3-(1H-tetrazol-5-yl)-1,4,5,6-tetrahydrocyclopenta[c]pyrazole
更新时间：2025-09-02 20:58:22
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| 常用名 | MK-0354 | CAS号 | 851776-28-8 |
|---|---|---|---|
| 价格 | 纯度 | 98.0% | |
| 备货期 | 10天 | 库存 | 现货 |
| 产品详情（用途，包装等）
用途： MK-0354 is a partial agonist of GPR109a receptor, for hGPR109a/ mGPR109a with EC50 of 1.65/1.08 μM, showed no activation of GPR109b.IC50 value: 1.65 μM (EC50, for hGPR109a), 1.08 μM (EC50, for mGPR109a) [1]Target: GPR109ain vitro: MK-0354 demonstrated clear and statistically significant partial agonism in the cAMP assays for both the mouse and human receptors with efficacy approximately 60-70% of that of either nicotinic acid or β-hydroxy butyrate, a putative physiologically relevant ligand for hGPR109a, in the same assay platform. In addition, MK-0354 showed no activation of GPR109b in the cAMP assay at any concentration up to 100 μM. Following these interesting observations, we then prepared a number of other 5,5-fused pyrazoles analogous to those that showed receptor activity in our earlier studies. MK-0354 appeared to be somewhat unique among the members of the pyrazole tetrazole series in having reasonable receptor activity.[1]in vivo: MK-0354 retained the plasma free fatty acid lowering effects in mice associated with GPR109a agonism, but did not induce vasodilation at the maximum feasible dose. Moreover, preadministration of MK-0354 blocked the flushing effect induced by nicotinic acid but not that induced by PGD2. This profile made MK-0354 a suitable candidate for further study for the treatment of dyslipidemia.[1] MK-0354 is a GPR109A partial agonist that activates the antilipolytic pathway in adipocytes. The single-dose and multiple-dose pharmacokinetics and pharmacodynamics, as well as tolerability, of MK-0354 were examined in two Phase I studies conducted in healthy male volunteers. The lipid efficacy of MK-0354 was assessed in a Phase II study conducted in male and female patients with dyslipidemia.[2] 物理化学性质： CAS号：851776-28-8 常用中文名：MK-0354 常用英文名：MK-0354 分子式：C7H8N6 分子量：176.179 密度：1.6±0.1 g/cm3 沸点：535.3±60.0 °C at 760 mmHg 熔点：N/A 闪点：273.9±25.8 °C 储存条件：2-8℃ |
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- 上海化源生化科技有限公司
- 上海市 上海市 普陀区
- 产品名：3-(1H-tetrazol-5-yl)-1,4,5,6-tetrahydrocyclopenta[c]pyrazole
- 价格：
- 纯度：98.0%
- 备货期：10天
- 联系人：徐经理
- 上海源溪生物科技有限公司
- 上海市 上海市 浦东新区
- 产品名：MK-0354
- 价格： ￥需询单/1g
- 纯度：98.9%
- 备货期：1天
- 联系人：赖经理
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参考价格：$198/10mM*1mLinDMSO