TASP0277308 |
カタログ番号GC91690
One-Click Copy Product Info
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TASP0277308 is a sphingosine-1-phosphate receptor 1 (S1P1) antagonist (IC50 = 4.2 nM).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 945725-50-8
Sample solution is provided at 25 µL, 10mM.
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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 | |
| Formula | C23H28Cl2N6O3S | M.Wt | 539.5 |
| 溶解度 | DMSO: Sparingly soluble: 1-10 mg/ml,Methanol: Slightly soluble: 0.1-1 mg/ml | Storage | -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. |
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| 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 | 1.8536 mL | 9.2678 mL | 18.5357 mL |
| 5 mM | 370.7 μL | 1.8536 mL | 3.7071 mL |
| 10 mM | 185.4 μL | 926.8 μL | 1.8536 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 saline, 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: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)