Product Name :
PF-543 hydrochloride
Description:
PF-543 hydrochloride (Sphingosine Kinase 1 Inhibitor II hydrochloride) is a potent, selective, reversible and sphingosine-competitive SPHK1 inhibitor with an IC50 of 2 nM and a Ki of 3.6 nM. PF-543 hydrochloride is >100-fold selectivity for SPHK1 over SPHK2. PF-543 hydrochloride is an effective potent inhibitor of sphingosine 1-phosphate (S1P) formation in whole blood with an IC50 of 26.7 nM. PF-543 hydrochloride induces apoptosis, necrosis, and autophagy.
CAS:
1706522-79-3
Molecular Weight:
502.07
Formula:
C27H32ClNO4S
Chemical Name:
[(2R)-1-{[4-({3-[(benzenesulfonyl)methyl]-5-methylphenoxy}methyl)phenyl]methyl}pyrrolidin-2-yl]methanol hydrochloride
Smiles :
Cl.CC1C=C(CS(=O)(=O)C2C=CC=CC=2)C=C(C=1)OCC1C=CC(CN2CCC[C@@H]2CO)=CC=1
InChiKey:
WNKWAZFYPZMDGJ-VQIWEWKSSA-N
InChi :
InChI=1S/C27H31NO4S.ClH/c1-21-14-24(20-33(30,31)27-7-3-2-4-8-27)16-26(15-21)32-19-23-11-9-22(10-12-23)17-28-13-5-6-25(28)18-29;/h2-4,7-12,14-16,25,29H,5-6,13,17-20H2,1H3;1H/t25-;/m1./s1
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.{{Glutathione Agarose} site|{Glutathione Agarose} Epigenetics|{Glutathione Agarose} Technical Information|{Glutathione Agarose} In Vitro|{Glutathione Agarose} custom synthesis}
Shelf Life:
≥12 months if stored properly.
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.
Additional information:
PF-543 hydrochloride (Sphingosine Kinase 1 Inhibitor II hydrochloride) is a potent, selective, reversible and sphingosine-competitive SPHK1 inhibitor with an IC50 of 2 nM and a Ki of 3.6 nM. PF-543 hydrochloride is >100-fold selectivity for SPHK1 over SPHK2. PF-543 hydrochloride is an effective potent inhibitor of sphingosine 1-phosphate (S1P) formation in whole blood with an IC50 of 26.7 nM. PF-543 hydrochloride induces apoptosis, necrosis, and autophagy.|Product information|CAS Number: 1706522-79-3|Molecular Weight: 502.07|Formula: C27H32ClNO4S|Chemical Name: [(2R)-1-{[4-({3-[(benzenesulfonyl)methyl]-5-methylphenoxy}methyl)phenyl]methyl}pyrrolidin-2-yl]methanol hydrochloride|Smiles: Cl.CC1C=C(CS(=O)(=O)C2C=CC=CC=2)C=C(C=1)OCC1C=CC(CN2CCC[C@@H]2CO)=CC=1|InChiKey: WNKWAZFYPZMDGJ-VQIWEWKSSA-N|InChi: InChI=1S/C27H31NO4S.ClH/c1-21-14-24(20-33(30,31)27-7-3-2-4-8-27)16-26(15-21)32-19-23-11-9-22(10-12-23)17-28-13-5-6-25(28)18-29;/h2-4,7-12,14-16,25,29H,5-6,13,17-20H2,1H3;1H/t25-;/m1.{{Pemetrexed disodium} MedChemExpress|{Pemetrexed disodium} Cell Cycle/DNA Damage|{Pemetrexed disodium} Technical Information|{Pemetrexed disodium} Description|{Pemetrexed disodium} custom synthesis|{Pemetrexed disodium} Autophagy} /s1|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.PMID:32063051 |Shelf Life: ≥12 months if stored properly.|Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.|Drug Formulation: To be determined|HS Tariff Code: 382200|How to use|In Vitro:|PF-543 (10-1000 nM; 24 hours; PASM cells) treatment abolishes SK1 expression at nM concentrations. PF-543 (0.1-10 μM; 24 hours; PASM cells) treatment induces caspase-3/7 activity. PF-543 inhibits C17-S1P formation in 1483 cells with an IC50 of 1.0 nM. SphK1 inhibition by PF-543 causes a dose-dependent depletion of the intracellular level of S1P with EC50 concentration of 8.4 nM and a concomitant elevation of the intracellular level of sphingosine in 1483 cells. The level of endogenous S1P in 1483 cells after a 1 h treatment with 200 nM PF-543 is decreased 10-fold, producing a proportional increase in the level of sphingosine.|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. 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.|Products are for research use only. Not for human use.|
