4-Methylhistamine

4-Methylhistamine is a potent and selective agonist of histamine 4 receptor (H4R) with a Ki of 50 nM. 4-Methylhistamine has a >100-fold selectivity for the hH4R over the other histamine receptor subtypes. 4-Methylhistamine can potently activate the hH4R (pEC50 = 7.4) . 4-Methylhistamine can be used for the researches of cancer, inflammation and immunology, such as lung cancer and skin inflammation[1][2][3][4].

Product Specifications

CAS Number

[36507-31-0]

UNSPSC

12352005

Hazard Statement

H315, H319, H320

Target

Histamine Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein; Immunology/Inflammation; Neuronal Signaling

Applications

COVID-19-immunoregulation

Field of Research

Cancer; Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/4-methylhistamine.html

Purity

90.00

Solubility

10 mM in DMSO

Smiles

NCCC1=C(C)N=CN1

Molecular Formula

C6H11N3

Molecular Weight

125.17

Precautions

H315, H319, H320

References & Citations

[1]Lim HD, et al. Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist. J Pharmacol Exp Ther. 2005 Sep;314 (3) :1310-21.|[2]Ahmad SF, et al. Stimulation of the histamine 4 receptor with 4-methylhistamine modulates the effects of chronic stress on the Th1/Th2 cytokine balance. Immunobiology. 2015 Mar;220 (3) :341-9.|[3]Kim CH, et al. Inhibitory Effect of Imiquimod-Induced Psoriasis-Like Skin Inflammation in Mice by Histamine H4 Receptor Agonist 4-Methylhistamine. Scand J Immunol. 2016 Jun;83 (6) :409-17.|[4]Cai WK, et al. Activation of histamine H4 receptors decreases epithelial-to-mesenchymal transition progress by inhibiting transforming growth factor-β1 signalling pathway in non-small cell lung cancer. Eur J Cancer. 2014 Apr;50 (6) :1195-206.