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AZD1981

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Catalog No. T6399Cas No. 802904-66-1

AZD1981 is an effective and specific CRTh2 (DP2) receptor antagonist (IC50: 4 nM), showing >1000-fold selectivity over more than 340 other enzymes and receptors, including DP1. AZD1981 has been used in trials studying the treatment and basic science of Asthma, Postmenopausal, Pharmakokinetic, Asthma Patients, and Drug Interaction, among others.

AZD1981

AZD1981

🥰Excellent
Purity: 99.54%
Catalog No. T6399Cas No. 802904-66-1
AZD1981 is an effective and specific CRTh2 (DP2) receptor antagonist (IC50: 4 nM), showing >1000-fold selectivity over more than 340 other enzymes and receptors, including DP1. AZD1981 has been used in trials studying the treatment and basic science of Asthma, Postmenopausal, Pharmakokinetic, Asthma Patients, and Drug Interaction, among others.
Pack SizePriceAvailabilityQuantity
10 mg44 €In Stock
25 mg93 €In Stock
50 mg182 €In Stock
100 mg274 €In Stock
200 mg400 €In Stock
1 mL x 10 mM (in DMSO)27 €In Stock
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Purity:99.54%
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Product Introduction

Bioactivity
Description
AZD1981 is an effective and specific CRTh2 (DP2) receptor antagonist (IC50: 4 nM), showing >1000-fold selectivity over more than 340 other enzymes and receptors, including DP1. AZD1981 has been used in trials studying the treatment and basic science of As
Targets&IC50
CRTh2 (DP2) receptor:4 nM
In vitro
AZD1981, as a potent antagonist in a disease relevant cell system, inhibits DK-PGD2-induced CD11b expression in human eosinophils with IC50 of 10 nM. [1] AZD1981 blocks DP2-mediated shape change in human eosinophils and basophils in blood, as well as DP2-mediated chemotaxis of human Th2 cells and eosinophils. Moreover, AZD1981 also blocks the binding of [3H]PGD2 to mouse, rat, guinea pig, rabbit and dog recombinant DP2. [2]
In vivo
AZD1981 has high oral bioavailability in male sprague dawley rats. [1] In guinea pig hind limb model, AZD1981 (100 nM) completely inhibits DK-PGD2-induced eosinophil mobilization. [2]
Chemical Properties
Molecular Weight388.87
FormulaC19H17ClN2O3S
Cas No.802904-66-1
SmilesCC(=O)Nc1cccc2n(CC(O)=O)c(C)c(Sc3ccc(Cl)cc3)c12
Relative Density.1.37 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
H2O: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 9 mg/mL (23.1 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.5716 mL12.8578 mL25.7155 mL128.5777 mL
5 mM0.5143 mL2.5716 mL5.1431 mL25.7155 mL
10 mM0.2572 mL1.2858 mL2.5716 mL12.8578 mL
20 mM0.1286 mL0.6429 mL1.2858 mL6.4289 mL

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Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify
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