PF 05190457 - ≥98%(HPLC), high purity , CAS No.1334782-79-4, Antagonist of ghrelin receptor

Item Number

P288410

Grouped product items
SKU	Size	Availability	Price
P288410-5mg	5mg	3	$88.90
P288410-10mg	10mg	2	$157.90
P288410-25mg	25mg	2	$345.90
P288410-50mg	50mg	Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!	$642.90
P288410-100mg	100mg	Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!	$1,236.90

High affinity and selective ghrelin receptor inverse agonist

View related series

Basic Description

Synonyms	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]ethanone \| UNII-FF33NL9U5G \| GTPL9060 \| 1-[2-[(1R)-2,3-Dihydro-5-(6-methyl-4-pyrimidinyl)-1H-inden-1-yl]-2,7-diazasp
Specifications & Purity	Moligand™, ≥98%(HPLC)
Biochemical and Physiological Mechanisms	High affinity and selective ghrelin receptor inverse agonist (Kd= 3 nM). Exhibits selectivity for ghrelin receptors over a panel of other targets. Increases intracellular Ca2+concentration in and insulin secretion from human isletsin vitro. Increases gas
Storage Temp	Store at -20°C
Shipped In	Ice chest + Ice pads
Grade	Moligand™
Action Type	ANTAGONIST
Mechanism of action	Antagonist of ghrelin receptor

Names and Identifiers

Pubchem Sid	504771679
Pubchem Sid Url	https://pubchem.ncbi.nlm.nih.gov/substance/504771679
IUPAC 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]ethanone
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
InChi Key	ZIUDADZJCKGWKR-AREMUKBSSA-N
Canonical SMILES	CC1=CC(=NC=N1)C2=CC3=C(C=C2)C(CC3)N4CC5(C4)CCN(CC5)C(=O)CC6=CN7C=C(SC7=N6)C
Isomeric SMILES	CC1=CC(=NC=N1)C2=CC3=C(C=C2)[C@@H](CC3)N4CC5(C4)CCN(CC5)C(=O)CC6=CN7C=C(SC7=N6)C
Alternate CAS	1334782-79-4
PubChem CID	58438464
MeSH Entry Terms	2-(2-methylimidazo(2,1-b)(1,3)thiazol-6-yl)-1-(2-(5-(6-methylpyrimidin-4-yl)-2,3-dihydro-1H-inden-1-yl)-2,7-diazaspiro(3.5)non-7-ylethanone;PF-05190457;PF-5190457
Molecular Weight	512.67

Certificates（CoA,COO,BSE/TSE and Analysis Chart)

C of A & Other Certificates(BSE/TSE, COO):

Analytical Chart:

Find and download the COA for your product by matching the lot number on the packaging.

5 results found

Lot Number	Certificate Type	Date	Item
C23031044	Certificate of Analysis	Oct 09, 2022	P288410
C23031049	Certificate of Analysis	Oct 09, 2022	P288410
C23031077	Certificate of Analysis	Oct 09, 2022	P288410
C23031085	Certificate of Analysis	Oct 09, 2022	P288410
C23031104	Certificate of Analysis	Oct 09, 2022	P288410

References

1. Bhattacharya SK, Andrews K, Beveridge R, Cameron KO, Chen C, Dunn M, Fernando D, Gao H, Hepworth D, Jackson VM et al.. (2014) Discovery of PF-5190457, a Potent, Selective, and Orally Bioavailable Ghrelin Receptor Inverse Agonist Clinical Candidate.. ACS Med Chem Lett, 5 (5): (474-9). [PMID:24900864] [10.1021/op500134e]
2. Kong J, Chuddy J, Stock IA, Loria PM, Straub SV, Vage C, Cameron KO, Bhattacharya SK, Lapham K, McClure KF et al.. (2016) 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): (1452-64). [PMID:26784385] [10.1021/op500134e]

Solution Calculators

Determine the necessary mass, volume, or concentration for preparing a solution.

Determine the dilution needed to prepare a stock solution.

Basic Description