ChemicalBook--->CAS DataBase List--->1322001-35-3

1322001-35-3

1322001-35-3 Structure

1322001-35-3 Structure
IdentificationBack Directory
[Name]

PF4455242 hydrochloride
[CAS]

1322001-35-3
[Synonyms]

PF 4455242,PF4455242
PF4455242 hydrochloride
PF-4455242 hydrochloride
PF 4455242 hydrochloride
PF04455242 hydrochloride
PF 04455242 hydrochloride
PF-04455242 (hydrochloride)
PF-04455242 hydrochloride >=98% (HPLC)
2-methyl-N-((2'-(pyrrolidin-1-ylsulfonyl)-[1,1'-biphenyl]-4-yl)methyl)propan-1-amine
2-METHYL-N-((2'-(PYRROLIDIN-1-YLSULFONYL)-[1,1'-BIPHENYL]-4-YL)METHYL)PROPAN-1-AMINE HCL
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
[Molecular Formula]

C21H29ClN2O2S
[MDL Number]

MFCD22666388
[MOL File]

1322001-35-3.mol
[Molecular Weight]

408.99
Chemical PropertiesBack Directory
[storage temp. ]

room temp
[solubility ]

DMSO: soluble5mg/mL (clear solution, warmed)
[form ]

powder
[color ]

white to beige
Safety DataBack Directory
[WGK Germany ]

3
Hazard InformationBack Directory
[Uses]

PF-4455242 hydrochloride is a selective, short-acting antagonist of the κ-opioid receptor, exhibiting potential analgesic effects. PF-4455242 hydrochloride has been identified through a strategy utilizing parallel chemistry and physicochemical property design. PF-4455242 hydrochloride demonstrated confirmed potency and selectivity in the tail-flick analgesia model.
[Biological Activity]

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

[1] Design and discovery of a selective small molecule κ opioid antagonist (2-methyl-N-((2'-(pyrrolidin-1-ylsulfonyl)biphenyl-4-yl)methyl)propan-1-amine, PF-4455242)
Spectrum DetailBack Directory
[Spectrum Detail]

PF4455242 hydrochloride(1322001-35-3)1HNMR
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