W146 (trifluoroacetate salt)
(Synonyms: [(3R)-3-氨基-4-[(3-己基苯基)氨基]-4-氧代丁基]-膦酸单(三氟乙酸盐)) 目录号 : GC45155A selective S1P1 receptor antagonist
Cas No.:909725-62-8
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >95.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Sphingosine-1-phosphate (S1P) is a bioactive lipid that exhibits a broad spectrum of biological activities including cell proliferation, survival, migration, cytoskeletal organization, and morphogenesis. [1][2][3] It exerts its activity by binding to five distinct G protein-coupled receptors, S1P1/EDG-1, S1P2/EDG-5, S1P3/EDG-3, S1P4/EDG-6, and S1P5/EDG-8. W146 is a S1P1 receptor antagonist that exhibits a Ki value of 77 nM for the human receptor in a GTP-γS binding assay with equipotency at the murine S1P1 receptor (2a = W146; 2b = W140 in supplemental material). [4] No agonist or antagonist activity was observed at 10 µM W146 at S1P2, S1P3, or S1P5 receptors. W146 is active in vivo causing skin capillary leakage in murine lung and skin as well as inhibition of S1P1 agonist-induced lymphocyte sequestration. The half-life of W146 in rat blood is 73 minutes.
Reference:
[1]. Takuwa, Y., Takuwa, N., and Sugimoto, N. The Edg family G protein-coupled receptors for lysophospholipids: Their signaling properties and biological activities. J. Biochem. 131(6), 767-771 (2002).
[2]. Ishii, I., Fukushima, N., Ye, X., et al. Lysophospholipid receptors: Signaling and biology. Annu. Rev. Biochem. 73, 321-354 (2004).
[3]. Kluk, M.J., and Hla, T. Signaling of sphingosine-1-phosphate via the S1P/EDG-family of G-protein-coupled receptors. Biochim. Biophys. Acta 1582(1-3), 72-80 (2002).
[4]. Sanna, M.G., Wang, S.K., Gonzalez-Cabrera, P.J., et al. Enhancement of capillary leakage and restoration of lymphocyte egress by a chiral S1P1 antagonist in vivo. Nature Chemical Biology 2(8), 434-441 (2006).
| Cas No. | 909725-62-8 | SDF | |
| 别名 | [(3R)-3-氨基-4-[(3-己基苯基)氨基]-4-氧代丁基]-膦酸单(三氟乙酸盐) | ||
| 化学名 | [3R-amino-4-[(3-hexylphenyl)amino]-4-oxobutyl]-phosphonic acid, mono(trifluoroacetate) | ||
| Canonical SMILES | CCCCCCC1=CC=CC(NC([C@H](N)CCP(O)(O)=O)=O)=C1.FC(F)(C(O)=O)F | ||
| 分子式 | C18H28F3NO6P | 分子量 | 456.39 |
| 溶解度 | 0.1mg/mL in methanol | 储存条件 | Store at -20°C,protect from light |
| 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 | 2.1911 mL | 10.9555 mL | 21.9111 mL |
| 5 mM | 0.4382 mL | 2.1911 mL | 4.3822 mL |
| 10 mM | 0.2191 mL | 1.0956 mL | 2.1911 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。