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Referencia número: 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.

Para uso exclusivo en investigación. No vendemos a pacientes.

No. CAS: 1607004-34-1
Fòrmula: C₂₀H₂₂F₃N₃O₃
Peso molecular:409.40

Almacenamiento:

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

ADAMTS-4/5-IN-1 Chemical Structure

No. CAS: 1607004-34-1

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Use of MCE Products

Fluorescent Dye

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

Actividad biológica
- Descripciòn
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Pureza y Documentación
Referencias
Calculators
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

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

No. CAS 1607004-34-1
Peso molecular 409.40
Fòrmula C₂₀H₂₂F₃N₃O₃
SMILES

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

Room temperature in continental US; may vary elsewhere.
Almacenamiento

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

Pureza y Documentación

Instrucciones de manejo (2659 KB)

Referencias

[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]

Calculators

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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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100 mg

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