VPC 23019
目录号 : GC15694A sphingosine-1-phosphate receptor antagonist
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 | |
| 化学名 | (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 | ||
| 分子式 | C17H29N2O5P | 分子量 | 372.4 |
| 溶解度 | 0.25mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >95.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet