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Mizagliflozin 是口服有效的、选择性的 SGLT1抑制剂,对人 SGLT1 的 Ki 值为 27 nM。Mizagliflozin 对 SGLT1 的选择性是 SGLT2的303 倍。Mizagliflozin 是抗糖尿病药物,可以改善餐后血糖波动并有可能有改善慢性便秘的潜力。
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Mizagliflozin 是口服有效的、选择性的 SGLT1抑制剂,对人 SGLT1 的 Ki 值为 27 nM。Mizagliflozin 对 SGLT1 的选择性是 SGLT2的303 倍。Mizagliflozin 是抗糖尿病药物,可以改善餐后血糖波动并有可能有改善慢性便秘的潜力。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 678 | 现货 | |
2 mg | ¥ 995 | 现货 | |
5 mg | ¥ 1,620 | 现货 | |
10 mg | ¥ 2,860 | 现货 | |
25 mg | ¥ 4,760 | 现货 | |
50 mg | ¥ 6,780 | 现货 | |
100 mg | ¥ 9,180 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 1,980 | 现货 |
产品描述 | Mizagliflozin is an orally active, selective SGLT1 inhibitor with a Ki value of 27 nM for human SGLT1. Mizagliflozin is 303 times more selective for SGLT1 than for SGLT2. Mizagliflozin is an anti-diabetic drug that can improve postprandial blood sugar fluctuations and may have the potential to improve chronic constipation. |
靶点活性 | SGLT2 (human):8170 nM(ki), SGLT1 (human):(ki)27 nM |
体内活性 | 方法:Mizagliflozin (GSK-1614235 free base)(0.3 mg/kg,静脉给药)和口服给药(3 mg/kg,口服给药)给大鼠,研究其药代动力学和代谢物谱。 结果:Mizagliflozin在大鼠中给药方式不同,半衰期也不同(分别为0.23和1.14小时);绝对生物利用度仅为0.02%;口服给药Mizagliflozin后主要在肠道中代谢为其苷元KP232。[2] |
别名 | KGA-3235 free base, GSK-1614235 free base, DSP-3235 free base |
分子量 | 564.67 |
分子式 | C28H44N4O8 |
CAS No. | 666843-10-3 |
Smiles | CC(C)c1[nH]nc(O[C@@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2O)c1Cc1ccc(OCCCNCC(C)(C)C(N)=O)cc1C |
密度 | 1.274 g/cm3 (Predicted) |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | Methanol: 250 mg/mL (442.74 mM), Sonication is recommended. DMSO: 100 mg/mL (177.09 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
DMSO/Methanol
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