TRPC6-IN-1|901715-05-7|-陌孚医药/Medlife

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TRPC6-IN-1

目录号: PL12442 纯度: ≥99%

CAS No. :901715-05-7

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中文名称	TRPC6-IN-1
英文名称	TRPC6-IN-1
英文别名	1-Piperidinecarboxylic acid, 4-[3-(4-fluorophenyl)-7-hydroxy-2-methylpyrazolo[1,5-a]pyrimidin-5-yl]-, ethyl ester;TRPC6-IN-1;Ethyl 4-[3-(4-fluorophenyl)-7-hydroxy-2-methylpyrazolo[1,5-a]pyrimidin-5-yl]-1-piperidinecarboxylate (ACI)
Cas No.	901715-05-7
分子式	C₂₁H₂₃FN₄O₃
分子量	398.43
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情	TRPC6-IN-1 是 TRPC6 的一个抑制剂，其 EC₅₀ 值为 4.66 μM。
生物活性	TRPC6-IN-1 is a Transient Receptor Potential Canonical 6 Channel (TRPC6) inhibitor, with an EC 50 of 4.66 μM.
性状	Solid
IC50 & Target[1][2]	EC50: 0.45 μM (TRPC3), 1.13 μM (TRPC7), 4.66 μM(TRPC3).
体外研究(In Vitro)	TRPC6-IN-1 (compound 4o) rises in the TRPC6 cells in a concentration dependent manner, with a mean EC50 value of 4.66±0.03 μM, demonstrating a comparable activity of the compound on TRPC6 as the original lead. TRPC6-IN-1 is also tested on HEK293 cells that co-expressed μ opioid receptor (MOR) and TRPC4β, which belongs to a different subgroup of TRPC channels than TRPC3/6/7. Upon stimulation by a μ agonist, these cells show a robust increase in [Ca]i. TRPC6-IN-1 also evokes whole-cell currents in HEK293 cells that express human TRPC3. TRPC6-IN-1 elicits concentration dependent current increases in the TRPC7 cells. Different from TRPC6, the currents show some desensitization in the high TRPC6-IN-1 concentrations (10 and 30 μM) at both negative and positive potentials even though the low Ca (0.1 mM) bath solution is used. Nonetheless, a stepwis
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Powder -20°C 3 years；4°C 2 years
参考文献	[1]. Qu C, et al. Pyrazolopyrimidines as Potent Stimulators for Transient Receptor Potential Canonical 3/6/7 Channels. J Med Chem. 2017 Jun 8;60(11):4680-4692.

溶解度数据	In Vitro: DMSO : 100 mg/mL (250.99 mM; Need ultrasonic)配制储备液

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2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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