Pyr 10 is a TRPC3-selective inhibitor. IC50 of Ca2+ influx inhibition by Pyr10 in carbachol-stimulated YFP-TRPC3-transfected HEK293 cells for ROCE and thapsigargin-depleted native RBL-2H3 cells for SOCE is 0.72 uM and 13.08 uM.
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描述 | Pyr10, a pyrazole derivative, is a selective inhibitor of the Transient Receptor Potential Cation Channel, Subfamily C, Member 3 (TRPC3). It inhibits calcium influx in TRPC3-transfected HEK293 cells stimulated by carbachol with an IC50 of 0.72 μM, while its IC50 for inhibiting store-operated calcium entry in BRL-2H3 cells is 13.08 μM. This specificity allows Pyr10 to differentiate between receptor-operated TRPC3 channels and native STIM1/Orai1 channels[1]. |
Animal study | The genetic deletion of TRPC3 (TRPC3-/-) and the pharmacological blockade of these channels using Pyr10 mitigate ventricular cardiac fibroblast activation and myocardial fibrosis in hypertensive mice treated with N(ω)-nitro-l-arginine methyl ester (l-NAME)[2]. |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
2.23mL 0.45mL 0.22mL |
11.13mL 2.23mL 1.11mL |
22.25mL 4.45mL 2.23mL |
CAS号 | 1315323-00-2 |
分子式 | C18H13F6N3O2S |
分子量 | 449.37 |
SMILES Code | O=S(C1=CC=C(C)C=C1)(NC2=CC=C(N3N=C(C(F)(F)F)C=C3C(F)(F)F)C=C2)=O |
MDL No. | MFCD28411625 |
别名 | |
运输 | 蓝冰 |
InChI Key | CVALMMCIOLXHDM-UHFFFAOYSA-N |
Pubchem ID | 53475435 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Sealed in dry, 2-8°C |
溶解方案 |
请根据您的动物给药指南选择适当的溶解方案。 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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动物实验配方 |
IP 2% DMSO+water 0.1 mg/mL clear PO 0.5% CMC-Na 44 mg/mL suspension |