BMS-582949 hydrochloride|cas:912806-16-7|西域试剂

BMS-582949 hydrochloride,98.29%

产品编号：Bellancom-14305A| CAS NO：912806-16-7| 分子式：C₂₂H₂₇ClN₆O₂| 分子量：442.94

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-14305A	￥1500.00	杭州北京（现货）
Bellancom-14305A	￥2500.00	杭州北京（现货）
Bellancom-14305A	￥5000.00	杭州北京（现货）
Bellancom-14305A	￥7500.00	杭州北京（现货）
Bellancom-14305A	￥12000.00	杭州北京（现货）

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BMS-582949 hydrochloride

产品介绍

BMS-582949 hydrochloride 是具有口服活性的、高度选择性的p38α MAPK 抑制剂，其IC₅₀ 值为13 nM。BMS-582949 hydrochloride 具有明显改善的药代动力学特征，能用于炎症性疾病的研究。

生物活性

BMS-582949 hydrochloride is an orally active and highly selective p38α MAPK inhibitor, with an IC₅₀ of 13 nM. BMS-582949 hydrochloride displays a significantly improved pharmacokinetic profile and is effective in inflammatory disease.

体外研究

BMS-582949 displays a p38α IC₅₀ of 13 nM and a cellular TNFα IC₅₀ of 50 nM.
BMS-582949 is a weak inhibitor of CYP3A4 BMS-582949 displays >2000-fold selectivity for p38α over a diverse panel of 57 kinases that include serine kinases, nonreceptor tyrosine kinases, receptor tyrosine kinases, and the p38γ and δ isoforms.

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

体内研究

BMS-582949 (5-100 mg/kg, orally) is effective in both the acute murine model of inflammation and rat adjuvant arthritis model despite its slightly reduced potency.

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

Animal Model:	Male Sprague-Dawley rats (250-300 g) adjuvant arthritis model.
Dosage:	1, 10, 100 mg/kg.
Administration:	Orally once daily (from day 11 to day 19).
Result:	Displayed dose-dependent reduction in paw swelling with qd dosing, with efficacy observed at doses of 10 and 100 mg/kg.

体内研究

BMS-582949 (5-100 mg/kg, orally) is effective in both the acute murine model of inflammation and rat adjuvant arthritis model despite its slightly reduced potency.

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

Animal Model:	Male Sprague-Dawley rats (250-300 g) adjuvant arthritis model.
Dosage:	1, 10, 100 mg/kg.
Administration:	Orally once daily (from day 11 to day 19).
Result:	Displayed dose-dependent reduction in paw swelling with qd dosing, with efficacy observed at doses of 10 and 100 mg/kg.

性状

Solid

溶解性数据

In Vitro:

DMSO : 25 mg/mL (56.44 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.2576 mL	11.2882 mL	22.5764 mL
5 mM	0.4515 mL	2.2576 mL	4.5153 mL
10 mM	0.2258 mL	1.1288 mL	2.2576 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 90% corn oil
Solubility: ≥ 2.5 mg/mL (5.64 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.64 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 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。