research use only

AZD1981 GPR antagonist

Cat.No.S7263

AZD1981 is a potent, selective CRTh2 (DP2) receptor antagonist with IC50 of 4 nM, showing >1000-fold selectivity over more than 340 other enzymes and receptors, including DP1. Phase 2.

Chemical Structure

Molecular Weight: 388.87

Jump to

Quality Control

Batch: S726301 DMSO]11 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.82%

Cited in Nature Medicine for its top-tier quality
COA
NMR
SDS
Datasheet

99.82

Related Targets	Adrenergic Receptor Estrogen/progestogen Receptor Androgen Receptor Glucocorticoid Receptor ACE RAAS Progesterone Receptor Opioid Receptor PGES THR
Other GPR Inhibitors	ONC212 Fasiglifam(TAK-875) Hemihydrate GW9508 AH7614 3-chloro-5-hydroxybenzoic Acid JMS-17-2 GSK1292263 TC-G-1008 (GPR39-C3) SNAP94847 hydrochloride 6-OAU

Chemical Information, Storage & Stability

Molecular Weight	388.87	Formula	C₁₉H₁₇ClN₂O₃S	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	802904-66-1	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CC1=C(C2=C(C=CC=C2N1CC(=O)O)NC(=O)C)SC3=CC=C(C=C3)Cl

Solubility

In vitro
Batch:

DMSO : 11 mg/mL (28.28 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Features	An orally available selective DP2(CRTh2) receptor antagonist in clinical development for asthma.
Targets/IC₅₀/Ki	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. This compound 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, it also blocks the binding of [³H]PGD2 to mouse, rat, guinea pig, rabbit and dog recombinant DP2.
In vivo	AZD1981 has high oral bioavailability in male sprague dawley rats. In guinea pig hind limb model, this compound (100 nM) completely inhibits DK-PGD2-induced eosinophil mobilization.
References	[1] https://pubmed.ncbi.nlm.nih.gov/21944852/ [2] https://pubmed.ncbi.nlm.nih.gov/23146091/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT02367066	Completed	Type 2 Diabetes Mellitus	AstraZeneca	March 2015	Phase 1
NCT02031679	Completed	Chronic Idiopathic Urticaria	Johns Hopkins University\|AstraZeneca	January 2014	Phase 2
NCT01199341	Completed	Pharmakokinetic	AstraZeneca	October 2010	Phase 1
NCT01196689	Completed	Asthma	AstraZeneca	October 2010	Phase 1

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):