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

MMP13-IN-3 

Cat. No.: HY-124029
Handling Instructions

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

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

MMP13-IN-3 Chemical Structure

MMP13-IN-3 Chemical Structure

CAS No. : 1222173-37-6

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Description

MMP13-IN-3 is a potent, selective, and orally active MMP-13 inhibitor (IC50=1 nM[1]) for the potential treatment of osteoarthritis[2]. MMP13-IN-3 is >1000 selective over other MMPs[1].

IC50 & Target[1]

MMP-13

1 nM (IC50)

MMP-14

8.3 μM (IC50)

MMP-9

8.9 μM (IC50)

MMP-10

16 μM (IC50)

MMP-2

18 μM (IC50)

In Vitro

MMP13-IN-3 (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. MMP13-IN-3 inhibits MMP-2, MMP-9, MMP-10 and MMP-14 with IC50s of 18, 8.9, 16 and 8.3 μM, respectively[1].

In Vivo

When dosed orally at 10 mg/kg or i.v. 1 mg/kg, MMP13-IN-3 (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 Vss is quite low at 0.26 mL/mi/kg rat pharmacokinetic profile. MMP13-IN-3 has short terminal elimination half-life (t1/2=0.47 h for rat (1 mg/kg, i.v.) and rat (10 mg/kg, orally), respectively)[1].

Animal Model: Srapgue Dally Rats[1]
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: T1/2=0.47 h for rat (1 mg/kg, i.v.) and rat (10 mg/kg, orally) , respectively.
Molecular Weight

446.46

Formula

C₂₄H₂₂N₄O₅

CAS No.

1222173-37-6

SMILES

O=C(C(N1)=CC2=C1C=CC(C3=CC(C(NCC4=CC=C(C(O)=O)C=C4)=O)=NN3C)=C2)OCC

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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Keywords:

MMP13-IN-3MMPMatrix metalloproteinasesMMP-13osteoarthritisInhibitorinhibitorinhibit

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