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。

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

Solid

MCH1 receptor

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. has not independently confirmed the accuracy of these methods. They are for reference only.

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 t max 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 (t 1/2 ) of 18 to 21 h. Slightly l

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[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.

In Vitro: Ethanol : 2 mg/mL (4.95 mM; Need ultrasonic)配制储备液