| 货号 | 规格 | 价格 | 上海 | 北京 | 珠海 | 重庆 | 武汉 | 购买数量 |
|---|---|---|---|---|---|---|---|---|
S89286-1mg买3赠1 |
≥98% | ￥200.00 |
4 | - | - | - | - |
|
S89286-5mg买3赠1 |
99.00% | ￥480.00 |
8 | - | - | - | - |
|
S89286-10mg买3赠1 |
99.00% | ￥720.00 |
6 | - | - | - | - |
|
S89286-25mg买3赠1 |
99.00% | ￥1440.00 |
5 | - | - | - | - |
|
S89286-100mg买3赠1 |
≥98% | ￥4320.00 |
货期：2-3天 | - | - | - | - |
|
| 产品描述： | ML380 is a potent, subtype-selective, and brain-penetrant positive allosteric modulator (PAM) of M5 mAChR, with EC50s of 190 and 610 nM for human and rat M5, respectively. ML380 exhibits moderate selectivity versus the M1 and M3 mAChR subtypes. ML380 could increase the affinity of ACh for the M5 mAChR | ||||||||||||||||||||
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| 靶点： | IC50: 190 nM (hM5), 610 nM (rM5);AChR | ||||||||||||||||||||
| 体外研究： | ML380 (0.01 nM-100 μM) robustly stimulates inositol phosphate (IP) accumulation and Ca2+ mobilization in CHO-hM5 cells, with pEC50s of 5.33 and 5.71, respectively. ML380 (0.01-30 μM) increases the ACh-stimulated IP accumulation and Ca2+ mobilization in CHO-hM5 cells. |
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| 体内研究： | ML380 (1 mg/kg; i.v.) displays high clearance (66 mL/min/kg), a moderate volume of distribution (1.6 L/kg), and a short half-life (t1/2, 22 min) in rats. | ||||||||||||||||||||
| 参考文献： | 1. Gentry PR, et, al. Development of a highly potent, novel M5 positive allosteric modulator (PAM) demonstrating CNS exposure: 1-((1H-indazol-5-yl)sulfoneyl)-N-ethyl-N-(2-(trifluoromethyl)benzyl)piperidine-4-carboxamide (ML380). J Med Chem. 2014 Sep 25;57(18):7804-10. 2. Berizzi AE, et, al. Molecular Mechanisms of Action of M5 Muscarinic Acetylcholine Receptor Allosteric Modulators. Mol Pharmacol. 2016 Oct;90(4):427-36. 3. Berizzi AE, et, al. Structure-Activity Relationships of Pan-Gα q/11 Coupled Muscarinic Acetylcholine Receptor Positive Allosteric Modulators. ACS Chem Neurosci. 2018 Jul 18;9(7):1818-1828. | ||||||||||||||||||||
| 溶解性： | Soluble in DMSO | ||||||||||||||||||||
| 保存条件： | -20℃ | ||||||||||||||||||||
| 配置溶液浓度参考： |
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| 注意： | 部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
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