2. Metabolic Enzyme/Protease
  3. ADAMTS
  4. ADAMTS-4/5-IN-1

ADAMTS-4/5-IN-1 is an orally active, and selective dual ADAMTS-4/5 inhibitor with IC50 values of 2 nM for human ADAMTS-4 and human ADAMTS-5, respectively. ADAMTS-4/5-IN-1 exhibits high selectivity against MMP enzymes. ADAMTS-4/5-IN-1 reduces aggrecan degradation products in synovial fluid. ADAMTS-4/5-IN-1 can be used for the research of osteoarthritis.

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

ADAMTS-4/5-IN-1

ADAMTS-4/5-IN-1 Chemical Structure

CAS No. : 1607004-34-1

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ADAMTS-4/5-IN-1 Related Antibodies

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Description

ADAMTS-4/5-IN-1 is an orally active, and selective dual ADAMTS-4/5 inhibitor with IC50 values of 2 nM for human ADAMTS-4 and human ADAMTS-5, respectively. ADAMTS-4/5-IN-1 exhibits high selectivity against MMP enzymes. ADAMTS-4/5-IN-1 reduces aggrecan degradation products in synovial fluid. ADAMTS-4/5-IN-1 can be used for the research of osteoarthritis[1].

In Vitro

ADAMTS-4/5-IN-1 (Compound 7) potently inhibits human ADAMTS-5 in rat plasma (IC50 = 18 nM), while displaying high selectivity against multiple human MMP enzymes[1].

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

ADAMTS-4/5-IN-1 Related Antibodies
Parmacokinetics
Species Dose Route Cmax AUC0-24 T1/2 CL Vd Plasma Concentration Tmax F
Rat[1] 1 mg/kg i.v. 1600 nM 1300 nM·h 1.5 h 33 mL/min/kg 4.3 L/kg <5 nM / /
Rat[1] 10 mg/kg p.o. 6600 nM 22000 nM·h 2.6 h / / 29 nM 0.5 h 100 %
In Vivo

ADAMTS-4/5-IN-1 (compound 7) (10-75 mg/kg; i.g.; b.i.d.; day 3 to day 7) produces reductions in aggrecan cleavage fragments in a rat osteoarthritis model[1].

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

Animal Model: Male Lewis rats (7-8 weeks old) induced with monoiodoacetate (MIA)[1]
Dosage: 10; 30; 75 mg/kg
Administration: i.g.; b.i.d.; day 3 to day 7
Result: Reduced synovial fluid ARGNV (aggrecan cleavage fragment) levels.
Produced statistically significant reductions at all tested doses.
Molecular Weight

409.40

Formula

C20H22F3N3O3
CAS No.
SMILES

FC(F)(F)C(C=C1)=CC=C1C[C@@H](C2CC2)C(NC[C@@]3(C4CC4)NC(NC3=O)=O)=O
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Room temperature in continental US; may vary elsewhere.
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Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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ADAMTS-4/5-IN-1 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

ADAMTS-4/5-IN-11607004-34-1ADAMTSAdamalysin-like metalloproteinase with thrombospondin motifsMMP enzymesratsosteoarthritisrat plasmarat MIA modelADAMTS-5ADAMTS-4synovial fluidaggrecan degradation productsInhibitorinhibitorinhibit

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