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121345-64-0

中文名稱 SR 33805
英文名稱 SR 33805
CAS 121345-64-0
分子式 C32H40N2O5S
分子量 564.735
MOL 文件 121345-64-0.mol
121345-64-0 結(jié)構(gòu)式 121345-64-0 結(jié)構(gòu)式

基本信息

中文別名
3,4-二甲氧基-N-甲基-N-[3-[4-[[1-甲基-2-2-(1-甲基乙基))-1H-吲哚-‐3-基]磺?;鵠苯氧基]丙基]苯乙胺
英文別名
SR 33805

物理化學(xué)性質(zhì)

儲(chǔ)存條件-20°C儲(chǔ)存
形態(tài)Solid
顏色White to off-white

常見問題列表

生物活性
SR33805 是一種有效的 Ca2+ 通道拮抗劑,在去極化和極化條件下的 EC50 值分別為 4.1 nM 和 33 nM。SR33805 阻止 L 型而不是 T 型 Ca2+ 通道。SR33805 可用于研究急性或慢性心臟衰竭。
靶點(diǎn)

L-type calcium channel

4.1 nM (EC 50 , in depolarized conditions)

L-type calcium channel

33 nM (EC 50 , in polarized conditions)

體外研究

SR33805 (0.01-10 μM; 3 d) inhibits growth factor-induced proliferation of SMC (0.20 50<0.46 μM) in a dose-dependent manner.
SR33805 (10 μM; 10 min) restores the myocardial infarction (MI)-altered cell shortening without affecting the Ca 2+ transient amplitude.
SR33805 (10 μM) decreases the activity of recombinant PKA.

Cell Viability Assay

Cell Line: Smooth muscle cells (SMC)
Concentration: 0.01, 0.1, 1, 10 μM
Incubation Time: 3 days
Result: Inhibited in a dose-dependent manner FCS-, bFGF and PDGF-induced proliferation of porcine SMC with IC 50 s of 0.26±0.08, 0.46±0.1 and 0.20±0.04 μM, respectively.
體內(nèi)研究

SR33805 (20 mg/kg; a single i.p.) improves end-systolic strain and fractional shortening of MI hearts in rats.
SR33805 (5 mg/kg/day; p.o. for 38 d) significantly reduces intimal hyperplasia in pigs.

Animal Model: Male Wistar rats (5 weeks) are subjected to coronary artery ligature
Dosage: 0.2, 2, 20 mg/kg
Administration: A single i.p. injection
Result: Increased significantly both end-systolic strain (ESS) and fractional shortening (FS) by about +38 and +26%, respectively at the dose of 20 mg/kg.
Did not affect other contractile parameters.
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