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CP-544439
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。
CP-544439图片
CAS NO:230954-09-3

CP-544439 是一种具有口服活性的MMP-13抑制剂,IC50为 0.75 nM。
生物活性

CP-544439 is a potent and orally active matrix metalloproteinase-13(MMP-13)inhibitor with anIC50of 0.75 nM[1][2].

IC50& Target[2][1][1]

MMP-13

0.75 nM (IC50)

MMP-12

0.24 nM (IC50)

MMP-1

420 nM (IC50)

MMP-2

1.6 nM (IC50)

MMP-3

16 nM (IC50)

MMP-8

1.4 nM (IC50)

MMP-9

12 nM (IC50)

MMP-14

7.4 nM (IC50)

体内研究
(In Vivo)

In vivo studies using a hamster model, in which the cartilage collagen degradation was induced by intra-articular injection of recombinant human MMP-13, demonstrated that oral administration of CP-544439 inhibits degradation of the cartilage collagen with an ED50of 14 mg/kg and efficacious plasma concentrations ranging from 0.5 to 1.0 g/ml[1].

分子量

410.42

Formula

C18H19FN2O6S

CAS 号

230954-09-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

 
 
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