Description
PF-5190457 (PF-05190457) is a potent and selective ghrelin receptor inverse agonist with a pKi of 8.36.
Product information
CAS Number: 1334782-79-4
Molecular Weight: 512.67
Formula: C29H32N6OS
Chemical Name: 2-{2-methylimidazo[2,1-b][1,3]thiazol-6-yl}-1-{2-[(1R)-5-(6-methylpyrimidin-4-yl)-2,3-dihydro-1H-inden-1-yl]-2,7-diazaspiro[3.5]nonan-7-yl}ethan-1-one
Smiles: CC1C=C(N=CN=1)C1=CC2CC[C@H](C=2C=C1)N1CC2(C1)CCN(CC2)C(=O)CC1=CN2C=C(C)SC2=N1
InChiKey: ZIUDADZJCKGWKR-AREMUKBSSA-N
InChi: 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
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 250 mg/mL (487.64 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
PF-5190457 has a superior balance of ghrelin receptor pharmacology and off-target selectivity.
In Vivo:
PF-5190457 has excellent selectivity and demonstrates robust increases in glucose-stimulated insulin secretion in human whole and dispersed islets.
Products are for research use only. Not for human use.
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