PF-543 CitrateSphK1 inhibitor,potent and cell-permeate CAS# 1415562-83-2 |
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Quality Control & MSDS
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| Cas No. | 1415562-83-2 | SDF | Download SDF |
| PubChem ID | 71576669 | Appearance | Powder |
| Formula | C33H39NO11S | M.Wt | 657.73 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | DMSO : ≥ 100 mg/mL (152.04 mM) H2O : 50 mg/mL (76.02 mM; Need ultrasonic) *"≥" means soluble, but saturation unknown. | ||
| Chemical Name | [(2R)-1-[[4-[[3-(benzenesulfonylmethyl)-5-methylphenoxy]methyl]phenyl]methyl]pyrrolidin-2-yl]methanol;2-hydroxypropane-1,2,3-tricarboxylic acid | ||
| SMILES | 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 | ||
| Standard InChIKey | PWXXWUWKNPXSGW-VQIWEWKSSA-N | ||
| Standard InChI | InChI=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 | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | PF-543 Citrate is a novel cell-permeant inhibitor of SPHK1 with a Ki of 4.3 nM and more than 100-fold selectivity for SPHK1 over SPHK2.In Vitro:PF-543 is a novel selective sphingosine-competitive inhibitor of SphK1 that is over 1000-fold more potent in suppressing cellular S1P formation than DMS and SKI-2, commonly used pharmacological tools for SphK. PF-543 inhibits SphK1 with a Ki of 3.6 nM, is sphingosine-competitive and is more than 100-fold selective for SphK1 over the SphK2 isoform. In 1483 head and neck carcinoma cells, which are characterized by high levels of SphK1 expression and an unusually high rate of S1P production, PF-543 decreases the level of endogenous S1P 10-fold with a proportional increase in the level of sphingosine[1]. PF-543 inhibits SphK1 in the in vitro enzyme assay with an IC50 value of 2.0±0.6 nM and is able to inhibit the enzyme >95% at a concentration of 20 nM[1]. PF-543 bounds in a bent conformation analogous to that expected of a bound sphingosine substrate but with a rotated head group[2].In Vivo:Administration of the potent sphingosine kinase 1 inhibitor, PF-543 in a mouse hypoxic model of pulmonary hypertension has no effect on vascular remodelling but reduces right ventricular hypertrophy. Administration of 10 mg/kg PF-543 for 24 h to mice induces a decrease in SK1 expression in pulmonary vessels[3]. References: | |||||
PF-543 Citrate Dilution Calculator
PF-543 Citrate Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 1.5204 mL | 7.6019 mL | 15.2038 mL | 30.4076 mL | 38.0095 mL |
| 5 mM | 0.3041 mL | 1.5204 mL | 3.0408 mL | 6.0815 mL | 7.6019 mL |
| 10 mM | 0.152 mL | 0.7602 mL | 1.5204 mL | 3.0408 mL | 3.801 mL |
| 50 mM | 0.0304 mL | 0.152 mL | 0.3041 mL | 0.6082 mL | 0.7602 mL |
| 100 mM | 0.0152 mL | 0.076 mL | 0.152 mL | 0.3041 mL | 0.3801 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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PF-543 is a novel cell-permeant inhibitor of SphK1. PF-543 inhibits SphK1 with a K(i) of 3.6 nM, is sphingosine-competitive and is more than 100-fold selective for SphK1 over the SphK2 isoform. PF-543 is the most potent inhibitor of SphK1 described to date and it will be useful for dissecting specific roles of SphK1-driven S1P signalling.
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