[CAS NO. 1173154-32-9]  ALB-127158(a)

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PRODUCTS SPECIFICATIONS [1173154-32-9]

Catalog
HY-111398
Brand
MCE
CAS
1173154-32-9

DESCRIPTION [1173154-32-9]

Overview

MDL-
Molecular Weight404.44
Molecular FormulaC23H21FN4O2
SMILESO=C1C=C(OCC2=NC=C(F)C=C2)C=CN1C3=CC4=C(C=C3)C(CNCC5)=C5N4C

For research use only. We do not sell to patients.

Summary

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


IC50 & Target

MCH 1 receptor [1]


In Vitro

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 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 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.


Appearance

Solid


Shipping

Room temperature in continental US; may vary elsewhere.


Storage

Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month

Solvent & Solubility

In Vitro:

Ethanol : 2 mg/mL ( 4.95 mM ; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4726 mL 12.3628 mL 24.7255 mL
5 mM --- --- ---
10 mM --- --- ---
* Please refer to the solubility information to select the appropriate solvent.