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1333210-07-3

中文名稱 1333210-07-3
英文名稱 Benzonitrile, 4-[[(1R,2R)-2-[(3R)-3-aMino-1-piperidinyl]-2,3-dihydro-1H-inden-1-yl]oxy]-3-chloro-
CAS 1333210-07-3
分子式 C21H22ClN3O
分子量 367.87
MOL 文件 1333210-07-3.mol
更新日期 2024/07/08 16:38:19
1333210-07-3 結(jié)構(gòu)式 1333210-07-3 結(jié)構(gòu)式

基本信息

中文別名
SAR7334游離態(tài)
英文別名
SAR7334
TRCP6-IN-1
TRCP6 inhibitor
4-(((1R,2R)-2-((R)-3-Aminopiperidin-1-yl)-2,3-dihydro-1H-inden-1-yl)oxy)-3-chlorobenzonitrile
Benzonitrile, 4-[[(1R,2R)-2-[(3R)-3-aMino-1-piperidinyl]-2,3-dihydro-1H-inden-1-yl]oxy]-3-chloro-
所屬類別
生物化工:激動劑抑制劑

物理化學性質(zhì)

沸點534.6±50.0 °C(Predicted)
密度1.30±0.1 g/cm3(Predicted)
儲存條件-20°C儲存
溶解度insoluble in H2O; ≥106.4 mg/mL in EtOH; ≥125.4 mg/mL in DMSO
酸度系數(shù)(pKa)10.95±0.20(Predicted)
形態(tài)Solid
顏色Light yellow to yellow

安全數(shù)據(jù)

危險性符號(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險性描述H302-H315-H319-H335

常見問題列表

生物活性
SAR7334是一種新型,高效且可生物利用的TRPC6通道抑制劑。SAR7334在膜片鉗實驗中阻斷了TRPC6電流,IC50為7.9 nM。
靶點
TargetValue
TPRC6
(Cell-free assay)
7.9nM
體外研究

SAR7334 inhibits TRPC6, TRPC3 and TRPC7-mediated Ca 2+ influx into cells with IC 50 s of 9.5, 282 and 226?nM, whereas TRPC4 and TRPC5-mediated Ca 2+ entry is not affected. SAR7334 (1?μM) results in a major block of the Ang II-evoked calcium influx in the podocytes. SAR7334 (1 μM) has negligible effect on SOCE. SAR7334 dose-dependently reduces TRPC6 currents with an IC 50 of 7.9?nM. SAR7334 (100?nM) substantially reduces TRPC6 currents.

體內(nèi)研究

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).

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