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MCHR1 antagonist 2 

Cat. No. M30725
MCHR1 antagonist 2  Structure
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Biological Activity

MCHR1 antagonist 2 is an antagonist of melanin concentrating hormone receptor 1, with an IC50 of 65 nM; MCHR1 antagonist 2 also inhibits hERG, with an IC50 of 4.0 nM in IMR-32 cells.

Chemical Information
Molecular Weight 424.42
Formula C23H21FN2O5
CAS Number 863115-70-2
Form Solid
Solubility (25°C) DMSO 10 mg/mL (ultrasonic and adjust pH to 6 with HCl)
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Anders Johansson, et al. J Med Chem. Discovery of (3-(4-(2-Oxa-6-azaspiro[3.3]heptan-6-ylmethyl)phenoxy)azetidin-1-yl)(5-(4-methoxyphenyl)-1,3,4-oxadiazol-2-yl)methanone (AZD1979), a Melanin Concentrating Hormone Receptor 1 (MCHr1) Antagonist with Favorable Physicochemical Properties

[2] Anders Johansson, et al. Expert Opin Ther Pat. Novel MCH1 receptor antagonists: a patent review

[3] Denise Andersen, et al. J Org Chem. Stereoselective synthesis of a MCHr1 antagonist

[4] D J David, et al. J Pharmacol Exp Ther. Efficacy of the MCHR1 antagonist N-[3-(1-{[4-(3,4-difluorophenoxy)phenyl]methyl}(4-piperidyl))-4-methylphenyl]-2-methylpropanamide (SNAP 94847) in mouse models of anxiety and depression following acute and chronic administration is independent of hippocam䲧癐Ỵ癑㧀癏羹瘸

[5] Anil Vasudevan, et al. Bioorg Med Chem Lett. Synthesis and evaluation of 2-amino-8-alkoxy quinolines as MCHr1 antagonists. Part 2

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