1. Metabolic Enzyme/Protease
  2. MMP
  3. MMP13-IN-2

MMP13-IN-2 

Cat. No.: HY-122624
Handling Instructions

MMP13-IN-2 is a potent, selective and orally active MMP-13 inhibitor. MMP13-IN-2 exhibits excellent potency for MMP-13 (IC50=0.036 nM) and selectivities (greater than 1,500-fold) over MMP-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.

For research use only. We do not sell to patients.

MMP13-IN-2 Chemical Structure

MMP13-IN-2 Chemical Structure

CAS No. : 935759-55-0

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Description

MMP13-IN-2 is a potent, selective and orally active MMP-13 inhibitor. MMP13-IN-2 exhibits excellent potency for MMP-13 (IC50=0.036 nM) and selectivities (greater than 1,500-fold) over MMP-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)

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].

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

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].

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

Molecular Weight

506.51

Formula

C₂₄H₁₉FN₆O₄S

CAS No.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

References
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Product Name:
MMP13-IN-2
Cat. No.:
HY-122624
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