An MC4R agonist
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PF-00446687

Item No. 41739

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
[(3S,4R)-4-(2,4-difluorophenyl)-1-(1,1-dimethylethyl)-3-pyrrolidinyl][(3R,5S)-4-hydroxy-3,5-dimethyl-4-phenyl-1-piperidinyl]-methanone
CAS Number
862281-92-3
Synonyms
  • PF446687
Molecular Formula
C28H36F2N2O2
Formula Weight
470.6
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
Acetonitrile: Slightly soluble: 0.1-1 mg/mlDMSO: SolventSolubilityWater: Slightly soluble: 0.1-1 mg/ml
SMILES
C[C@H]1CN(C([C@H]2[C@H](C3=CC=C(F)C=C3F)CN(C(C)(C)C)C2)=O)C[C@@H](C)[C@]1(O)C4=CC=CC=C4
InChi Code
InChI=1S/C28H36F2N2O2/c1-18-14-31(15-19(2)28(18,34)20-9-7-6-8-10-20)26(33)24-17-32(27(3,4)5)16-23(24)22-12-11-21(29)13-25(22)30/h6-13,18-19,23-24,34H,14-17H2,1-5H3/t18-,19+,23-,24+,28-/m0/s1
InChi Key
WHPJOAUPIZDJNX-AGGGUQDCSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $164

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    5 mg

    $656

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    Product Description

    PF-00446687 is an agonist of melanocortin receptor 4 (MC4R).1 It selectively activates adenylyl cyclase in HEK293 cells expressing MC4R (EC50 = 0.012 µM) over HEK293 cells expressing MC1R, MC3R, or MC5R (EC50s = 1.02, 1.16, and 1.98 µM, respectively). PF-00446687 (1 mg/kg per day) increases time spent huddling and in close contact with chosen partners in prairie voles.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Lansdell, M.I., Hepworth, D., Calabrese, A., 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. 53(8), 3183-3197 (2009).

    2. Barrett, C.E., Modi, M.E., Zhang, B.C., et al. Neonatal melanocortin receptor agonist treatment reduces play fighting and promotes adult attachment in prairie voles in a sex-dependent manner. Neuropharmacology 85, 357-366 (2014).