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802904-66-1 (AZD1981)

1

Identification

AZD1981 AZD1981
Name AZD1981
Formula C19H17ClN2O3S
MW 388.87
CAS No. 802904-66-1
EINECS
Smiles O=C(O)CN1C(C)=C(SC2=CC=C(Cl)C=C2)C3=C1C=CC=C3NC(C)=O
Synonyms AZD 1981;AZD-1981; 2-(4-acetamido-3-((4-chlorophenyl)thio)-2-methyl-1H-indol-1-yl)acetic acid
InChI 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)
2

Introduction

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.

Background Information

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. 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. what's more, AZD1981 also blocks the binding of [3H]PGD2 to mouse, rat, guinea pig, rabbit and dog recombinant DP2. In guinea pig hind limb model, AZD1981 (100 nM) completely inhibits DK-PGD2-induced eosinophil mobilization. ......by AbMole BioScience
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. ......by AdooQ BioScience, LLC
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. ......by BOC Sciences
AZD-1981 is a potent and selective antagonist of the chemoattractant receptor-homologous expressed on Th2 lymphocytes receptor (CRTh2 or DP2) with an IC₅₀ value of 4 nM; blocks functional responses in eosinophils, Th2 cells and basophils. It exhibits similar potency irrespective of the cell type, DP2 agonist or species used. ......by BioVision, Inc.,
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. ......by MedKoo Biosciences, Inc.
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. ......by Selleck Chemicals LLC
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. ......by Target Molecule Corp.
3

Protocol(Only for Reference)

Cell Experiment

Animal Experiment

Animal Models Male sprague dawley rats.
Dosage 1 mg/kg(i.v.), 4 mg/kg(oral)
Formulation
Administration i.v. or oral administration
Source Selleck Chemicals LLC
4

Physical and Chemical Properties

Appearance:White to off-white Solid EBNumber:EB000011579

Storage condition

4°C by MedChemexpress Co., Ltd.

Solubility

DMSO:30mg/mL by CHEMSCENE, LLC
DMSO:30mg/mL by MedChemexpress Co., Ltd.
(25°C) * In vitro DMSO 11 mg/mL (28.28 mM); Water<1 mg/mL (<1 mM); Ethanol<1 mg/mL (<1 mM) by Selleck Chemicals LLC
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Mechanism and Indication

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Clinical Information

Product Name Sponsor & Collaborators Indications Start Date End Date Phase
AZD1981 AstraZeneca Healthy 2011/3/3 Phase 1
AZD1981 AstraZeneca Healthy 2009/6/10 Phase 1
AZD1981 AstraZeneca Chronic Idiopathic Urticaria 2014/1/7 Phase 2
AZD1981 - Phase 2 Clinical
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Safety Data of AZD1981

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Spectral Information

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Suppliers List

Company Price and Availability Country/Region
AbMole BioScience 10mg/USD180();25mg/USD280() USA
AdooQ BioScience, LLC 5mg/USD48() USA
Apexbio Technology LLC 5mg/USD68(In stock);25mg/USD259(In stock) USA
Ark Pharm, Inc. USA
Axon Medchem BV 5mg/USD126(In Stock) Netherlands
BOC Sciences
BioVision, Inc., USA
Biochempartner Co., Ltd China
CHEMSCENE, LLC 5mg/USD78();10mg/USD132() USA
Cayman Chemical Company USA
Lancrix Chemicals. 5mg/USD108();25mg/USD324();100mg/USD770() China
MedChemexpress Co., Ltd. 5mg/USD78();10mg/USD132() USA
MedKoo Biosciences, Inc. 10mg/USD150();25mg/USD250();50mg/USD450();100mg/USD650();200mg/USD950();500mg/USD1650();1g/USD2850() USA
Selleck Chemicals LLC 5mg/USD97(In stock);25mg/USD370(In stock) USA
Shanghai Haoyuan Chemexpress Co., Ltd. 5mg/USD78();10mg/USD132() China
Target Molecule Corp. 10mg/USD110();50mg/USD410();100mg/USD768() USA
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Related Products

Other Forms of 802904-66-1

Name CAS No Formula MW

Recommended Compounds in CRTH2 (GPR44)

Name CAS No Formula MW
NVP-QAV680 872365-16-7 C18H18N2O4S 358.4115
Fevipiprant 872365-14-5 C19H17F3N2O4S 426.41

Recommended Compounds in Same Indication

Name CAS No Formula MW
VGX-1027 6501-72-0 C11H11NO3 205.21
4-Thiazolidinone, 5-[[3-chloro-4-[(2R)-2,3-dihydroxypropoxy]phenyl]methylene]-3-(2-methylphenyl)-2-(propylimino)-, (2Z,5Z)- 854107-55-4 C22H23ClN2O4S 446.95
RSV604 676128-63-5 C22H17FN4O2 388.39
Cilobradine (hydrochloride) 186097-54-1 C28H39ClN2O5 519.07
Vipadenant 442908-10-3 C16H15N7O 321.3366
Cilobradine 147541-45-5 C28H38N2O5 482.61
PF-04418948 1078166-57-0 C23H20FNO5 409.41
JNJ-40411813 1127498-03-6 C20H25ClN2O 344.88
GLPG0634 1206161-97-8 C21H23N5O3S 425.504
GLPG0492 1215085-92-9 C19H14F3N3O3 389.328
BI 224436 1155419-89-8 C27H26N2O4 442.51
Heparin 9005-49-6 C26H42N2O37S5 1134.93
Vadadustat 1000025-07-9 C14H11ClN2O4 0.0
MGB-BP-3 1000277-08-6 C36H37N7O4 631.72
VITAMIN K1 12001-79-5 C31H46O2 450.7
Tenapanor 1234423-95-0 C50H66Cl4N8O10S2 1145.05
GLPG0187 1320346-97-1 C29H37N7O5S 595.71
Iberdomide 1323403-33-3 C25H27N3O5 449.49898
Fradafiban 148396-36-5 C20H21N3O4 367.4
Terbogrel 149979-74-8 C23H27N5O2 405.49
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Route of Synthesis

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References

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More Information

AZD1981

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