SR33805|CAS 121345-64-0|DC Chemicals

Cas No.:	121345-64-0
Chemical Name:	Benzeneethanamine,3,4-dimethoxy-N-methyl-N-[3-[4-[[1-methyl-2-(1-methylethyl)-1H-indol-3-yl]sulfonyl]phenoxy]propyl]-
SMILES:	CN(CCCOC1=CC=C(C=C1)S(=O)(=O)C2=C(C(C)C)N(C)C3C2=CC=CC=3)CCC4=CC(OC)=C(OC)C=C4
Formula:	C₃₂H₄₀N₂O₅S
M.Wt:	564.7354
Purity:	>98%
Sotrage:	Powder-20°C3 years 4°C2 yearsIn solvent-80°C6 months-20°C1 month

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].
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.
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.

Cat. No.	Product name	Field of application
DC73598	IPPQ	IPPQ is a small molecule that selectively target the interface between the N-type calcium (CaV2.2) channel and CaVβ, specifically binds to CaVβ2a and inhibits CaVβ2's interaction with CaV.2-AID (alpha interacting domain).
DC72651	SG-094	SG094 is a potent TPC2 inhibitor with antiproliferative effects. SG-094 can be used for the research of cancer.
DC70883	VK-II-86	VK-II-86 is a carvedilol analogue lacking antagonist activity at β-adrenoceptors, effectively suppresses SOICR by directly reducing the open duration of the cardiac ryanodine receptor (RyR2).VK-II-86 exhibited >2,000-fold lower beta-AR binding affinity than carvedilol.VK-II-86 prevented stress-induced ventricular tachyarrhythmias in RyR2-mutant mice and did so more effectively when combined with either of the selective beta blockers metoprolol or bisoprolol.VK-II-86 prevented hypokalaemia-induced AP prolongation and depolarization but did not alter AP parameters in normokalaemia.
DC49692	T-Type calcium channel inhibitor(TTA-P2)	T-Type calcium channel inhibitor is a potent inhibitor of T-Type calcium channel. T-Type calcium channel inhibitor penetrates well the CNS and blocks the native T-type currents in deep cerebellar nuclear neurons, the window current is completely abolished both for wild-type and mutant Cav3.1 channels. T-Type calcium channel inhibitor has the potential for the research of neurology disease.
DC44831	MCU-i4	MCU-i4 is a negative modulator of the mitochondrial calcium uniporter (MCU) complex that directly binds a specific cleft in MICU1 and decreases mitochondrial Ca2+ influx.,MCU-i4 decreases mitochondrial Ca2+ influx. Docking simulations reveal that MCU-i4 directly binds a specific cleft in MICU1, a key element of the MCU complex that controls channel gating. Accordingly, in MICU1-silenced or deleted cells, the inhibitory effect of MCU-i4 is lost. Moreover, MCU-i4 fails to inhibit mitochondrial Ca2+ uptake in cells expressing a MICU1 mutated in the critical amino acids that forge the predicted binding cleft.[1]
DC42326	Azumolene	Azumolene (EU4093 free base), a Dantrolene analog, is a muscle relaxant. Azumolene is a ryanodine receptor (RyR) modulator and inhibits the calcium-release through ryanodine receptor. Azumolene can be used for malignant hyperthermia research.
DC41018	SR33805	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.
DC40144	TTA-A2	TTA-A2 is a potent, selective and orally active t-type voltage gated calcium?channel antagonist with reduced pregnane X receptor (PXR) activation. TTA-A2 is equally potent against the Cav3.1 (a1G) and Cav3.2 (a1H) channels with IC50 values of 89 nM and 92 nM, respectively, at -80 and -100 mV holding potentials. TTA-A2 can be used for the research of a variety of human neurological diseases, including sleep disorders and epilepsy.
DC28967	Gallopamil hydrochloride	Gallopamil hydrochloride (Methoxyverapamil hydrochloride), a methoxy derivative of Verapamil, is a phenylalkylamine calcium antagonist. Gallopamil hydrochloride inhibits acid secretion in a concentration-dependent manner with an IC50 of 10.9 μM. Gallopamil hydrochloride is a potent antiarrhythmic and vasodilator agent.
DC10947	FPL64176	FPL64176 is a potent L-type Ca++ channel activator with EC50 of 16 nM.