MMP13-IN-2

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MMP13-IN-2

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

935759-55-0

包装与价格：

包装	价格(元)
10 mM * 1 mL in DMSO	电议
5mg	电议
10mg	电议
25mg	电议
50mg	电议
100mg	电议

产品介绍

MMP13-IN-2 是一种有效、选择性和口服活性的MMP-13抑制剂。MMP13-IN-2 对 MMP-13 具有优异的效价 (IC₅₀=0.036 nM)，对 MMP-1、3、7、8、9、14 和 TACE 的选择性(大于 1500 倍)。MMP13-IN-2 在体外具有阻止软骨释放胶原蛋白的能力。MMP13-IN-2 具有胶原酶相关疾病研究的潜力。

生物活性

MMP13-IN-2 is a potent, selective and orally activeMMP-13inhibitor. MMP13-IN-2 exhibits excellent potency forMMP-13(IC₅₀=0.036 nM) and selectivities (greater than 1,500-fold) overMMP-1, 3, 7, 8, 9, 14, and TACE. MMP13-IN-2 has the ability to block the release of collagen from cartilage in vitro. MMP13-IN-2 has the potential for collagenase related disease research^[1].

IC₅₀& Target^[1]

MMP-13

0.036 nM (IC₅₀)

MMP-2

180 nM (IC₅₀)

MMP-3

1100 nM (IC₅₀)

体外研究
(In Vitro)

In a bovine nasal cartilage (BNC) assay, the chondrocyte-mediated degradation of cartilage was studied using bovine nasal cartilage slices cultured for up to 14 days. MMP13-IN-2 (0.01-1 μM) is effective at preventing the IL-1/OSM induced in vitro degradation of BNC (-17.6%, 48.4% and 70.8% inhibition of cartilage degradation, respectively).^[1].

体内研究
(In Vivo)

MMP13-IN-2 (oral gavage; 1 mg/kg) shows the best combination of CYP3A4 inhibition risk and oral exposure at a dose of 1 mg/kg in rats and mice (F% = 33 and 38, respectively)^[1].

分子量

506.51

性状

Solid

Formula

C₂₄H₁₉FN₆O₄S

CAS 号

935759-55-0

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

溶解性数据

In Vitro:

DMSO : 100 mg/mL(197.43 mM;ultrasonic and warming and heat to 60℃)

配制储备液

浓度溶剂体积质量

1 mg

5 mg

10 mg

1 mM	1.9743 mL	9.8715 mL	19.7429 mL
5 mM	0.3949 mL	1.9743 mL	3.9486 mL
10 mM	0.1974 mL	0.9871 mL	1.9743 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℃, 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。