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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。
MMP13-IN-2图片
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°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 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 mg5 mg10 mg
1 mM1.9743 mL9.8715 mL19.7429 mL
5 mM0.3949 mL1.9743 mL3.9486 mL
10 mM0.1974 mL0.9871 mL1.9743 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。