Cas No.: | 1333207-63-8 |
Chemical Name: | 4-[[(1R,2R)-2-[(3R)-3-Amino-1-piperidinyl]-2,3-dihydro-1H-inden-1-yl]oxy]-3-chlorobenzonitrile dihydrochloride |
Synonyms: | SAR-7334; SAR 7334; SAR7334. SAR-7334 HCl, SAR-7334 hydrochloride |
SMILES: | N[C@@H](C1)CCCN1[C@@H]2CC3=CC=CC=C3[C@H]2OC4=CC=C(C#N)C=C4Cl.Cl.Cl |
Formula: | C21H24Cl3N3O |
M.Wt: | 440.793 |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | SAR7334 hydrochloride is a potent and specific TRPC6 inhibitor, inhibiting TRPC6 currents with IC50 of 7.9 nM. |
In Vivo: | SAR7334 (10 mg/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]. |
In Vitro: | SAR7334 inhibits TRPC6, TRPC3 and TRPC7-mediated Ca2+ influx into cells with IC50s of 9.5, 282 and 226 nM[1][2][3], whereas TRPC4 and TRPC5-mediated Ca2+ entry is not affected. SAR7334 (1 μM) 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 7.9 nM. SAR7334 (100 nM) substantially reduces TRPC6 currents[3]. |