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AZD1981

Catalog No.
B1534
CRTh2 antagonist,potent and selective
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$80.00
In stock
5mg
$68.00
In stock
25mg
$259.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

AZD1981 is a selective, orally bioavailable and potent antagonist of the chemoattractant receptor-homologous expressed on Th2 lymphocytes receptor (CRTh2 or DP2) with an IC50 value of 4 nM [1].

AZD1981 has shown to inhibit eosinophil migration with a pIC50 value of 7.6±0.1. AZD1981 could block chemotaxis of DP2+ T-cell lines with a pIC50 value of 7.5±0.1. AZD1981 has been demonstrated to inhibit PGD2 binding to mouse, rat, rabbit, dog, guinea pig and human DP2. AZD1981 could inhibit shape change induced by DP2 in dog and guinea pig granulocytes as well as in human eosinophils and basophils in blood [2].

References:
[1] Luker T1, Bonnert R, Brough S, Cook AR, Dickinson MR, Dougall I, Logan C, Mohammed RT, Paine S, Sanganee HJ, Sargent C, Schmidt JA,Teague S, Thom S. Substituted indole-1-acetic acids as potent and selective CRTh2 antagonists-discovery of AZD1981. Bioorg Med Chem Lett. 2011 Nov 1;21(21):6288-92.
[2] Schmidt JA1, Bell FM, Akam E, Marshall C, Dainty IA, Heinemann A, Dougall IG, Bonnert RV, Sargent CA. Biochemical and pharmacological characterization of AZD1981, an orally available selective DP2 antagonist in clinical development for asthma. Br J Pharmacol. 2013 Apr;168(7):1626-38.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt388.87
Cas No.802904-66-1
FormulaC19H17ClN2O3S
Solubilityinsoluble in H2O; insoluble in EtOH; ≥19.8 mg/mL in DMSO
Chemical Name2-[4-acetamido-3-(4-chlorophenyl)sulfanyl-2-methylindol-1-yl]acetic acid
SDFDownload SDF
Canonical SMILESCC1=C(C2=C(N1CC(=O)O)C=CC=C2NC(=O)C)SC3=CC=C(C=C3)Cl
Shipping ConditionShip with blue ice, or upon other requests.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. We do not recommend long-term storage for the solution, please use it up soon.

Quality Control

Quality Control & MSDS

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Chemical structure

AZD1981