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Cat. No.: HY-153505

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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.

CAS No.: 1607004-34-1
Formula: C₂₀H₂₂F₃N₃O₃
Molecular Weight:409.40

Storage:

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

ADAMTS-4/5-IN-1 Chemical Structure

CAS No.: 1607004-34-1

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

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.

Parmacokinetics

Species	Dose	Route	C_max	AUC_0-24	T_1/2	CL	V_d	Plasma Concentration	T_max	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.

Chemical Information

CAS No. 1607004-34-1
Molecular Weight 409.40
Formula C₂₀H₂₂F₃N₃O₃
SMILES

FC(F)(F)C(C=C1)=CC=C1C[C@@H](C2CC2)C(NC[C@@]3(C4CC4)NC(NC3=O)=O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Durham TB, et al. A Highly Selective Hydantoin Inhibitor of Aggrecanase-1 and Aggrecanase-2 with a Low Projected Human Dose. J Med Chem. 2017;60(13):5933-5939. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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