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121345-64-0

中文名称 SR 33805
英文名称 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 结构式 121345-64-0 结构式

基本信息

中文别名
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]磺酰基]苯氧基]丙基]苯乙胺
英文别名
SR 33805

物理化学性质

储存条件-20°C储存
形态Solid
颜色White to off-white

常见问题列表

生物活性
SR33805 是一种有效的 Ca2+ 通道拮抗剂,在去极化和极化条件下的 EC50 值分别为 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脏衰竭。
靶点

L-type calcium channel

4.1 nM (EC 50 , in depolarized conditions)

L-type calcium channel

33 nM (EC 50 , in polarized conditions)

体外研究

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.
体内研究

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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