1. Membrane Transporter/Ion Channel
    Neuronal Signaling
  2. Calcium Channel
  3. SR33805

SR33805 

目录号: HY-136909 纯度: 99.04%
产品使用指南

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。

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SR33805 Chemical Structure

SR33805 Chemical Structure

CAS No. : 121345-64-0

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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].

IC50 & Target[1]

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.
Molecular Weight

564.74

Formula

C₃₂H₄₀N₂O₅S

CAS No.

121345-64-0

SMILES

O=S(C1=CC=C(OCCCN(C)CCC2=CC=C(OC)C(OC)=C2)C=C1)(C3=C(C(C)C)N(C)C4=C3C=CC=C4)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
References
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Keywords:

SR33805SR 33805SR-33805Calcium ChannelCa2+ channelsCa channelsCa2+channeldepolarizedpolarizedL-typeacutechronicfailingheartsInhibitorinhibitorinhibit

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