AZD1981
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 510315

CAS#: 802904-66-1

Description: AZD1981is an orally available selective CRTH or DP2 antagonist currently in clinical development for asthma. AZD1981 blocks functional responses in eosinophils, Th2 cells and basophils. AZD1981 displaced radio-labelled PGD2 from human recombinant DP2 with high potency (pIC50 = 8.4). Binding was reversible, non-competitive and highly selective against a panel of more than 340 other enzymes and receptors, including DP1 (>1000-fold selective). AZD1981 inhibited DP2 -mediated shape change and CD11b up-regulation in human eosinophils, shape change in basophils and chemotaxis of human eosinophils and Th2 cells with similar potency. AZD1981 exhibited good cross-species binding activity against mouse, rat, guinea pig, rabbit and dog DP2 . Evaluation in mouse, rat or rabbit cell systems was not possible as they did not respond to DP2 agonists. Agonist responses were seen in guinea pig and dog, and AZD1981 blocked DP2 -mediated eosinophil shape change. Such responses were more robust in the guinea pig, where AZD1981 also blocked DP2 -dependent eosinophil emigration from bone marrow.


Chemical Structure

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AZD1981
CAS# 802904-66-1

Theoretical Analysis

MedKoo Cat#: 510315
Name: AZD1981
CAS#: 802904-66-1
Chemical Formula: C19H17ClN2O3S
Exact Mass: 388.06484
Molecular Weight: 388.87
Elemental Analysis: C, 58.68; H, 4.41; Cl, 9.12; N, 7.20; O, 12.34; S, 8.25

Price and Availability

Size Price Availability Quantity
10.0mg USD 150.0 2 Weeks
25.0mg USD 250.0 2 Weeks
50.0mg USD 450.0 2 Weeks
100.0mg USD 650.0 2 Weeks
200.0mg USD 950.0 2 Weeks
500.0mg USD 1650.0 2 Weeks
1.0g USD 2650.0 2 Weeks
2.0g USD 3850.0 2 Weeks
5.0g USD 6950.0 2 Weeks
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Synonym: AZD1981; AZD-1981; AZD 1981.

IUPAC/Chemical Name: 2-(4-acetamido-3-((4-chlorophenyl)thio)-2-methyl-1H-indol-1-yl)acetic acid

InChi Key: JWYIGNODXSRKGP-UHFFFAOYSA-N

InChi Code: InChI=1S/C19H17ClN2O3S/c1-11-19(26-14-8-6-13(20)7-9-14)18-15(21-12(2)23)4-3-5-16(18)22(11)10-17(24)25/h3-9H,10H2,1-2H3,(H,21,23)(H,24,25)

SMILES Code: O=C(O)CN1C(C)=C(SC2=CC=C(Cl)C=C2)C3=C1C=CC=C3NC(C)=O

Appearance: Solid powder

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

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

Preparing Stock Solutions

The following data is based on the product molecular weight 388.87 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL

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1: Snell N, Foster M, Vestbo J. Efficacy and safety of AZD1981, a CRTH2 receptor antagonist, in patients with moderate to severe COPD. Respir Med. 2013 Nov;107(11):1722-30. doi: 10.1016/j.rmed.2013.06.006. Epub 2013 Jul 1. PubMed PMID: 23827726.

2: Schmidt JA, 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. doi: 10.1111/bph.12053. PubMed PMID: 23146091; PubMed Central PMCID: PMC3605871.

3: Luker T, 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. doi: 10.1016/j.bmcl.2011.08.124. Epub 2011 Sep 5. PubMed PMID: 21944852.

AZD1981

10.0mg / USD 150.0


Additional Information