PF-00446687( PF-446687 | PF00446687 )

Catalog No. M16240 CAS No. 862281-92-3

COA

Datasheet

HNMR

HPLC

MSDS

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Product Name

PF-00446687
Note

Research use only, not for human use.
Brief Description

PF-00446687 (PF-446687) is a potent, selective melanocortin-4 receptor (MC4R) agonist with EC50 of 12 nM.
Description

PF-00446687 (PF-446687) is a potent, selective melanocortin-4 receptor (MC4R) agonist with EC50 of 12 nM; displays >100-fold selectivity over MC1R/1 uM); is find to be active in preliminary human trials, with the 200mg dose being of similar effectiveness to 100mg sildenafil, though lower doses were ineffective.Sexual Dysfunction Phase 2 Clinical.
In Vitro

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In Vivo

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Synonyms

PF-446687 | PF00446687
Pathway

GPCR/G Protein
Target

Melanocortin Receptor
Recptor

Melanocortin Receptor
Research Area

Endocrinology
Indication

Sexual Dysfunction

CAS Number

862281-92-3
Formula Weight

470.593
Molecular Formula

C28H36F2N2O2
Purity

>98% (HPLC)
Solubility

In Vitro:?DMSO : 62.5 mg/mL (132.81 mM)
SMILES

CC1CN(CC(C1(C2=CC=CC=C2)O)C)C(=O)C3CN(CC3C4=C(C=C(C=C4)F)F)C(C)(C)C
Chemical Name

[(3S,4R)-1-tert-butyl-4-(2,4-difluorophenyl)pyrrolidin-3-yl]-[(3S,5R)-4-hydroxy-3,5-dimethyl-4-phenylpiperidin-1-yl]methanone

1. Lansdell MI, et al. J Med Chem. 2010 Apr 22;53(8):3183-97. 2. Modi ME, et al. Neuropsychopharmacology. 2015 Jul;40(8):1856-65.

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