp25-gp53, gp25-gp48, and gp48-gp53, which locate the gp48 binding site over the inner edge of the ring but outside the central hub. The data also supports the view that wedges are assembled from the outer edge inward toward the central hub. Wedge-wedge contact in rings was mediated primarily by gp12 and gp9, the absence of which dramatically destabilized the ring ↔ wedge equilibrium in favor of wedges. Although no heterologous complexes containing gp9 were identified, gp12 contacts unique to rings were observed with both gp10 and gp11.

Journal of Virology published new progress about 70539-42-3. 70539-42-3 belongs to alcohols-buliding-blocks, auxiliary class pyrrolidine,Ester,Amide,Inhibitor,Inhibitor, name is Bis(2,5-dioxopyrrolidin-1-yl) O,O’-ethane-1,2-diyl disuccinate, and the molecular formula is C18H19ClN4, Related Products of alcohols-buliding-blocks.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Watts, Norman R. M. published the artcileStructure of the bacteriophage T4 baseplate as determined by chemical cross-linking, Application of Bis(2,5-dioxopyrrolidin-1-yl) O,O’-ethane-1,2-diyl disuccinate, the publication is Journal of Virology (1990), 64(1), 143-54, database is CAplus and MEDLINE.

A series of reversible chem. crosslinking experiments using the reagent ethylene glycol-bis(succinimidylsuccinate) were carried out to determine the 3-dimensional structure of the bacteriophage T4 baseplate. In a previous report, near-neighbor contacts in baseplate precursors and substructures were examined (Watts, N. R. M.; Coombs, J. 1989). Finished baseplates and tails were also examined Most of the previous contacts were confirmed, and several new contacts, including those within the central hub (gp5-gptd₂, gp26-gptd), between the hub and the outer wedges (gp6-gp27₂), between baseplate and sheath (gp54-gp18), and between sheath and core (gp19-gp18) are reported. On the basis of this and other available information, a partial 3-dimensional model of the baseplate is proposed.

Journal of Virology published new progress about 70539-42-3. 70539-42-3 belongs to alcohols-buliding-blocks, auxiliary class pyrrolidine,Ester,Amide,Inhibitor,Inhibitor, name is Bis(2,5-dioxopyrrolidin-1-yl) O,O’-ethane-1,2-diyl disuccinate, and the molecular formula is C14H26O2, Application of Bis(2,5-dioxopyrrolidin-1-yl) O,O’-ethane-1,2-diyl disuccinate.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Siezen, Roland J. published the artcilePermanent suppression of phase separation cataract in calf lens using amine modification agents, Recommanded Product: Bis(2,5-dioxopyrrolidin-1-yl) O,O’-ethane-1,2-diyl disuccinate, the publication is Biochemical and Biophysical Research Communications (1985), 133(1), 239-47, database is CAplus and MEDLINE.

Low-temperature-induced opacification (cold cataract) of the nucleus of young mammalian lenses was associated with a phase separation of proteins in the lens cell cytoplasm. Calf lenses were treated with a variety of imidoesters and N-hydroxysuccinimide esters, which react specifically with amino groups. Many potent inhibitors of phase-separation cataract were identified which lower the opacification temperature by ≥6°. Lenses generally remained clear, colorless and soft. Furthermore, suppression of the cold-cataract temperature was permanent upon removal of excess reagent.

Biochemical and Biophysical Research Communications published new progress about 70539-42-3. 70539-42-3 belongs to alcohols-buliding-blocks, auxiliary class pyrrolidine,Ester,Amide,Inhibitor,Inhibitor, name is Bis(2,5-dioxopyrrolidin-1-yl) O,O’-ethane-1,2-diyl disuccinate, and the molecular formula is C7H14N4, Recommanded Product: Bis(2,5-dioxopyrrolidin-1-yl) O,O’-ethane-1,2-diyl disuccinate.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts