PF-543 Citrate

未知

PF-543 柠檬酸盐

2-Hydroxypropane-1,2,3-tricarboxylic acid--[(2R)-1-{[4-({3-[(benzenesulfonyl)methyl]-5-methylphenoxy}methyl)phenyl]methyl}pyrrolidin-2-yl]methanol (1/1) | Sphingosine Kinase 1 Inhibitor II (Citrate) | (R)-(1-(4-((3-methyl-5-(phenylsulfonylmethyl)phenoxy)m

PF-543 Citrate

P647407-5mg

5mg

≥98%

2-8°C储存,干燥

冰袋运输

PF-543 Citrate (Sphingosine Kinase 1 Inhibitor II Citrate) is a potent, selective, reversible and sphingosine-competitive SPHK1 inhibitor with an IC 50 of 2 nM and a K i of 3.6 nM. PF-543 Citrate is >100-fold selectivity for SPHK1 over SPHK2 . PF-543 Citrate is an effective potent inhibitor of sphingosine 1-phosphate (S1P) formation in whole blood with an IC 50 of 26.7 nM. PF-543 Citrate induces apoptosis , necrosis, and autophagy In Vitro PF-543 (10-1000 nM; 24?hours; PASM cells) treatment abolishes SK1 expression at nM concentrations. ?\nPF-543 (0.1-10 μM; 24 hours; PASM cells) treatment induces caspase-3/7 activity. ?\nPF-543 inhibits C 17 -S1P formation in 1483 cells with an IC 50 of 1.0 nM. ?\nSphK1 inhibition by PF-543 causes a dose-dependent depletion of the intracellular level of S1P with EC 50 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: Human pulmonary arterial smooth muscle (PASM) cells Concentration: 10 nM, 100 nM, 1000 nM Incubation Time: 24 hours Result: Abolished SK1 expression at nM concentrations. Apoptosis AnalysisCell Line: Human pulmonary arterial smooth muscle (PASM) cells Concentration: 0.1 μM, 1 μM, 10 μM Incubation Time: 24 hours Result: Induced caspase-3/7 activity in cultured human pulmonary smooth muscle cells. 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. ?\nMice are initially dosed (ip) with 10 mg/kg or 30 mg/kg of PF-543 for 24 h and the T 1/2 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Female C57BL/6 J mice (7-12 week-old) with hypoxic-induced pulmonary arterial hypertensionDosage: 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. Form:Solid IC50& Target:SphK1

PF-543 Citrate（鞘氨醇激酶 1 抑制剂 II Citrate）是一种强效、选择性、可逆和鞘氨醇竞争性 SPHK1 抑制剂，其 IC 50 为 2 nM，K i 为 3.6 nM。PF-543 Citrate 对 SPHK1 的选择性大于 SPHK2 的 100 倍。PF-543 枸橼酸盐

1415562-83-2

C33H39NO11S

657.73 g/mol

71576669

CC1=CC(=CC(=C1)OCC2=CC=C(C=C2)CN3CCC[C@@H]3CO)CS(=O)(=O)C4=CC=CC=C4.C(C(=O)O)C(CC(=O)O)(C(=O)O)O

[(2R)-1-[[4-[[3-(benzenesulfonylmethyl)-5-methylphenoxy]methyl]phenyl]methyl]pyrrolidin-2-yl]methanol;2-hydroxypropane-1,2,3-tricarboxylic acid

1S/C27H31NO4S.C6H8O7/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;7-3(8)1-6(13,5(11)12)2-4(9)10/h2-4,7-12,14-16,25,29H,5-6,13,17-20H2,1H3;13H,1-2H2,(H,7,8)(H,9,10)(H,11,12)/t25-;/m1./s1

PWXXWUWKNPXSGW-VQIWEWKSSA-N

CC1=CC(=CC(=C1)OCC2=CC=C(C=C2)CN3CCCC3CO)CS(=O)(=O)C4=CC=CC=C4.C(C(=O)O)C(CC(=O)O)(C(=O)O)O

71576669

1415562-83-2

DMSO : ≥ 100 mg/mL (152.04 mM) H2O : 50 mg/mL (76.02 mM; Need ultrasonic)

5

12

14

657.224 Da

657.224 Da

207.000 Ų

46

0

906.000

0

2