MC4R Antagonist-1
MC4R Antagonist-1 (compound 1) is an MC4R-selective antagonist (IC50<10 nM). MC4R Antagonist-1 can be used for the research of cachexia, anorexia, anorexia nervosa, involuntary weight loss, failure to thrive, sarcopenia, muscle wasting, muscle weakness, frailty, osteoporosis.
For research use only. We do not sell to patients.
- Formula: C25H28FN7O2
- Molecular Weight:477.53
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
- Purity & Documentation
- References
-
Help & FAQs
Biological Activity
|
MC4R <10 nM (IC50) |
MC4R Antagonist-1 (compound 1) (0.1-1000 nM; 8-16 h) restores α-MSH-induced cAMP signaling in HEK293 cells overexpressing T162I-MC4R, with an EC50 < 50 nM and an Emax > 150%[1].
MC4R Antagonist-1 (10 μM; 10-16 h) significantly increases plasma membrane MC4R levels and elevates the plasma membrane/total MC4R ratio in HEK293 cells transfected with 24 MC4R loss-of-function mutants[1].
MC4R Antagonist-1 forms only 4 GSH adducts with a total relative abundance of 3.6% in an in vitro human liver microsome system, and no GSH adducts are produced in the absence of liver microsomes[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:HEK293 cells transiently transfected with 24 loss-of-function MC4R variants
-
Concentration:0.75 μM, 10 μM
-
Incubation Time:10-16 h
-
Result:Significantly increased plasma membrane MC4R levels and the ratio of plasma membrane to total cellular MC4R for all tested MC4R loss-of-function variants.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Homozygous MC4RR165Q/R165Q MC4R-deficient (MC4R-D) mice (8 weeks old, single-housed, preconditioned with 45% high-fat diet)[1]
-
Dosage:10 mpk, 30 mpk, 60 mpk
-
Administration:subcutaneous injection, twice daily (BID) for 19 days
-
Result:At 30 mpk and 60 mpk BID, significantly decreased body weight and cumulative food intake compared with the vehicle-treated group, whereas 10 mpk BID did not produce significant effects on body weight or cumulative food intake.
Chemical Information
-
Molecular Weight 477.53
-
Formula C25H28FN7O2
-
SMILES
C[C@H](C1=CC(OC)=NC=C1F)C(N2C[C@@]3(CC2)CN(C)C4=CC(C5=NC=CC=N5)=C(C)N=C4N3)=O
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
MC4R Antagonist-1 Related Classifications
HY-182773 Related Classifications
Powered by Bioz