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BMS-903452是一种有效的、具有选择性的 GPR119激动剂,EC50为14 nM。BMS-903452可用于治疗急性和慢性啮齿动物糖尿病。GPR119主要在胰腺 b 细胞和胃肠道肠内分泌细胞中表达,对9种不同的细胞色素 P450酶没有显著的抑制作用(IC50 > 40 μM),不激活 PXR (EC50>50 μM),并且对肝脏(HEPG2)细胞系没有毒性。


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BMS-903452是一种有效的、具有选择性的 GPR119激动剂,EC50为14 nM。BMS-903452可用于治疗急性和慢性啮齿动物糖尿病。GPR119主要在胰腺 b 细胞和胃肠道肠内分泌细胞中表达,对9种不同的细胞色素 P450酶没有显著的抑制作用(IC50 > 40 μM),不激活 PXR (EC50>50 μM),并且对肝脏(HEPG2)细胞系没有毒性。
| 规格 | 价格 | 库存 | 数量 |
|---|---|---|---|
| 1 mg | ¥ 636 | 现货 | |
| 5 mg | ¥ 1,600 | 现货 | |
| 10 mg | ¥ 2,290 | 现货 | |
| 25 mg | ¥ 3,460 | 现货 | |
| 50 mg | ¥ 4,630 | 现货 | |
| 100 mg | ¥ 6,300 | 现货 | |
| 200 mg | ¥ 8,270 | 现货 | |
| 1 mL x 10 mM (in DMSO) | ¥ 1,780 | 现货 |
BMS-903452 相关产品
| 产品描述 | BMS-903452 is a potent and selective GPR119 agonist with EC50 of 14 nM. BMS-903452 is indicated for the treatment of acute and chronic rodent diabetes. GPR119 was mainly expressed in pancreatic b cells and gastrointestinal endocrine cells. GPR119 had no significant inhibitory effect on 9 different cytochrome P450 enzymes (IC50 > 40 μM), did not activate PXR (EC50>50 μM), and was not toxic to liver (HEPG2) cell lines. |
| 靶点活性 | GPR119:14nM(EC50) |
| 体内活性 | An oral glucose tolerance test (OGTT) to measure the acute efficacy of this agonist in C57/BL6 mice. Glucose excursion was 37%-40% lower in mice treated with BMS-903452 (0.1, 0.3, and 1 mg/kg) than in control mice. Treatment of SD rats with 0.3 mg/kg BMS-903452 stimulated GLP-1 production, and co-administration of BMS-903452 with a DPP-4 inhibitor synergistically augmented GLP-1 levels. [1] |
| 分子量 | 513.37 |
| 分子式 | C21H19Cl2FN4O4S |
| CAS No. | 1339944-47-6 |
| Smiles | O=C1N(C=C(Cl)C(OC2CCN(CC2)C=3N=CC(Cl)=CN3)=C1)C4=C(F)C=C(S(C)(=O)=O)C=C4 |
| 存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||
| 溶解度信息 | DMSO: 10 mg/mL (19.48 mM), Sonication is recommended. | ||||||||||||||||||||
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