SR33805

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

SR33805 是 Ca2+ 通道的有效拮抗剂（在去极化和极化条件下 EC50 分别为 4.1 nM 和 33 nM）。SR33805 的急性治疗恢复了 MI 改变的细胞缩短，而不影响 Ca(2+) 瞬态振幅，表明MI 肌细胞中肌丝 Ca(2+) 敏感性。

SR33805 is a potent antagonist of Ca2+ channel(EC50s of 4.1 nM and 33 nM in depolarized and polarized conditions, respectively)Acute treatment with SR33805 restored the MI-altered cell shortening without affecting the Ca(2+) transient amplitude, suggesting an increase of myofilament Ca(2+) sensitivity in MI myocytes.?Indeed, a SR33805-induced sensitization of myofilament activation was found to be associated with a slight increase in myosin light chain-2 phosphorylation and a more significant decrease on troponin I (TnI) phosphorylation.?Decreased TnI phosphorylation was related to inhibition of protein kinase A activity by SR33805.?Finally, administration of a single intra-peritoneal bolus of SR33805 (20 mg/kg) improved end-systolic strain and fractional shortening of MI hearts.

SR33805 (0.01-10 μM; 3 d) inhibits growth factor-induced proliferation of SMC (0.2050<0.46 μM) in a dose-dependent manner.SR33805 (10 μM; 10 min) restores the myocardial infarction (MI)-altered cell shortening without affecting the Ca2+ 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 IC50s of 0.26±0.08, 0.46±0.1 and 0.20±0.04 μM, respectively.

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.

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GPCR/G Protein

Calcium Channel

Calcium Channel

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121345-64-0

564.74

C32H40N2O5S

>98% (HPLC)

In Vitro:?DMSO : ≥ 100 mg/mL (177.07 mM)

COc1ccc(CCN(C)CCCOc2ccc(cc2)S(=O)(=O)c2c(C(C)C)n(C)c3ccccc23)cc1OC

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(-20℃)

With Ice Pack

≥ 2 years