A 943931 - CAS 1027330-97-7
Category: Inhibitor
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Molecular Formula:
C17H21N5
Molecular Weight:
295.38
COA:
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Targets:
Histamine Receptor
Description:
A 943931 is a potent and selective histamine H4 receptor antagonist.
Brife Description:
histamine H4 receptor antagonist
Purity:
99%
Synonyms:
A-943931; D0P8DW; 4-[(3R)-3-aminopyrrolidin-1-yl]-6,7-dihydro-5H-benzo[1,2]cyclohepta[3,4-b]pyrimidin-2-amine
MSDS:
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InChIKey:
SDTRYHWIXVHTLM-GFCCVEGCSA-N
InChI:
InChI=1S/C17H21N5/c18-12-8-9-22(10-12)16-14-7-3-5-11-4-1-2-6-13(11)15(14)20-17(19)21-16/h1-2,4,6,12H,3,5,7-10,18H2,(H2,19,20,21)/t12-/m1/s1
Canonical SMILES:
C1CC2=CC=CC=C2C3=C(C1)C(=NC(=N3)N)N4CCC(C4)N
1.Rotationally constrained 2,4-diamino-5,6-disubstituted pyrimidines: a new class of histamine H4 receptor antagonists with improved druglikeness and in vivo efficacy in pain and inflammation models.
Cowart MD;Altenbach RJ;Liu H;Hsieh GC;Drizin I;Milicic I;Miller TR;Witte DG;Wishart N;Fix-Stenzel SR;McPherson MJ;Adair RM;Wetter JM;Bettencourt BM;Marsh KC;Sullivan JP;Honore P;Esbenshade TA;Brioni JD J Med Chem. 2008 Oct 23;51(20):6547-57. doi: 10.1021/jm800670r. Epub 2008 Sep 26.
A new structural class of histamine H 4 receptor antagonists (6-14) was designed based on rotationally restricted 2,4-diaminopyrimidines. Series compounds showed potent and selective in vitro H 4 antagonism across multiple species, good CNS penetration, improved PK properties compared to reference H 4 antagonists, functional H 4 antagonism in cellular and in vivo pharmacological assays, and in vivo anti-inflammatory and antinociceptive efficacy. One compound, 10 (A-943931), combined the best features of the series in a single molecule and is an excellent tool compound to probe H 4 pharmacology. It is a potent H 4 antagonist in functional assays across species (FLIPR Ca (2+) flux, K b < 5.7 nM), has high (>190x) selectivity for H 4, and combines good PK in rats and mice (t 1/2 of 2.6 and 1.6 h, oral bioavailability of 37% and 90%) with anti-inflammatory activity (ED 50 = 37 micromol/kg, mouse) and efficacy in pain models (thermal hyperalgesia, ED 50 = 72 micromol/kg, rat).
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CAS 1027330-97-7 A 943931

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