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TC-SP 14

Catalog No.GC17019

agonist of Sphingosine-1-Phosphate Receptor 1 (S1P1)

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TC-SP 14 Chemical Structure

Cas No.: 1257093-40-5

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10mg
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50mg
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

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.

Chemical Properties

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
Solubility <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.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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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
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Average Rating: 5 ★★★★★ (Based on Reviews and 40 reference(s) in Google Scholar.)

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