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。
| 生物活性 | SR33805 is a potentCa2+channelantagonist, withEC50s 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) |
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体外研究
(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. |
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体内研究
(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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : ≥ 100 mg/mL(177.07 mM) *"≥" means soluble, but saturation unknown. 配制储备液 | 1 mM | 1.7707 mL | 8.8536 mL | 17.7073 mL | | 5 mM | 0.3541 mL | 1.7707 mL | 3.5415 mL | | 10 mM | 0.1771 mL | 0.8854 mL | 1.7707 mL |
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储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.08 mg/mL (3.68 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (3.68 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.08 mg/mL (3.68 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (3.68 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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