SR33805

Names

[ Name ]:
SR33805

[Synonym ]:
3,4-Dimethoxy-N-methyl-N(3-(4-((1-methyl-2-(1-methylethyl)-1H-indol-3-yl)sulfonyl)phenoxy)propyl)benzeneethanamine
Benzeneethanamine,3,4-dimethoxy-N-methyl-N(3-(4-((1-methyl-2-(1-methylethyl)-1H-indol-3-yl)sulfonyl)phenoxy)propyl)
N-[2-(3,4-dimethoxyphenyl)ethyl]-N-methyl-3-(4-{[1-methyl-2-(propan-2-yl)-1H-indol-3-yl]sulfonyl}phenoxy)propan-1-amine

Biological Activity

[Description]:

SR33805 is a potent Ca2+ channel antagonist, with EC50s of 4.1 nM and 33 nM in depolarized and polarized conditions, respectively. SR33805 blocks L-type but not T-type Ca2+ channels. SR33805 can be used for the research of acute or chronic failing hearts[1][2].

[Related Catalog]:

Signaling Pathways >> Membrane Transporter/Ion Channel >> Calcium Channel

Research Areas >> Cardiovascular Disease

[Target]

L-type calcium channel:4.1 nM (EC50, in depolarized conditions)

L-type calcium channel:33 nM (EC50, in polarized conditions)

[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.

[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.

[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.

Chemical & Physical Properties

[ Density]:
1.15g/cm3

[ Boiling Point ]:
724.1ºC at 760mmHg

[ Molecular Formula ]:
C₃₂H₄₀N₂O₅S

[ Molecular Weight ]:
564.73500

[ Flash Point ]:
391.7ºC

[ Exact Mass ]:
564.26600

[ PSA ]:
78.38000

[ LogP ]:
7.17590

[ Vapour Pressure ]:
8.05E-21mmHg at 25°C

[ Index of Refraction ]:
1.57

Related Compounds

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