An inverse agonist of GHS-R
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PF-05190457

Item No. 40142

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1-[2-[(1R)-2,3-dihydro-5-(6-methyl-4-pyrimidinyl)-1H-inden-1-yl]-2,7-diazaspiro[3.5]non-7-yl]-2-(2-methylimidazo[2,1-b]thiazol-6-yl)-ethanone
CAS Number
1334782-79-4
Molecular Formula
C29H32N6OS
Formula Weight
512.7
Purity
≥95%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMSO: SolubleMethanol: Soluble
SMILES
O=C(CC1=CN2C=C(SC2=N1)C)N3CCC4(CC3)CN(C4)[C@@H]5CCC6=CC(C7=NC=NC(C)=C7)=CC=C65
InChi Code
InChI=1S/C29H32N6OS/c1-19-11-25(31-18-30-19)22-3-5-24-21(12-22)4-6-26(24)35-16-29(17-35)7-9-33(10-8-29)27(36)13-23-15-34-14-20(2)37-28(34)32-23/h3,5,11-12,14-15,18,26H,4,6-10,13,16-17H2,1-2H3/t26-/m1/s1
InChi Key
ZIUDADZJCKGWKR-AREMUKBSSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    25 mg

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    Cayman Chemical
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    OBESITY RESEARCH SOLUTIONS
    Product Description

    PF-05190457 is an inverse agonist of the growth hormone secretagogue receptor (GHS-R), which is also known as the ghrelin receptor.1 It selectively binds to GHS-R (Ki = 4.37 nM) over M2 muscarinic acetylcholine receptors (mAChRs; Ki = 1,950 nM) and the serotonin (5-HT) receptor subtype 5-HT2B (IC50 = 3,700 nM). PF-05190457 (1 µM) increases glucose-induced insulin secretion in primary human pancreatic islets. It potentiates intracellular calcium levels induced by glucagon-like peptide 1 (GLP-1) in isolated dispersed rat islets when used at a concentration of 100 nM.2 Intragastric administration of PF-05190457 increases ex vivo vagal nerve firing rate in rats (EC50 = 10.7 nM).

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Bhattacharya, S.K., Andrews, K., Beveridge, R., et al. Discovery of PF-5190457, a potent, selective, and orally bioavailable ghrelin receptor inverse agonist clinical candidate. ACS Med. Chem. Lett. 5(5), 474-479 (2014).

    2. Kong, J., Chuddy, J., Stock, I.A., et al. Pharmacological characterization of the first in class clinical candidate PF-05190457: A selective ghrelin receptor competitive antagonist with inverse agonism that increases vagal afferent firing and glucose-dependent insulin secretion ex vivo. Br. J. Pharmacol. 173(9), 1452-1464 (2016).