Powder-20°C3 years 4°C2 yearsIn solvent-80°C6 months-20°C1 month
Biological activity
Description
CAS NO.：121345-64-0 Product Name：Benzeneethanamine,3,4-dimethoxy-N-methyl-N-[3-[4-[[1-methyl-2-(1-methylethyl)-1H-indol-3-yl]sulfonyl]phenoxy]propyl]- Synonyms： EINEC: Molecular Formula：C32H40N2O5S Molecular Weight：564.7354
Target:
L-type calcium channel:4.1 nM (EC50, in depolarized conditions)
L-type calcium channel:33 nM (EC50, in polarized conditions)
In Vivo
SR33805 (20 mg/kg; a single i.p.) improves end-systolic strain and fractional shortening of MI hearts in rats[2]. SR33805 (5 mg/kg/day; p.o. for 38 d) significantly reduces intimal hyperplasia in pigs[3]. Animal Model: Male Wistar rats (5 weeks) are subjected to coronary artery ligature[2] 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.
In Vitro
SR33805 (0.01-10 µM; 3 d) inhibits growth factor-induced proliferation of SMC (0.2050<0.46 µM) in a dose-dependent manner[3]. SR33805 (10 µM; 10 min) restores the myocardial infarction (MI)-altered cell shortening without affecting the Ca2+ transient amplitude[2]. SR33805 (10 µM) decreases the activity of recombinant PKA[2]. Cell Viability Assay[3] 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.
Kinase Assay
Cell Assay
Animal Administration
References
[1]. Romey G, et, al. Effects of two chemically related new Ca2+ channel antagonists, SR33557 (fantofarone) and SR33805, on the L-type cardiac channel. Eur J Pharmacol. 1994 Sep 22; 263(1-2): 101-5.
[2]. Mou YA, et, al. Beneficial effects of SR33805 in failing myocardium. Cardiovasc Res. 2011 Aug 1; 91(3): 412-9.
[3]. Hainaud P, et, al. The calcium inhibitor SR33805 reduces intimal formation following injury of the porcine carotid artery. Atherosclerosis. 2001 Feb 1; 154(2): 301-8.
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