TC-SP 14 |
| Katalog-Nr.GC17019 |
TC-SP 14 (Verbindung 14) ist ein oral aktiver und potenter S1P1-Agonist (EC50 = 0,042 μM) mit minimaler AktivitÄt bei S1P3 (EC50 = 3,47 μM).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1257093-40-5
Sample solution is provided at 25 µL, 10mM.
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EC50: 0.042 μM for hS1P1
TC-SP 14 is an agonist of Sphingosine-1-Phosphate Receptor 1 (S1P1).
Studies have revealed that the lysophospholipid sphingosine-1-phosphate (S1P1) is a pleiotropic modulator of diverse cellular processes. Such effects are reported to be mediated by the interactions of S1P with a set of paralogous G proteincoupled receptors, which are widely expressed in the immune, central nervous and cardiovascular systems.
In vitro: As a small lipophilic substituent proved equally effective to a larger substituent in reducing S1P3 activity, TC-SP 14 was screened. TC-SP 14 was found to be a potent S1P1 agonist (EC50 = 0.042 μM) with reduced activity for S1P3 (EC50 = 3.47 μM) [1].
In vivo: In Lewis rats, TC-SP 14 produced a dose-dependent reduction in circulating blood lymphocytes, which was consistent with S1P1 agonism. Moreover, statistical significance was shown at a dose of 0.3 mg/kg, and the dose fo 3.0 mg/kg led to near maximal lymphopenia. TC-SP 14 was subsequently investigated in a DTH antigen challenge model. Results showed a statistically significant reduction in ear swelling at doses of 0.3 mg/kg and higher. In addition, reduced ear swelling was found to closely track circulating lymphocyte counts [1].
Clinical trial: N/A
Reference:
[1] Lanman BA,Cee VJ,Cheruku SR et al. Discovery of a Potent, S1P3-Sparing Benzothiazole Agonist of Sphingosine-1-Phosphate Receptor 1 (S1P1). ACS Med Chem Lett.2010 Nov 9;2(2):102-6.
| Cas No. | 1257093-40-5 | SDF | |
| Chemical Name | 1-(3-fluoro-4-(5-(2-fluorobenzyl)benzo[d]thiazol-2-yl)benzyl)azetidine-3-carboxylic acid | ||
| Canonical SMILES | FC1=CC=CC=C1CC2=CC(N=C3C4=C(F)C=C(CN5CC(C(O)=O)C5)C=C4)=C(S3)C=C2 | ||
| Formula | C25H20F2N2O2S | M.Wt | 450.5 |
| Löslichkeit | <22.52mg/ml in DMSO | Storage | Desiccate at RT |
| 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 | 2.2198 mL | 11.0988 mL | 22.1976 mL |
| 5 mM | 0.444 mL | 2.2198 mL | 4.4395 mL |
| 10 mM | 0.222 mL | 1.1099 mL | 2.2198 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: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 40 reference(s) in Google Scholar.)
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