AM 251

AM 251 속성

AM 251 C화학적 특성, 용도, 생산

개요

AM251 is a cannabinoid 1 (CB₁) receptor 1 antagonist. It binds to CB₁ receptors in rat forebrain membrane preparations (K_i = 7.5 nM) and is selective over CB₂ receptors in mouse spleen preparations (K_i = 2,290 nM) in radioligand binding assays. AM251 inhibits GTPγS binding induced by the CB receptor agonist CP 55,940 in HEK293 cells expressing human CB₁ receptors (EC₅₀ = 8 nM). AM251 (10 mg/kg) decreases immobility time in the forced swim test in wild-type but not CB₁ receptor-deficient mice. It reduces fasting-induced food intake and body weight gain in mice when administered at a dose of 30 mg/kg. AM251 also induces GTPγS binding in HEK293 cells expressing the orphan receptor GPR55 (EC₅₀ = 39 nM) and potentiates GABA-induced GABA_A receptor currents (EC₅₀ = 0.4 μM). It prevents TGF-β1-induced epithelial-to-mesenchymal transition (EMT), inhibits SMAD2/3 and p38 MAPK activation, and reduces the expression of EMT-related transcription factors in HK-2 renal tubule epithelial cells. AM251 induces cell cycle arrest at the G₂/M phase and apoptosis in A375 human melanoma cells.

화학적 성질

White to Off-White Solid

용도

Inhibitor of CB1 receptors. AM 251is a biarylpyrazole compound which has been considered for many years as the prototypical cannabinoid (CB) receptor antagonist

생물학적 활성

Potent CB 1 receptor antagonist (IC 50 = 8 nM, K i = 7.49 nM) that displays 306-fold selectivity over CB 2 receptors. Also potent GPR55 agonist (EC 50 = 39 nM). Also available as part of the Cannabinoid CB 1 Receptor Tocriset™ .

AM 251 준비 용품 및 원자재

원자재

준비 용품

AM 251 공급 업체

공급자	전화	이메일	국가	제품 수	이점
ATK CHEMICAL COMPANY LIMITED	+undefined-21-51877795	ivan@atkchemical.com	China	32836	60
Hubei Jusheng Technology Co.,Ltd.	18871490254	linda@hubeijusheng.com	CHINA	28180	58
TargetMol Chemicals Inc.	+1-781-999-5354 +1-00000000000	marketing@targetmol.com	United States	19892	58
HANGZHOU CLAP TECHNOLOGY CO.,LTD	86-571-88216897,88216896 13588875226	sales@hzclap.com	CHINA	6313	58
Zhejiang J&C Biological Technology Co.,Limited	+1-2135480471 +1-2135480471	sales@sarms4muscle.com	China	10522	58
InvivoChem	+1-708-310-1919 +1-13798911105	sales@invivochem.cn	United States	6393	58
LEAPCHEM CO., LTD.	+86-852-30606658	market18@leapchem.com	China	43348	58
Aladdin Scientific	+1-+1(833)-552-7181	sales@aladdinsci.com	United States	57511	58
Amadis Chemical Company Limited	571-89925085	sales@amadischem.com	China	131980	58
J & K SCIENTIFIC LTD.	010-82848833 400-666-7788	jkinfo@jkchemical.com	China	96815	76

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