Enerisant hydrochloride (TS091) | H3R antagonist | Probechem Biochemicals

Chemical Structure : Enerisant hydrochloride

CAS No.: 1152749-07-9

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Enerisant hydrochloride (TS091 hydrochloride)

货号: PC-72277Not For Human Use, Lab Use Only.

Enerisant hydrochloride (TS091 hydrochloride) is a potent, selective histamine H3 receptor antagonist/inverse agonist with IC50 of 2.89 and 14.5 nM against hH3R and rH3R, respectively.

规格	价格	库存
5 mg	￥1980	In stock
10 mg	￥2980	In stock
25 mg	￥4980	In stock
50 mg		Get quote
100 mg		Get quote

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生物&药学活性

Enerisant hydrochloride (TS091 hydrochloride) is a potent, selective histamine H3 receptor antagonist/inverse agonist with IC50 of 2.89 and 14.5 nM against hH3R and rH3R, respectively.
Enerisant inhibited R-α-methylhistamine–stimulated [35S]GTPγS binding to human histamine H3 receptor and rat histamine H3 receptor with IC50 values of 1.06 and 10.05 nM, respectively, inhibited basal [35S]GTPγS binding to human histamine H3 receptor with an EC50 value of 0.357 nM.
Enerisant displays negligible effects on binding to human histamine H1, H2, and H4 receptor subtypes, as well as negligible affinities for 66 other receptors, transporters, and ion channels at 1-10 uM.
Oral administration of enerisant hydrochloride attenuated the dipsogenia response on R-α-methylhistamine–induced dipsogenia in rats, the intraperitoneal administration of enerisant hydrochloride increased the total extracellular acetylcholine levels in the mPFC.
Enerisant hydrochloride significantly decreased slow-wave deep sleep at doses of 1-10 mg/kg (P < 0.01-0.05). Enerisant hydrochloride (1, 3 and 10 mg/kg, p.o.) did not affect the accumulated locomotor activity time at up to 7 hours after administration.

物理化学性质&存储条件

分子量	434.965
分子式	C22H31ClN4O3
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(R)-(1-(4-(3-(2-methylpyrrolidin-1-yl)propoxy)phenyl)-1H-pyrazol-4-yl)(morpholino)methanone hydrochlorid

参考文献

1. Noriko Hino, et al. J Pharmacol Exp Ther. 2020 Nov;375(2):276-285.

Enerisant hydrochloride (TS091 hydrochloride)

生物&药学活性

物理化学性质&存储条件

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Enerisant hydrochloride (TS091 hydrochloride)

生物&药学活性

物理化学性质&存储条件

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