CGS 27023A

Cat. No.: HY-18694: Ficha de datos Instrucciones de manejo
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CGS 27023A is a non-peptidic and orally active MMP inhibitor with the K_i values of 43, 33, 20 and 8 nM for MMP-3, MMP-1, MMP-2 amd MMP-9, respectively. CGS 27023A prevents cartilage degradation in stromelysin-induced rabbit cartilage degradation model. CGS 27023A can be used for study of arthritis.

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CGS 27023A Estructura química

No. CAS : 169799-04-6

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•Related Small Molecules:

•Related Proteins:

Ver todos los productos específicos de isoformas MMP:

Ver todas las isoformas

MMP-1 MMP-2 MMP-3 MMP-8 MMP-9 MMP-13 MMP-14 MMP-17 ADAM10 ADAM17 MMP-7 MMP-12 MMP-10 MMP ADAM8 MMP-19

Actividad biológica
Pureza y Documentación
Referencias
Revisión del cliente

Descripciòn

IC₅₀ & Target

stromelysins 1

43 nM (Ki)

collagenases 1

33 nM (Ki)

MMP-2

20 nM (Ki)

MMP-9

8 nM (Ki)

Cellular Effect

Cell Line	Type	Value	Description	References
MCF7	IC₅₀	3 μM Compound: 1, CGS-27023A	Inhibition of ADAM17 in human MCF7 cells assessed as inhibition of EGF-induced sALCAM release by ELISA Inhibition of ADAM17 in human MCF7 cells assessed as inhibition of EGF-induced sALCAM release by ELISA	[PMID: 20180536]
MCF7	IC₅₀	3000 nM Compound: 1, CGS-27023A	Inhibition of ADAM17 in human MCF7 cells assessed as inhibition of EGF-induced sALCAM release by ELISA Inhibition of ADAM17 in human MCF7 cells assessed as inhibition of EGF-induced sALCAM release by ELISA	[PMID: 20180536]
MCF7	IC₅₀	6900 nM Compound: 1, CGS-27023A	Inhibition of ADAM17 in human MCF7 cells assessed as inhibition of constitutive sALCAM release by ELISA Inhibition of ADAM17 in human MCF7 cells assessed as inhibition of constitutive sALCAM release by ELISA	[PMID: 20180536]
MCF7	IC₅₀	750 nM Compound: 1, CGS-27023A	Inhibition of ADAM17 in human MCF7 cells assessed as inhibition of pervanadate-induced sALCAM release by ELISA Inhibition of ADAM17 in human MCF7 cells assessed as inhibition of pervanadate-induced sALCAM release by ELISA	[PMID: 20180536]
MDA-MB-468	IC₅₀	10 μM Compound: 1, CGS-27023A	Inhibition of ADAM17 in human MDA-MB-468 cells assessed as inhibition of pervanadate-induced sALCAM release by ELISA Inhibition of ADAM17 in human MDA-MB-468 cells assessed as inhibition of pervanadate-induced sALCAM release by ELISA	[PMID: 20180536]
MDA-MB-468	IC₅₀	10000 nM Compound: 1, CGS-27023A	Inhibition of ADAM17 in human MDA-MB-468 cells assessed as inhibition of pervanadate-induced sALCAM release by ELISA Inhibition of ADAM17 in human MDA-MB-468 cells assessed as inhibition of pervanadate-induced sALCAM release by ELISA	[PMID: 20180536]
MDA-MB-468	IC₅₀	1400 nM Compound: 1, CGS-27023A	Inhibition of ADAM17 in human MDA-MB-468 cells assessed as inhibition of constitutive sALCAM release by ELISA Inhibition of ADAM17 in human MDA-MB-468 cells assessed as inhibition of constitutive sALCAM release by ELISA	[PMID: 20180536]
MDA-MB-468	IC₅₀	750 nM Compound: 1, CGS-27023A	Inhibition of ADAM17 in human MDA-MB-468 cells assessed as inhibition of EGF-induced sALCAM release by ELISA Inhibition of ADAM17 in human MDA-MB-468 cells assessed as inhibition of EGF-induced sALCAM release by ELISA	[PMID: 20180536]
SK-OV-3	IC₅₀	110 nM Compound: 1, CGS-27023A	Inhibition of ADAM17 in human SKOV3 cells assessed as inhibition of EGF-induced sALCAM release by ELISA Inhibition of ADAM17 in human SKOV3 cells assessed as inhibition of EGF-induced sALCAM release by ELISA	[PMID: 20180536]
SK-OV-3	IC₅₀	13 μM Compound: 1, CGS-27023A	Inhibition of ADAM17 in human SKOV3 cells assessed as inhibition of constitutive sALCAM release by ELISA Inhibition of ADAM17 in human SKOV3 cells assessed as inhibition of constitutive sALCAM release by ELISA	[PMID: 20180536]
SK-OV-3	IC₅₀	13000 nM Compound: 1, CGS-27023A	Inhibition of ADAM17 in human SKOV3 cells assessed as inhibition of constitutive sALCAM release by ELISA Inhibition of ADAM17 in human SKOV3 cells assessed as inhibition of constitutive sALCAM release by ELISA	[PMID: 20180536]

In Vivo

CGS 27023A (oral gavage, 75 µmol/kg for 10 h) prevents cartilage degradation in stromelysin-induced rabbit cartilage degradation model^[1].

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

Peso molecular

429.92

Fòrmula

C₁₈H₂₄ClN₃O₅S

No. CAS

169799-04-6

SMILES

CC(C)[C@@H](N(S(=O)(C1=CC=C(OC)C=C1)=O)CC2=CC=CN=C2)C(NO)=O.[H]Cl

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]. MacPherson LJ, et al. Discovery of CGS 27023A, a non-peptidic, potent, and orally active stromelysin inhibitor that blocks cartilage degradation in rabbits. J Med Chem. 1997;40(16):2525-2532. [Content Brief]

CGS 27023A Related Classifications

Inflammation/Immunology

Calculadora de molaridad
Calculadora de dilución

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass		Concentration		Volume		Molecular Weight *
	=		×		×

The dilution calculator equation

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)	×	Volume _(start)	=	Concentration _(final)	×	Volume _(final)
	×		=		×
C1		V1		C2		V2

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:

CGS 27023A169799-04-6MMPMatrix metalloproteinasesstromelysin-induced cartilage degradationarthritisInhibitorinhibitorinhibit

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