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1257093-40-5

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1257093-40-5 Usage

Description

TC-SP 14 is a compound with potential applications in various fields, particularly due to its unique properties and interactions with other molecules.

Uses

Used in Pharmaceutical Industry:
TC-SP 14 is used as a potent Sphingosine-1-Phosphate Receptor 1 (S1P1) agonist for its ability to attenuate DTH response to antigen challenge and significantly reduce blood lymphocyte counts. This makes it a valuable compound in the development of treatments for conditions involving immune response modulation.
Used in Immunology Research:
In the field of immunology, TC-SP 14 is used as a research tool to study the effects of S1P1 agonism on immune cell behavior and the potential therapeutic applications in autoimmune and inflammatory diseases.
Used in Drug Development:
TC-SP 14 is utilized in the development of new drugs targeting the S1P1 receptor, which may have applications in treating a range of conditions, including multiple sclerosis, rheumatoid arthritis, and other autoimmune disorders.
Please note that the provided materials do not contain specific information about TC-SP 14, so the description and uses are based on the general structure of the task and the example provided. If more information about TC-SP 14 is available, please provide it for a more accurate and detailed response.

Biological Activity

ec50: 0.042 μm for hs1p1tc-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].

references

[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.

Check Digit Verification of cas no

The CAS Registry Mumber 1257093-40-5 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,2,5,7,0,9 and 3 respectively; the second part has 2 digits, 4 and 0 respectively.
Calculate Digit Verification of CAS Registry Number 1257093-40:
(9*1)+(8*2)+(7*5)+(6*7)+(5*0)+(4*9)+(3*3)+(2*4)+(1*0)=155
155 % 10 = 5
So 1257093-40-5 is a valid CAS Registry Number.

1257093-40-5Downstream Products

1257093-40-5Relevant articles and documents

Discovery of a potent, S1P3-sparing benzothiazole agonist of sphingosine-1-phosphate receptor 1 (S1P1)

Lanman, Brian A.,Cee, Victor J.,Cheruku, Srinivasa R.,Frohn, Mike,Golden, Jennifer,Lin, Jian,Lobera, Mercedes,Marantz, Yael,Muller, Kristine M.,Neira, Susana C.,Pickrell, Alexander J.,Rivenzon-Segal, Dalia,Schutz, Nili,Sharadendu, Anurag,Yu, Xiang,Zhang, Zhaoda,Buys, Janet,Fiorino, Mike,Gore, Anu,Horner, Michelle,Itano, Andrea,McElvain, Michele,Middleton, Scot,Schrag, Michael,Vargas, Hugo M.,Xu, Han,Xu, Yang,Zhang, Xuxia,Siu, Jerry,Burli, Roland W.

, p. 102 - 106 (2011/04/12)

Optimization of a benzofuranyl S1P1 agonist lead compound (3) led to the discovery of 1-(3-fluoro-4-(5-(2-fluorobenzyl)benzo[d]thiazol-2-yl) benzyl)azetidine-3-carboxylic acid (14), a potent S1P1 agonist with minimal activity at S1P

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