A-943931

Modify Date: 2024-02-24 12:35:29

A-943931 Structure
A-943931 structure
Common Name A-943931
CAS Number 1027330-97-7 Molecular Weight 295.38200
Density N/A Boiling Point N/A
Molecular Formula C17H21N5 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of A-943931


A-943931 is a potent and selective histamine H4 receptor (H4R) antagonist with pKi values of 4.6, 3.8 nM for human and rat H4R, respectively. A-943931 shows anti-inflammatory and antinociceptive efficacy[1][2].

 Names

Name 4-[(3R)-3-aminopyrrolidin-1-yl]-6,7-dihydro-5H-benzo[1,2]cyclohepta[3,4-b]pyrimidin-2-amine
Synonym More Synonyms

 A-943931 Biological Activity

Description A-943931 is a potent and selective histamine H4 receptor (H4R) antagonist with pKi values of 4.6, 3.8 nM for human and rat H4R, respectively. A-943931 shows anti-inflammatory and antinociceptive efficacy[1][2].
Related Catalog
Target

Human H4 Receptor:4.6 nM (Ki)

Rat H4 receptor:3.8 nM (Ki)

In Vivo A-943931 在酵母聚糖诱导的小鼠腹膜炎中表现出抗炎活性,皮下注射和腹腔注射的ED50 值分别为 34, 33 µmol/kg[2]。 A-943931 (10, 30, 100 µmol/kg; 腹腔注射) 在大鼠的炎症性疼痛和神经性疼痛模型中表现出镇痛效果[2]。 Animal Model: Rats (carrageenan-induced inflammatory pain and spinal nerve ligation model of neuropathic pain)[2] Dosage: 10, 30, 100 µmol/kg Administration: I.p. Result: Showed antinociceptive efficacy in an inflammatory pain model in rat at an ED50 value of 72 µmol/kg, ip, and in a neuropathic pain model at an ED50 value of 100 µmol/kg, ip.
References

[1]. Ivan Milicic, et al. Identification of two potent and selective histamine H4 receptor antagonists with antipruritic activity. The FASEB journal homepage. 2009.

[2]. Cowart MD, et al. 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. J Med Chem. 2008 Oct 23;51(20):6547-57.  

 Chemical & Physical Properties

Molecular Formula C17H21N5
Molecular Weight 295.38200
Exact Mass 295.18000
PSA 81.79000
LogP 2.44730

 Synonyms

2,4-diamino-5,6-disubstituted pyrimidine,10
UNII-Q598HK01AO
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