VPC 23019 |
| Katalog-Nr.GC15694 |
VPC 23019, ein Arylamid-haltiges Sphingosin-1-phosphat (S1P)-Analogon, ist ein kompetitiver Antagonist an den S1P1- und S1P3-Rezeptoren (pKi = 7,86 bzw. 5,93) und ein Agonist an den S1P4- und S1P5-Rezeptoren (pEC50 = 6,58 und 7.07).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 449173-19-7
Sample solution is provided at 25 µL, 10mM.
_1-3.$$$39978408@51.jpg');)
_1-9.$$$38538795@65.jpg');)
_1-9.$$$39112701@51.jpg');)
_1-7.$$$37316672@70.jpg');)
_366-372.$$$36198801@70.jpg');)
.$$$38565142@65.jpg');)
_1867-1883.$$$33248023@67.jpg');)
_eads6055.$$$39977546@45.jpg');)
_eadm9805.$$$40080571@45.jpg');)
_eadj3020.$$$39666821@45.jpg');)
_1-20.$$$39757301@28.jpg');)
_1-24.$$$38898113@28.jpg');)
_273-287.$$$36806353@46.jpg');)
_1-16.$$$37156877@44.jpg');)
_1-19.$$$37460805@44.jpg');)
_1291-1307.$$$34518654@46.jpg');)
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 |
| Löslichkeit | 0.25mg/mL in DMSO | Storage | Store at 2-8°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 | 537.1 μL | 2.6853 mL | 5.3706 mL |
| 10 mM | 268.5 μL | 1.3426 mL | 2.6853 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 24 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *