TASP0277308
目录号 : GC91690TASP0277308 is a sphingosine-1-phosphate receptor 1 (S1P1) antagonist (IC50 = 4.2 nM).
Cas No.:945725-50-8
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
TASP0277308 is a sphingosine-1-phosphate receptor 1 (S1P1) antagonist (IC50 = 4.2 nM).[1] It is selective for S1P1 over S1P3, S1P4, and S1P5 (IC50s = >10,000, >10,000, and 8,756 nM, respectively). TASP0277308 inhibits S1P-induced [35S]GTPγS binding and forskolin-induced cAMP production in HEK293 cells expressing human S1P1 (IC50s = 7.8 and 4.3 nM, respectively). It inhibits S1P-induced migration of CHO cells expressing human S1P1 (IC50 = 18 nM). In vivo, TASP0277308 (100 mg/kg) induces lymphopenia in mice. It reduces bone erosion in a mouse model of collagen-induced arthritis. Intrathecal administration of TASP0277308 (3 or 10 nmol/animal) reduces flinching and guarding behaviors in a mouse model of cancer-induced bone pain.[2]
References:
[1].Fujii, Y., Hirayama, T., Ohtake, H., et al.Amelioration of collagen-induced arthritis by a novel S1P1 antagonist with immunomodulatory activitiesJ. Immunol.188(1)206-215(2012).
[2].Grenald, S.A., Doyle, T.M., Zhang, H., et al.Targeting the S1P/S1PR1 axis mitigates cancer-induced bone pain and neuroinflammationPain158(9)1733-1742(2017).
| Cas No. | 945725-50-8 | SDF | Download SDF |
| 分子式 | C23H28Cl2N6O3S | 分子量 | 539.5 |
| 溶解度 | DMSO: Sparingly soluble: 1-10 mg/ml,Methanol: Slightly soluble: 0.1-1 mg/ml | 储存条件 | -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 | 1.8536 mL | 9.2678 mL | 18.5357 mL |
| 5 mM | 0.3707 mL | 1.8536 mL | 3.7071 mL |
| 10 mM | 0.1854 mL | 0.9268 mL | 1.8536 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。