MC4R antagonist-3 hydrochloride
MC4R antagonist-3 hydrochloride is a selective melanocortin-4 receptor (MC4R) antagonist with a Kd value of 2 nM. MC4R antagonist-3 hydrochloride binds to MC4R and alters its conformation, specifically promoting ERK1/2 phosphorylation in constitutively active mutants while inhibiting basal cAMP production. MC4R antagonist-3 hydrochloride can be used for research on obesity.
For research use only. We do not sell to patients.
- CAS No.: 746661-90-5
- Formula: C34H51Cl2N5O2
- Molecular Weight:632.71
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
MC4R 2 nM (Kd) |
In Vitro
MC4R antagonist-3 (1 µM; 2-60 min) hydrochloride has no significant effect on ERK1/2 phosphorylation levels in HEK293T cells transfected with wild-type human MC4R and in GT1-7 cells endogenously expressing mouse MC4R[1].
MC4R antagonist-3 (1 µM; 5 min) hydrochloride significantly activates and increases ERK1/2 phosphorylation in HEK293T cells transfected with specific CAM human MC4R (P230L, L250Q, and F280L)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HEK293T cells transiently transfected with WT human MC4R and GT1-7 cells endogenously expressing mouse MC4R
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Concentration:1 μM
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Incubation Time:2, 5, 10, 20, 30, 45, 60 min
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Result:Showed no significant differences in the pERK1/2 level within 1 h in both HEK293T and GT1-7 cells.
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Cell Line:HEK293T cells transiently transfected with WT and six CAM (H76R, S127L, D146N, P230L, L250Q, F280L) human MC4Rs
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Concentration:1 μM
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Incubation Time:5 min
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Result:Induced significant increases of ERK1/2 phosphorylation in three CAM hMC4Rs (P230L, L250Q and F280L), but showed no significant change for WT and the other three CAM hMC4Rs (H76R, S127L and D146N).
Chemical Information
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CAS No. 746661-90-5
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Molecular Weight 632.71
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Formula C34H51Cl2N5O2
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SMILES
O=C(N(CCC(C)C)CCC(C)C)C1=CC2=C(N=C(N2CCCN3CCCCC3)NC4=CC=C(C(C)=O)C=C4)C=C1.Cl.Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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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-3 hydrochloride Related Classifications
HY-W559510A Related Classifications
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