VPC 23019 |
| رقم الكتالوجGC15694 |
VPC 23019 ، وهو نظير يحتوي على أريل أميد 1-فوسفات (S1P) ، هو مضاد تنافسي في مستقبلات S1P1 و S1P3 (pKi = 7.86 و 5.93 ، على التوالي) وناهض في S1P4 ومستقبلات S1P5 (pEC50 = 6.58 و 7.07 على التوالي)
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Cas No.: 449173-19-7
Sample solution is provided at 25 µL, 10mM.
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VPC 23019, phosphoric acid mono-[2-amino-2-(3-octyl-phenylcarbamoyl)-ethyl] ester, is an S1P1/S1P3 receptor antagonist. S1P is short for sphingosine-1-phosphate [1]. VPC 23019 abolished S1P-induced, cell migration, Gi-dependent Rac stimulation and tube formation [2]. VPC 23019 inhibited SIP1 activity with an IC50 value of 8 nM [3].
S1P can act on specific G protein-coupled receptors. 5 subtypes of these receptors have been found and termed S1P1–5. These receptors couple to intracellular second messenger systems including intracellular Ca2+, phospholipase C, adenylyl cyclase, phosphatidylinositol 3 (PI3)-kinase, mitogen-activated protein kinases, protein kinase Akt, and Ras- and Rho-dependent pathways [1].
In the bEnd.3 cell line, VPC 23019 did not affect basal NO production. Preincubation with 10 µmol/L VPC 23019 made Ang II–induced NO production decrease to approximately basal level [1]. S1P, in a dose-dependent manner, stimulated trans-well migration of mouse vascular endothelial cells with a peak response at 10-7M. VPC 23019 was able to abolish this stimulatory effect of S1P [2]. Preincubation with 10 µM of VPC 23019 partially inhibited S1P-induced calcium increase in L2071 cells [4].
In rat, VPC 23019 significantly increased the S1P-induced vasoconstriction in preparation with intact endothelium (P< 0.01), but did not change it in preparation without endothelium. In intact mouse basilar artery (relaxation to ACh, 45.6±7.2%, n= 16), VPC 23019 left-shifted the concentration-contraction curve to S1P by a half log. VPC 23019 did not modify contractile responses to 5-HT, KCl or U46619 [5].
References:
[1]. Arthur C.M. Mulders, Mariëlle C. Hendriks-Balk, Marie-Jeanne Mathy, et al. Sphingosine Kinase-dependent Activation of Endothelial Nitric Oxide Synthase by Angiotensin II. Arterioscler Thromb Vasc Biol., 2006, 26:2043-2048.
[2]. Isao Inoki, Noriko Takuwa, Naotoshi Sugimoto, et al. Negative regulation of endothelial morphogenesis and angiogenesis by S1P2 receptor. Biochemical and Biophysical Research Communications, 2006, 346: 293-300.
[3]. Ju Wang, Zi-Qi Shi, Xiaojun Xu, et al. Triptolide Inhibits Amyloid-β Production and Protects Neural Cells by Inhibiting CXCR2 Activity. Journal of Alzheimer’s Disease, 2013, 33:1-2.
[4]. Mi-Kyoung Kim, Kyoung Sun Park, Hyuck Lee, et al. Phytosphingosine-1-phosphate stimulates chemotactic migration of L2071 mouse fibroblasts via pertussis toxin-sensitive G-proteins. Exp. Mol. Med., 2007, 39(2):185-194.
[5]. S Salomone, EM Potts, S Tyndall, et al. Analysis of sphingosine 1-phosphate receptors involved in constriction of isolated cerebral arteries with receptor null mice and pharmacological tools. British Journal of Pharmacology, 2008, 153:140-147.
| Cas No. | 449173-19-7 | SDF | |
| Chemical Name | (R)-2-amino-3-((3-octylphenyl)amino)-3-oxopropyl dihydrogen phosphate | ||
| Canonical SMILES | O=C([C@@H](COP(O)(O)=O)N)NC1=CC(CCCCCCCC)=CC=C1 | ||
| Formula | C17H29N2O5P | M.Wt | 372.4 |
| الذوبان | 0.25mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.6853 mL | 13.4264 mL | 26.8528 mL |
| 5 mM | 0.5371 mL | 2.6853 mL | 5.3706 mL |
| 10 mM | 0.2685 mL | 1.3426 mL | 2.6853 mL |
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- Purity: >95.00%
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