WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 522485

CAS#: 1334782-79-4

Description: PF-5190457 is an orally available, potent and selective ghrelin receptor inverse agonist. PF-5190457 potently increases insulin secretion in glucose-stimulated human islets. PF-5190457 has a superior balance of ghrelin receptor pharmacology and off-target selectivity. On the basis of its promising pharmacological and safety profile, PF-5190457 was advanced to human clinical trials.

Chemical Structure

CAS# 1334782-79-4

Theoretical Analysis

MedKoo Cat#: 522485
Name: PF-5190457
CAS#: 1334782-79-4
Chemical Formula: C29H32N6OS
Exact Mass: 512.23583
Molecular Weight: 512.676
Elemental Analysis: C, 67.94; H, 6.29; N, 16.39; O, 3.12; S, 6.25

Price and Availability

Size Price Availability Quantity
5.0mg USD 350.0 2 Weeks
10.0mg USD 550.0 2 Weeks
25.0mg USD 1050.0 2 Weeks
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Synonym: PF-5190457; PF 5190457; PF5190457; PF-05190457; PF05190457; PF 05190457.

IUPAC/Chemical Name: (R)-2-(2-methylimidazo[2,1-b]thiazol-6-yl)-1-(2-(5-(6-methylpyrimidin-4-yl)-2,3-dihydro-1H-inden-1-yl)-2,7-diazaspiro[3.5]nonan-7-yl)ethan-1-one


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

SMILES Code: CC1=CC(C2=CC3=C([C@H](N4CC5(CCN(C(CC(N=C6S7)=CN6C=C7C)=O)CC5)C4)CC3)C=C2)=NC=N1

Appearance: Solid powder

Purity: >95% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

Preparing Stock Solutions

The following data is based on the product molecular weight 512.676 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL

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1: Ghareeb M, Leggio L, El-Kattan A, Akhlaghi F. Development and validation of an
UPLC-MS/MS assay for quantitative analysis of the ghrelin receptor inverse
agonist PF-5190457 in human or rat plasma and rat brain. Anal Bioanal Chem. 2015
Jul;407(19):5603-13. doi: 10.1007/s00216-015-8730-2. Epub 2015 May 7. PubMed
PMID: 25943263; PubMed Central PMCID: PMC4499019.

2: Bhattacharya SK, Andrews K, Beveridge R, Cameron KO, Chen C, Dunn M, Fernando
D, Gao H, Hepworth D, Jackson VM, Khot V, Kong J, Kosa RE, Lapham K, Loria PM,
Londregan AT, McClure KF, Orr ST, Patel J, Rose C, Saenz J, Stock IA, Storer G,
VanVolkenburg M, Vrieze D, Wang G, Xiao J, Zhang Y. Discovery of PF-5190457, a
Potent, Selective, and Orally Bioavailable Ghrelin Receptor Inverse Agonist
Clinical Candidate. ACS Med Chem Lett. 2014 Feb 24;5(5):474-9. doi:
10.1021/ml400473x. eCollection 2014 May 8. PubMed PMID: 24900864; PubMed Central
PMCID: PMC4027753.