A-943931

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

For research use only. We do not sell to patients.

A-943931 Chemical Structure

CAS No. : 1027330-97-7

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Other Forms of A-943931:

A-943931 hydrochloride Get quote

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H₁ Receptor H₂ Receptor H₃ Receptor H₄ Receptor Histamine Receptor

Biological Activity
Purity & Documentation
References
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Description

IC₅₀ & Target^[1]

Human H₄ Receptor

4.6 nM (Ki)

Rat H₄ receptor

3.8 nM (Ki)

In Vivo

A-943931 shows anti-inflammatory activity in zymosan-induced peritonitis in mice with the ED₅₀s of 34, 33 µmol/kg for s.c. and i.p., respectively^[2].
A-943931 (10, 30, 100 µmol/kg; i.p.) shows antinociceptive efficacy in inflammatory pain and neuropathic pain model in rats^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.

Molecular Weight

295.38

Formula

C₁₇H₂₁N₅

CAS No.

1027330-97-7

SMILES

N[C@@H](C1)CCN1C2=C3CCCC4=CC=CC=C4C3=NC(N)=N2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

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. [Content Brief]

A-943931 Related Classifications

Neurological Disease Inflammation/Immunology

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Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

A-9439311027330-97-7A943931A 943931Histamine Receptoranti-inflammatoryantinociceptivezymosanInhibitorinhibitorinhibit

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