PF-543
- Product Name
- PF-543
- CAS No.
- 1706522-79-3
- Chemical Name
- PF-543
- Synonyms
- PF 543 HCl;PF-543 hydrochloride ，S7177;WNKWAZFYPZMDGJ-VQIWEWKSSA-N;PF-543 Hydrochloride DISCONTINUED;PF-543 hydrochloride, 10 mM in DMSO;(2R)-1-[[(4-[[3-Methyl-5-[(phenylsulfonyl)methyl]phenoxy]methyl]phenyl]methyl]-2-pyrrolidinemethanol hydrochloride;Nrf-2,PF543 hydrochloride,anti-cancer,sphingosine-competitive,S1P,Sphingosine Kinase 1 Inhibitor II,Apoptosis,inhibit,PF 543,Lysophospholipid Receptor,PAH,necrosis,SphK,Inhibitor,Autophagy,PF543,PF 543 hydrochloride,caspase-3/7,SK1,Sphingosine kinase,LPL Receptor,anti-inflammatory
- CBNumber
- CB43355459
- Molecular Formula
- C27H32ClNO4S
- Formula Weight
- 502.07
- MOL File
- 1706522-79-3.mol
PF-543 Property
- Melting point:
- 156-158oC (dec.)
- storage temp.
- under inert gas (nitrogen or Argon) at 2-8°C
- solubility
- DMSO, Methanol
- form
- Solid
- color
- Beige
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- 17034
- Product name
- PF-543 (hydrochloride)
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $32
- Updated
- 2024/03/01
- Product number
- 17034
- Product name
- PF-543 (hydrochloride)
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $100
- Updated
- 2024/03/01
- Product number
- 17034
- Product name
- PF-543 (hydrochloride)
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $184
- Updated
- 2024/03/01
- Product number
- 17034
- Product name
- PF-543 (hydrochloride)
- Purity
- ≥98%
- Packaging
- 25mg
- Price
- $381
- Updated
- 2024/03/01
- Product number
- A451925
- Product name
- PF543HCl
- Purity
- 97%
- Packaging
- 100mg
- Price
- $481
- Updated
- 2021/12/16
PF-543 Chemical Properties,Usage,Production
Uses
(2R)-1-[[4-[[3-Methyl-5-[(phenylsulfonyl)methyl]phenoxy]methyl]phenyl]methyl]-2-pyrrolidinemethanol, is a novel Sphingonise Kinas 1 (SphK1, SK1) inhibitor.
Enzyme inhibitor
This potent SphK1 inhibitor (FWHCl-Salt = 502.07 g/mol; CAS 1706522-79- 3; Solubility: 10 mM in H2O, with gentle warming; 100 mM in DMSO), also named (2R)-1-[[(4-[[3-methyl-5-[(phenylsulfonyl)methyl]phenoxy] methyl]phenyl]methyl]-2-pyrrolidinemethanol hydrochloride, selectively targets sphingosine kinase 1 (IC50 = 2 nM; Ki = 3.6 nM). The latter phosphorylates sphingosine to form sphingosine-1-phosphate (S1P), a lipid messenger with both intracellular functions (regulating cell proliferation and survival) and extracellular functions (as a ligand for EDG1, or sphingosine-1-phosphate receptor 1). PF-543 also exhibits >100-fold selectivity for Sphk1 over Sphk2 as well as >5000 fold selectivity over S1P1-5 receptors and 48 protein and lipid kinases. P 543 attenuates proliferation and induces necrosis in human colorectal cancer cells in vitro. It also suppresses human colorectal cancer cell line HCT-116 as a tumor xenograft growth in mice
in vivo
PF-543 (1 mg/kg; intraperitoneal injection; every second day; for 21 days; female C57BL/6 J mice) treatment has no effect on vascular remodelling but reduces right ventricular hypertrophy. The protection involves a reduction in the expression of p53 and an increase in the expression of anti-oxidant nuclear factor Nrf-2[2].
Mice are initially dosed (ip) with 10 mg/kg or 30 mg/kg of PF-543 for 24 h and the T1/2 is 1.2 h in blood samples. Administration of 10 mg/kg PF-543 for 24 h to mice induces a decrease in SK1 expression in pulmonary vessels[2].
| Animal Model: | Female C57BL/6 J mice (7-12 week-old) with hypoxic-induced pulmonary arterial hypertension[2] |
| Dosage: | 1 mg/kg |
| Administration: | Intraperitoneal injection; every second day; for 21 days |
| Result: | Reduced right ventricular hypertrophy. The protection involves a reduction in the expression of p53 (that promotes cardiomyocyte death) and an increase in the expression of anti-oxidant nuclear factor Nrf-2. |
IC 50
SphK1
storage
Desiccate at RT
PF-543 Preparation Products And Raw materials
Raw materials
Preparation Products
PF-543 Suppliers
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