Cinanserin hydrochloride SQ 10643|cas:54-84-2|西域试剂

Cinanserin hydrochloride SQ 10643,99.74%

产品编号：Bellancom-100943| CAS NO：54-84-2| 分子式：C₂₀H₂₅ClN₂OS| 分子量：376.94

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货号	价格	库存与货期
Bellancom-100943	￥2550.00	杭州北京（现货）
Bellancom-100943	￥6500.00	杭州北京（现货）
Bellancom-100943	￥9750.00	杭州北京（现货）

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Cinanserin hydrochloride SQ 10643

产品介绍

Cinanserin hydrochloride (SQ 10643) 是一种有效，选择性和高度亲和力的 5-HT₂ 受体拮抗剂，K_i 为 41 nM。Cinanserin hydrochloride 对 5-HT₂ 的结合亲和力比对 5-HT₁ 受体 (K_i 为 3500 nM) 的结合亲和力高得多。Cinanserin hydrochloride 还是COVID-19 病毒的 3C 样蛋白酶 (3C-like proteinase) 的抑制剂，可大大减少体外的病毒复制。

生物活性

Cinanserin hydrochloride (SQ 10643) is a potent, selective and highly affinity 5-HT₂ receptor antagonist with a K_i of 41 nM. Cinanserin hydrochloride has a much higher binding affinity for the 5-HT₂ than for the 5-HT₁ receptor (K_i of 3500 nM). Cinanserin is also an inhibitor of 3C-like proteinase of severe acute respiratory syndrome coronavirus and strongly reduces virus replication in vitro.

体外研究

Cinanserin/Cinanserin hydrochloride have binding affinity to SARS-CoV 3CL^pro, HCoV-229E 3CL^pro, with the K_D values of 49.4 μM/78.0 μM for SARS-associated coronavirus (SARS-CoV) 3CL^pro and 18.2 μM/36.6 μM for human coronavirus 229E (HCoV-229E) 3CL^pro.
The IC₅₀ values of Cinanserin and Cinanserin hydrochloride for inhibiting the catalytic activity of SARS-CoV 3CL^pro are calculated as 4.92 μM and 5.05 μM, respectively, The corresponding IC₅₀ values for HCoV-229E 3CL^pro are 4.68 μM and 5.68 μM. None of the compounds have inhibitory activity against HRV-14 3C^pro at concentrations up to 200 μM.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

Cinanserin (5 mg/kg; intravenous injection; for 2 hours; male Wistar rats) treatment significantly reduces systemic burn edema to shamburn levels. Leukocyte-endothelial interactions are significantly reduced by administration of Cinanserin.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male Wistar rats (250 g) underwent thermal injury
Dosage:	5 mg/kg
Administration:	Intravenous injection; for 2 hours
Result:	Significantly reduced systemic burn edema to shamburn levels..

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male Wistar rats (250 g) underwent thermal injury
Dosage:	5 mg/kg
Administration:	Intravenous injection; for 2 hours
Result:	Significantly reduced systemic burn edema to shamburn levels..

性状

Solid

溶解性数据

In Vitro:

DMSO : 125 mg/mL (331.62 mM; Need ultrasonic)

H₂O : 100 mg/mL (265.29 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.6529 mL	13.2647 mL	26.5294 mL
5 mM	0.5306 mL	2.6529 mL	5.3059 mL
10 mM	0.2653 mL	1.3265 mL	2.6529 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 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 (5.52 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.52 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。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (5.52 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.52 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 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (5.52 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.52 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。