2. GPCR/G Protein Neuronal Signaling
  3. Melanocortin Receptor
  4. 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.

PF-00446687 hydrochloride

PF-00446687 hydrochloride Chemical Structure

CAS No. : 862282-10-8

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PF-00446687 hydrochloride Related Antibodies

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MC1R MC3R MC2R MC4R MC5R

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Description

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[1][2].

IC50 & Target[1][2]

MC4R

12 nM (EC50)

Cellular Effect
Cell Line Type Value Description References
CHO EC50
1.16 μM
Compound: 40a
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
[PMID: 20329799]
CHO EC50
12 nM
Compound: 40a
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
[PMID: 20329799]
HEK293 EC50
1.02 μM
Compound: 40a
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
[PMID: 20329799]
HEK293 EC50
1.98 μM
Compound: 40a
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
[PMID: 20329799]
Molecular Weight

507.06

Formula

C28H37ClF2N2O2
CAS No.
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
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
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PF-00446687 hydrochloride Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PF-00446687862282-10-8PF00446687PF 00446687Melanocortin ReceptorMC Receptorsexual dysfunctionInhibitorinhibitorinhibit

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PF-00446687 hydrochloride
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