1. GPCR/G Protein
  2. MCHR1 (GPR24)

ALB-127158(a) 

Cat. No.: HY-111398 Purity: 99.32%
Handling Instructions

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

For research use only. We do not sell to patients.
ALB-127158(a) Chemical Structure

ALB-127158(a) Chemical Structure

CAS No. : 1173154-32-9

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 231 In-stock
5 mg USD 210 In-stock
10 mg USD 330 In-stock
25 mg USD 650 In-stock
50 mg USD 990 In-stock
100 mg USD 1500 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Description

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

IC50 & Target

MCH1 receptor[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].

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].

References
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 2.4726 mL 12.3628 mL 24.7255 mL
5 mM 0.4945 mL 2.4726 mL 4.9451 mL
10 mM 0.2473 mL 1.2363 mL 2.4726 mL
Please refer to the solubility information to select the appropriate solvent.
References
Molecular Weight

404.44

Formula

C₂₃H₂₁FN₄O₂

CAS No.

1173154-32-9

SMILES

O=C1C=C(OCC2=NC=C(F)C=C2)C=CN1C3=CC4=C(C=C3)C(CNCC5)=C5N4C

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

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Product Name:
ALB-127158(a)
Cat. No.:
HY-111398
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