| Identification | Back 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 |
| Hazard Information | Back 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) |
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| Company Name: |
SPIRO PHARMA
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| Telephone: |
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| Website: |
www.spiropharma.com.cn |
| Company Name: |
AFINE CHEMICALS LIMITED
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| Telephone: |
+86-571-85134551 +86-18958018566 |
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www.afinechem.com/index.html |
| Company Name: |
Energy Chemical
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400-0056266 |
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www.energy-chemical.com |
| Company Name: |
Wuhan Topule
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+86-02787215551 19945035818 |
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http://www.topule.com/ |
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