4-Methylhistamine (dihydrochloride)

4-Methylhistamine hydrochloride is the dihydrochloride salt of 4-Methylhistamine (HY-W580721). 4-Methylhistamine hydrochloride is a potent and selective agonist of histamine 4 receptor (H4R) with a K_i of 50 nM. 4-Methylhistamine hydrochloride has a >100-fold selectivity for the hH4R over the other histamine receptor subtypes. 4-Methylhistamine hydrochloride can potently activate the hH4R (pEC₅₀ = 7.4). 4-Methylhistamine hydrochloride can be used for the researches of cancer, inflammation and immunology, such as lung cancer and skin inflammation^[1][2][3][4]. IC50 & Target:histamine 4 receptor^[1] In Vitro:4-Methylhistamine (1-10 μM, 12 h) hydrochloride inhibits cell proliferation in A549, H157, H460 and H322 cells^[4].
4-Methylhistamine (1 μM, 12 h) hydrochloride decreases the TGF-β1 mRNA expression in A549 cells^[4].
In Vivo:4-Methylhistamine (30 mg/kg, i.p., twice a day before 2 days prior to stress) hydrochloride modulates the effects of chronic stress on the Th1/Th2 cytokine balance in Balb/c mice^[2].
4-Methylhistamine (20-40 mg/kg, i.p., once a day for 10 days) hydrochloride attenuates Imiquimod (HY-B0180)-induced psoriasis-like skin inflammation in mice^[3].
4-Methylhistamine (100 μmol/kg, i.v., every other day for 33 days) hydrochloride decreases the average tumour volume and prolongs survival in A549 tumor mice^[4].