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ALB-127158(a)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
ALB-127158(a)图片
CAS NO:1173154-32-9
规格:98%
分子量:404.44
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
ALB-127158(a)是一种有效的选择性黑色素浓缩激素1(MCH1)受体拮抗剂。
CAS:1173154-32-9
分子式:C23H21FN4O2
分子量:404.44
纯度:98%
存储:Store at -20°C

Background:

ALB-127158(a) is a potent and selective melanin concentrating hormone 1 (MCH1) receptor antagonist.


ALB-127158(a) has high affinity for the MCH1 receptor (7 nM) with good selectivity over a range of other G-protein coupled receptors (GPCRs), ion channels and transporters, including the MCH2 receptor. In vitro functional assays confirmed that ALB-127158(a) is a potent and selective MCH1 receptor antagonist[1].


In a mouse diet induced obesity (DIO) model, ALB-127158(a) produces a significant sustained decrease in body weight and food intake in the range of 5-15 mg/kg bid. The weight reduction is predominantly due to a decrease in fat content. In high fat diet (HFD) rats, ALB-127158(a) produces significant weight loss and food reduction at doses as low as 1.25 mg/kg po. Doses >1.25 mg/kg po produces weight loss >6%, maximal weight loss of about 10% in rats is observed at 10 mg/kg. Following single and multiple oral administration of ALB-127158(a), ALB-127158(a) is rapidly absorbed (median tmax attains between 1 and 3 h post dose in lean and overweight/obese subjects) with a trend to decrease over dose suggesting a slower absorption rate of ALB-127158(a) at lower doses. After single doses, ALB-127158(a) has a mean half-life (t1/2) of 18 to 21 h. Slightly longer mean t1/2 estimates of approximately 26 h are obtained following multiple dosing in overweight/obese subjects; steady-state plasma ALB-127158(a) is attained within 6 to 8 days of dosing[1].


[1]. Moore NA, et al. From preclinical to clinical development: the example of a novel treatment for obesity. Neurobiol Dis. 2014 Jan;61:47-54.