BI-4394 MMP13-IN-3|cas:1222173-37-6|西域试剂

BI-4394 MMP13-IN-3,99.91%

产品编号：Bellancom-124029| CAS NO：1222173-37-6| 分子式：C₂₄H₂₂N₄O₅| 分子量：446.46

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-124029	￥2400.00	杭州北京（现货）
Bellancom-124029	￥3840.00	杭州北京（现货）
Bellancom-124029	￥11600.00	杭州北京（现货）

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BI-4394 MMP13-IN-3

产品介绍

BI-4394 (MMP13-IN-3) 是一种有效的，具有口服活性的选择性 MMP-13 抑制剂，IC₅₀ 为 1 nM，比作用于其他 MMP 的选择性高 1000倍多。BI-4394 有潜力用于骨关节炎的研究。

生物活性

BI-4394 (MMP13-IN-3) is a potent, selective, and orally active MMP-13 inhibitor (IC₅₀=1 nM) for the potential treatment of osteoarthritis. BI-4394 is >1000 selective over other MMPs.

体外研究

BI-4394 (Compound 15) is potent in a full-length MMP-13 collagen degradation assay (11 nM) and is able to inhibit degradation of bovine nasal cartilage with an IC₅₀ of 31 nM. BI-4394 inhibits MMP-2, MMP-9, MMP-10 and MMP-14 with IC₅₀s of 18, 8.9, 16 and 8.3 μM, respectively.

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

体内研究

When dosed orally at 10 mg/kg or i.v. 1 mg/kg, BI-4394 (Compound 15) reaches micromolar plasma levels (AUC=1109±64 nM h/mL), displays modest clearance (CL=34 mL/min/kg), and shows acceptable bioavailability (39%). The V_ss is quite low at 0.26 mL/mi/kg rat pharmacokinetic profile. BI-4394 has short terminal elimination half-life (t_1/2=0.47 h for rat (1 mg/kg, i.v.) and rat (10 mg/kg, orally), respectively).

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

Animal Model:	Srapgue Dally Rats
Dosage:	10 mg/kg (oral gavage); 1 mg/kg (i.v.)
Administration:	Dosed orally (10 mg/kg); i.v. (1 mg/kg)(Pharmacokinetic Analysis)
Result:	T_1/2=0.47 h for rat (1 mg/kg, i.v.) and rat (10 mg/kg, orally) , respectively.

体内研究

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

Animal Model:	Srapgue Dally Rats
Dosage:	10 mg/kg (oral gavage); 1 mg/kg (i.v.)
Administration:	Dosed orally (10 mg/kg); i.v. (1 mg/kg)(Pharmacokinetic Analysis)
Result:	T_1/2=0.47 h for rat (1 mg/kg, i.v.) and rat (10 mg/kg, orally) , respectively.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (223.98 mM; ultrasonic and warming and heat to 60°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.2398 mL	11.1992 mL	22.3984 mL
5 mM	0.4480 mL	2.2398 mL	4.4797 mL
10 mM	0.2240 mL	1.1199 mL	2.2398 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。-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。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式