ALB-127158(a)

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

Product information

CAS Number: 1173154-32-9

Molecular Weight: 404.44

Formula: C23H21FN4O2

Chemical Name: 4-[(5-fluoropyridin-2-yl)methoxy]-1-{5-methyl-1H,2H,3H,4H,5H-pyrido[4,3-b]indol-7-yl}-1,2-dihydropyridin-2-one

Smiles: CN1C2C=C(C=CC=2C2CNCCC1=2)N1C=CC(=CC1=O)OCC1C=CC(F)=CN=1

InChiKey: VUUUHLIHQHVLLE-UHFFFAOYSA-N

InChi: InChI=1S/C23H21FN4O2/c1-27-21-6-8-25-13-20(21)19-5-4-17(10-22(19)27)28-9-7-18(11-23(28)29)30-14-16-3-2-15(24)12-26-16/h2-5,7,9-12,25H,6,8,13-14H2,1H3

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

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.

In Vivo:

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.

Products are for research use only. Not for human use.