| CAS NO: | 1257093-40-5 |
| 包装 | 价格(元) |
| 10mg | 电议 |
| 50mg | 电议 |
| Cas No. | 1257093-40-5 |
| 化学名 | 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 |
| 分子式 | C25H20F2N2O2S |
| 分子量 | 450.5 |
| 溶解度 | <22.52mg/ml in DMSO |
| 储存条件 | Desiccate at RT |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
| 产品描述 | 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: |
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