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MK-0893
CAS No. 870823-12-4
MK-0893 ( MK0893 | MK 0893 )
产品货号. M16326 CAS No. 870823-12-4
一种有效的、选择性的、可逆的、竞争性的胰高血糖素受体拮抗剂，具有高结合亲和力 (IC50=6.6 nM) 和功能性 cAMP 活性 (IC50=15.7 nM)。
纯度: >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| 规格 | 价格/人民币 | 库存 | 数量 |
| 500MG | 获取报价 | 有现货 |
|
| 1G | 获取报价 | 有现货 |
|
生物学信息
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产品名称MK-0893
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注意事项本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断
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产品简述一种有效的、选择性的、可逆的、竞争性的胰高血糖素受体拮抗剂，具有高结合亲和力 (IC50=6.6 nM) 和功能性 cAMP 活性 (IC50=15.7 nM)。
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产品描述A potent, selective, reversible and competitive antagonist of glucagon receptor with high binding affinity (IC(=50=6.6 nM) and functional cAMP activity (IC50=15.7 nM); displays selectivity for glucagon receptor relative to other family B GPCRs, IC50 of 1020 nM for GIPR, 9200 nM for PAC1, and >10000 nM for GLP-1R, VPAC1, and VPAC2; blunts glucagon-induced glucose elevation in hGCGR mice and rhesus monkeys, also lowers ambient glucose levels in both acute and chronic mouse models.Diabetes Phase 2 Discontinued.
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体外实验——
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体内实验——
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同义词MK0893 | MK 0893
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通路GPCR/G Protein
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靶点Glucagon Receptor
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受体Glucagon Receptor
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研究领域Metabolic Disease
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适应症Diabetes
化学信息
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CAS Number870823-12-4
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分子量588.4805
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分子式C32H27Cl2N3O4
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纯度>98% (HPLC)
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溶解度10 mM in DMSO
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SMILESCC(C1=CC=C(C=C1)C(=O)NCCC(=O)O)N2C(=CC(=N2)C3=CC(=CC(=C3)Cl)Cl)C4=CC5=C(C=C4)C=C(C=C5)OC
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化学全称.beta.-Alanine, N-[4-[(1S)-1-[3-(3,5-dichlorophenyl)-5-(6-methoxy-2-naphthalenyl)-1H-pyrazol-1-yl]ethyl]benzoyl]-
运输与储存
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储存条件(-20℃)
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运输条件With Ice Pack
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稳定性≥ 2 years
参考文献
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Methylprodnisolone S...
Methylprednisolone succinate (Methylprednisolone hydrogen succinate) sodium 是一种糖皮质激素, 半衰期较Prednisolone长，是一种有效的抗炎剂。
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des-His1-[Glu9]-Gluc...
Glucagon receptor antagonist (pA2 = 7.2 for inhibition of glucagon-induced adenylyl cyclase activation in rat liver membranes); displays no agonist activity. Enhances glucose-stimulated pancreatic insulin release in vitro. Blocks added glucagon-induced hyperglycemia in normal rabbits without affecting glycogenolysis in vivo. Also blocks endogenous glucagon-induced hyperglycemia in streptozocin diabetic rats.
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(S, R)-LSN 3318839
(S, R)-LSN 3318839 is an allosteric modulator of the glucagon-like peptide-3318839 receptor (GLP-1R) that has demonstrated powerful hypoglycemic effects in animal models alone or in combination with sitagliptin.
