PF-00446687 hydrochloride
PF-00446687 hydrochloride is a potent, brain-penetrating, selective melanocortin 4 receptor (MC4R) agonist with an EC50 of 12 nM. PF-00446687 hydrochloride can be used in the research of sexual dysfunction.
For research use only. We do not sell to patients.
- CAS No.: 862282-10-8
- Formula: C28H37ClF2N2O2
- Molecular Weight:507.06
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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]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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MC4R 12 nM (EC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | EC50 |
1.16 μM
Compound: 40a
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Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
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[PMID: 20329799] |
| CHO | EC50 |
12 nM
Compound: 40a
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Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay
Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay
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[PMID: 20329799] |
| HEK293 | EC50 |
1.02 μM
Compound: 40a
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Agonist activity at human recombinant MC1 receptor expressed in HEK293 cells assessed as cAMP accumulation by enzyme fragment complementation assay
Agonist activity at human recombinant MC1 receptor expressed in HEK293 cells assessed as cAMP accumulation by enzyme fragment complementation assay
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[PMID: 20329799] |
| HEK293 | EC50 |
1.98 μM
Compound: 40a
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Agonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assay
Agonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assay
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[PMID: 20329799] |
Chemical Information
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CAS No. 862282-10-8
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Molecular Weight 507.06
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Formula C28H37ClF2N2O2
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SMILES
O=C(N1C[C@H]([C@@]([C@H](C1)C)(C2=CC=CC=C2)O)C)[C@H]3[C@H](C4=C(C=C(C=C4)F)F)CN(C3)C(C)(C)C.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
[1]. Lansdell MI, et al. Discovery of a selective small-molecule melanocortin-4 receptor agonist with efficacy in a pilot study of sexual dysfunction in humans. J Med Chem. 2010 Apr 22;53(8):3183-97. [Content Brief]
[2]. Modi ME, et al. Melanocortin Receptor Agonists Facilitate Oxytocin-Dependent Partner Preference Formation in the Prairie Vole. Neuropsychopharmacology. 2015 Jul;40(8):1856-65. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PF-00446687 hydrochloride Related Classifications
HY-10623 Related Classifications
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