| CAS NO: | 1160514-60-2 |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| Physical Appearance | A crystalline solid |
| Storage | Store at -20°C |
| M.Wt | 456.63 |
| Cas No. | 1160514-60-2 |
| Formula | C16H11Cl3F3N3O3 |
| Solubility | Soluble in DMSO |
| Chemical Name | ethyl 1-(4-(2,3,3-trichloroacrylamido)phenyl)-5-(trifluoromethyl)-1H-pyrazole-4-carboxylate |
| Canonical SMILES | Cl/C(C(NC1=CC=C(C=C1)N2N=CC(C(OCC)=O)=C2C(F)(F)F)=O)=C(Cl)\Cl |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
Pyr3, a pyrazole compound, selectively inhibits the canonical transient receptor potential channel 3 (TRPC3) [1].
TRPC3 is a member of TRPCs which control influxes of Ca2+ and other cations that induce diverse cellular processes upon stimulation of plasma membrane receptors coupled to phospholipase C. TRPC3 has been implicated in diverse biological functions, including B cell receptor-mediated Ca2+ oscillations, T cell receptor-dependent Ca2+ entry pathway, and cardiac hypertrophy [1].
In HEK293 cells, Pyr3 selectively inhibited TRPC3-mediated Ca2+ influx in a dose-dependent manner, with an IC50 value of 0.7 μM. In rat neonatal cardiomyocytes, Pyr3 suppressed activation of nuclear factor of activated T cells, with an IC50 value of 0.05 μM [1].
In sham operated mice, chronic treatment with Pyr3 (0.1 mg·kg–1·day–1, i.p.), Pyr3 attenuatedin vivo pressure overload-induced cardiac hypertrophy. In addition, the transverse aortic constriction operation-induced increase in expression of atrial natriuretic peptide mRNA, a reliable marker for cardiac hypertrophy, was also suppressed by Pyr3 [1].
Reference:
[1]. Kiyonaka S, Kato K, Nishida M, et al. Selective and direct inhibition of TRPC3 channels underlies biological activities of a pyrazole compound. Proceedings of the National Academy of Sciences of the United States of America, 2009, 106(13): 5400-5405.
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