ALB-127158 A|cas 1173154-32-9|DC Chemicals

Cas No.:	1173154-32-9
Chemical Name:	ALB-127158(a)
Synonyms:	ALB-127158(a);ALB-127158;ALB-127158A; ALB 127158A; ALB127158A; ALB-127158(A); ALB127158(A); ALB 127158(A); ALB-127158; ALB 127158; ALB127158;1173154-32-9;2(1H)-Pyridinone, 4-[(5-fluoro-2-pyridinyl)methoxy]-1-(2,3,4,5-tetrahydro-5-methyl-1H-pyrido[4,3-b]indol-7-yl)-;4-((5-fluoropyridin-2-yl)methoxy)-1-(5-methyl-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indol-7-yl)pyridin-2(1H)-one
SMILES:	C1(=O)N(C2=CC3=C(C=C2)C2CNCCC=2N3C)C=CC(OCC2=NC=C(F)C=C2)=C1
Formula:	C₂₃H₂₁FN₄O₂
M.Wt:	404.445
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:	ALB-127158(a) is a potent and selective melanin concentrating hormone 1 (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[1].
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[1].

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ALB-127158(a)