AMG 853 - ≥98%(HPLC), high purity , G protein-coupled receptor 44 antagonist, CAS No.1169483-24-2, G protein-coupled receptor 44 antagonist

Item Number
A286753
Grouped product items
SKUSizeAvailabilityPrice Qty
A286753-5mg
5mg
In stock
$166.90
A286753-10mg
10mg
In stock
$277.90
A286753-25mg
25mg
In stock
$625.90
A286753-50mg
50mg
In stock
$789.90
A286753-100mg
100mg
In stock
$1,251.90

Potent dual CRTH2 and prostaglandin D2(PGD2) receptor antagonist

Basic Description

Synonyms2-[4-[4-(tert-butylcarbamoyl)-2-[(2-chloro-4-cyclopropylphenyl)sulfonylamino]phenoxy]-5-chloro-2-fluorophenyl]acetic acid | 2-(4-(4-(tert-butylcarbamoyl)-2-((2-chloro-4-cyclopropylphenyl)sulfonamido)phenoxy)-5-chloro-2-fluorophenyl)acetic acid | 2-(4-(4-(
Specifications & PurityMoligand™, ≥98%(HPLC)
Biochemical and Physiological MechanismsPotent prostaglandin D2(PGD2, CRTH2) receptor antagonist (IC50values are 8 and 35 nM, respectively in plasma). Inhibits PGD2-induced down modulation of CRTH2 on CD16-granulocytes in human whole blood as well as PGD2-induced cAMP response in platelets. Inh
Storage TempStore at -20°C
Shipped InIce chest + Ice pads
GradeMoligand™
Action TypeANTAGONIST
Mechanism of actionG protein-coupled receptor 44 antagonist

Product Properties

ALogP6

Associated Targets(Human)

PTGDR Tclin Prostaglandin D2 receptor (3 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
PTGDR2 Tchem Prostaglandin D2 receptor 2 (3 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
CYP2C8 Tchem Cytochrome P450 2C8 (1492 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CYP2D6 Tclin Cytochrome P450 2D6 (33882 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CYP1A2 Tchem Cytochrome P450 1A2 (26471 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
PTGDR Tclin Prostanoid DP receptor (1356 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CYP3A5 Tclin Cytochrome P450 3A5 (525 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
UGT1A4 Tbio UDP-glucuronosyltransferase 1A4 (288 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CYP2C9 Tchem Cytochrome P450 2C9 (32119 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CYP2C19 Tchem Cytochrome P450 2C19 (29246 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CYP3A4 Tclin Cytochrome P450 3A4 (53859 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CYP2E1 Tchem Cytochrome P450 2E1 (2174 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CYP2B6 Tchem Cytochrome P450 2B6 (1338 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
PTGDR2 Tchem G protein-coupled receptor 44 (4688 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Homo sapiens (32628 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CYP2J2 Tchem Cytochrome P450 2J2 (258 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
UGT2B7 Tchem UDP-glucuronosyltransferase 2B7 (787 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
UGT2B17 Tbio UDP-glucuronosyltransferase 2B17 (197 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
UGT2B4 Tbio UDP-glucuronosyltransferase 2B4 (139 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
UGT2B15 Tbio UDP-glucuronosyltransferase 2B15 (172 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
UGT1A1 Tchem UDP-glucuronosyltransferase 1-1 (448 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
UGT1A6 Tbio UDP-glucuronosyltransferase 1-6 (221 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
UGT1A7 Tbio UDP-glucuronosyltransferase 1-7 (106 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
UGT1A8 Tbio UDP-glucuronosyltransferase 1-8 (233 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
UGT1A9 Tbio UDP-glucuronosyltransferase 1-9 (343 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
UGT1A10 Tbio UDP-glucuronosyltransferase 1-10 (257 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CYP3A7 Tclin Cytochrome P450 3A7 (35 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
UGT1A3 Tbio UDP-glucuronosyltransferase 1-3 (217 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Associated Targets(non-human)

CAPN1 Calpain 1 (219 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Cavia porcellus (23802 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Canis familiaris (36305 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Rattus norvegicus (775804 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Cynomolgus monkey (4946 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Liver microsome (341 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Mechanisms of Action

Mechanism of ActionAction Typetarget IDTarget NameTarget TypeTarget OrganismBinding Site NameReferences

Names and Identifiers

IUPAC Name 2-[4-[4-(tert-butylcarbamoyl)-2-[(2-chloro-4-cyclopropylphenyl)sulfonylamino]phenoxy]-5-chloro-2-fluorophenyl]acetic acid
INCHI InChI=1S/C28H27Cl2FN2O6S/c1-28(2,3)32-27(36)17-6-8-23(39-24-14-21(31)18(11-19(24)29)13-26(34)35)22(12-17)33-40(37,38)25-9-7-16(10-20(25)30)15-4-5-15/h6-12,14-15,33H,4-5,13H2,1-3H3,(H,32,36)(H,34,35)
InChi Key PFWVGKROPKKEDW-UHFFFAOYSA-N
Canonical SMILES CC(C)(C)NC(=O)C1=CC(=C(C=C1)OC2=C(C=C(C(=C2)F)CC(=O)O)Cl)NS(=O)(=O)C3=C(C=C(C=C3)C4CC4)Cl
Isomeric SMILES CC(C)(C)NC(=O)C1=CC(=C(C=C1)OC2=C(C=C(C(=C2)F)CC(=O)O)Cl)NS(=O)(=O)C3=C(C=C(C=C3)C4CC4)Cl
PubChem CID 42641863
Molecular Weight 609.49

Certificates

Certificate of Analysis(COA)

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5 results found

Lot NumberCertificate TypeDateItem
K2217140Certificate of AnalysisAug 22, 2022 A286753
K2217141Certificate of AnalysisAug 22, 2022 A286753
K2217142Certificate of AnalysisAug 22, 2022 A286753
K2217150Certificate of AnalysisAug 22, 2022 A286753
K2217151Certificate of AnalysisAug 22, 2022 A286753

Chemical and Physical Properties

SolubilitySolvent:DMSO, Max Conc. mg/mL: 60.95, Max Conc. mM: 100; Solvent:ethanol, Max Conc. mg/mL: 60.95, Max Conc. mM: 100

Related Documents

References

1. Busse WW, Wenzel SE, Meltzer EO, Kerwin EM, Liu MC, Zhang N, Chon Y, Budelsky AL, Lin J, Lin SL.  (2013)  Safety and efficacy of the prostaglandin D2 receptor antagonist AMG 853 in asthmatic patients..  J Allergy Clin Immunol,  131  (2): (339-45).  [PMID:23174659] [10.1021/op500134e]
2. Liu J, Li AR, Wang Y, Johnson MG, Su Y, Shen W, Wang X, Lively S, Brown M, Lai S et al..  (2011)  Discovery of AMG 853, a CRTH2 and DP Dual Antagonist..  ACS Med Chem Lett,  (5): (326-30).  [PMID:24900313] [10.1021/op500134e]

Solution Calculators