WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 522485
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.
MedKoo Cat#: 522485
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
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 Key: ZIUDADZJCKGWKR-AREMUKBSSA-N
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
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.
|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|
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