MDL | - |
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Molecular Weight | 404.44 |
Molecular Formula | C23H21FN4O2 |
SMILES | O=C1C=C(OCC2=NC=C(F)C=C2)C=CN1C3=CC4=C(C=C3)C(CNCC5)=C5N4C |
ALB-127158(a) is a potent and selective melanin concentrating hormone 1 ( MCH 1 ) receptor antagonist.
MCH 1 receptor [1]
ALB-127158(a) has high affinity for the MCH 1 receptor (7 nM) with good selectivity over a range of other G-protein coupled receptors (GPCRs), ion channels and transporters, including the MCH 2 receptor. In vitro functional assays confirmed that ALB-127158(a) is a potent and selective MCH 1 receptor antagonist [1] .
MCE 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 longer mean t 1/2 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] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Solid
Room temperature in continental US; may vary elsewhere.
Powder | -20°C | 3 years |
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4°C | 2 years | |
In solvent | -80°C | 6 months |
-20°C | 1 month |
Ethanol : 2 mg/mL ( 4.95 mM ; Need ultrasonic)
Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
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1 mM | 2.4726 mL | 12.3628 mL | 24.7255 mL |
5 mM | --- | --- | --- |
10 mM | --- | --- | --- |