AMG-009


Catalog No. Size PriceQuantity
M18711-C Contact sales@xcessbio.com for quotation $100Unavailable

Description

AMG-009 is a potent antagonist of prostaglandin D2, with IC50 of 3 nM and 12 nM for CRTH2 and DP receptors, respectively.

Product information

CAS Number: 1027847-67-1

Molecular Weight: 581.46

Formula: C26H26Cl2N2O7S

Chemical Name: 2-{4-[4-(butylcarbamoyl)-2-(2,4-dichlorobenzenesulfonamido)phenoxy]-3-methoxyphenyl}acetic acid

Smiles: COC1=CC(CC(O)=O)=CC=C1OC1=CC=C(C=C1NS(=O)(=O)C1=CC=C(Cl)C=C1Cl)C(=O)NCCCC

InChiKey: DKSKRBVXRDGYAS-UHFFFAOYSA-N

InChi: InChI=1S/C26H26Cl2N2O7S/c1-3-4-11-29-26(33)17-6-9-21(37-22-8-5-16(13-25(31)32)12-23(22)36-2)20(14-17)30-38(34,35)24-10-7-18(27)15-19(24)28/h5-10,12,14-15,30H,3-4,11,13H2,1-2H3,(H,29,33)(H,31,32)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

AMG-009 inhibits PGD2-induced down-modulation of CRTH2 on CD16 negative granulocytes (eosinophils) in human whole blood with a Ki of 1 nM. AMG 009 also inhibits PGD2-induced cAMP response mediated by DP in platelets in 80% human whole blood with a Ki of 148 nM. AMG 009 inhibits guinea pig CRTH2 receptors (IC50=3 nM) and a PGD2-induced cAMP response assay with cells expressing the guinea pig DP receptors (Ki=131 nM).

In Vivo:

AMG 009 (3, 10 or 30 mg/kg, s.c.) results in a dose dependent decrease in airway resistance provoked by PGD2 aerosol in an acute guinea pig model. In a guinea pig model of PGD2-induced airway constriction, AMG 009 significantly improves DP potency, with Kb of 82 nM.

Products are for research use only. Not for human use.

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