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Merck
CN

PZ0206

PF-04455242 hydrochloride

≥98% (HPLC)

Synonym(s):

2-Methyl-N-((2′-(pyrrolidin-1-ylsulfonyl)biphenyl-4-yl)methyl)propan-1-amine hydrochloride, N-(2-Methylpropyl)-2′-(1-pyrrolidinylsulfonyl)-[1,1′-biphenyl]-4-methanamine hydrochloride, PF-4455242 hydrochloride

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About This Item

Empirical Formula (Hill Notation):
C21H28N2O2S · HCl
CAS Number:
1322001-35-3
Molecular Weight:
408.99
NACRES:
NA.77
PubChem Substance ID:
329823774
UNSPSC Code:
51111800
MDL number:
MFCD22666388
Assay:
≥98% (HPLC)
Form:
powder
Quality level:
100
Storage condition:
desiccated

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InChI

1S/C21H28N2O2S.ClH/c1-17(2)15-22-16-18-9-11-19(12-10-18)20-7-3-4-8-21(20)26(24,25)23-13-5-6-14-23;/h3-4,7-12,17,22H,5-6,13-16H2,1-2H3;1H

SMILES string

Cl.CC(C)CNCc1ccc(cc1)-c2ccccc2S(=O)(=O)N3CCCC3

InChI key

WRNZYMZEVIVCFL-UHFFFAOYSA-N

assay

≥98% (HPLC)

form

powder

storage condition

desiccated

color

white to beige

solubility

DMSO: 5 mg/mL (clear solution, warmed)

storage temp.

room temp

Quality Level

100

Biochem/physiol Actions

PF-4455242 is a Kappa opioid receptor (KOR) antagonist.
PF-4455242 is a selective k opioid receptor (KOR) antagonist with 20-fold selectivity for kappa over mu receptors (k Ki = 3 nM, μ Ki =64 nM). PF-4455242 is orally active, has good brain penetration in rats and was able to block the effects of the kappa agonist U50488. Studies indicate that k blockade has afforded antidepressant activity in several animal models. PF-4455242 has been in phase I clinical trials for trial for bipolar depression.

Features and Benefits

This compound is featured on the Opioid Receptors page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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Certificates of Analysis (COA)

Lot/Batch Number
0000149347
0000149346
0000149346
0000149347
0000075195

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Articles

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