產(chǎn)品目錄

規(guī)格	5mg 10mg 50mg 100mg
CAS	1333207-63-8
別名	N/A
化學(xué)名	4-(((1R,2R)-2-((R)-3-aminopiperidin-1-yl)-2,3-dihydro-1H-inden-1-yl)oxy)-3-chlorobenzonitrile dihydrochloride
分子式	C21H24Cl3N3O
分子量	440.79
溶解度	DMF: 1 mg/mL,DMSO: 15 mg/mL,Ethanol: 25 mg/mL,Ethanol:PBS (pH 7.2) (1:5): 0.16mg/mL
儲(chǔ)存條件	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request

產(chǎn)品描述：

SAR7334 hydrochloride is a potent and specific TRPC6 inhibitor, inhibiting TRPC6 currents with IC50 of 7.9 nM.

SAR7334 inhibits TRPC6, TRPC3 and TRPC7-mediated Ca2+ influx into cells with IC50s of 9.5, 282 and 226nM[1][2][3], whereas TRPC4 and TRPC5-mediated Ca2+ entry is not affected. SAR7334 (1μM) results in a major block of the Ang II-evoked calcium influx in the podocytes[1]. SAR7334 (1 μM) has negligible effect on SOCE[2]. SAR7334 dose-dependently reduces TRPC6 currents with an IC50 of 7.9nM. SAR7334 (100nM) substantially reduces TRPC6 currents[3].

SAR7334 (10mg/kg, p.o.) suppresses TRPC6-dependent acute HPV in isolated perfused lungs from mice. SAR7334 demonstrates that it is suitable for chronic oral administration. In an initial short-term study, SAR7334 does not change mean arterial pressure in spontaneously hypertensive rats (SHR)[3].

[1]. Ilatovskaya DV, et al. The Role of Angiotensin II in Glomerular Volume Dynamics and Podocyte Calcium Handling. Sci Rep. 2017 Mar 22;7(1):299.

[2]. Chauvet S, et al. Pharmacological Characterization of the Native Store-Operated Calcium Channels of Cortical Neurons from Embryonic Mouse Brain. Front Pharmacol. 2016 Dec 12;7:486.

[3]. Maier T, et al. Discovery and pharmacological characterization of a novel potent inhibitor of diacylglycerol-sensitive TRPC cation channels. Br J Pharmacol. 2015 Jul;172(14):3650-60.

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1. 本產(chǎn)品僅供科研使用。請(qǐng)勿用于醫(yī)藥、臨床診斷或治療，食品及化妝品等用途。請(qǐng)勿存放于普通住宅區(qū)。

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原創(chuàng)作者：上海莼試生物技術(shù)有限公司

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