A selective S1P1 receptor agonist (EC50 = 1.2 nM); highly selective for S1P1 with EC50 values of >10

AUY954 – 5 mg

Brand:
Cayman
CAS:
820240-77-5
Storage:
-20
UN-No:
Non-Hazardous - /

AUY954 is an orally bioavailable and selective agonist of the sphingosine-1-phosphate receptor 1 (S1P1; EC50 = 1.2 nM for stimulating GTPγS binding to S1P1 in CHO cells).{14536} It is highly selective for the S1P1 receptor with EC50 values of >10,000, 1,210, >1,000, and 340 nM for S1P2, S1P3, S1P4, and S1P5 receptors, respectively. AUY954 reduces circulating lymphocytes and prevents rejection of rat heart allografts. In a rat model of experimental autoimmune neuritis, chronic treatment with AUY954 (10 mg/kg), starting on the day of immunization, almost completely prevents peripheral paralysis.{37100} In the same model, it also decreases T cell, B cell, and macrophage infiltration and perivascular demyelination in sciatic nerves.  

 

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SKU: 9000548 - 5 mg Category:

Description

A selective S1P1 receptor agonist (EC50 = 1.2 nM); highly selective for S1P1 with EC50 values of >10,000, 1,210, >1,000, and 340 nM for S1P2, S1P3, S1P4, and S1P5 receptors, respectively; reduces circulating lymphocytes and prevents rejection of rat heart allografts; almost completely prevents peripheral paralysis and decreases inflammation in a rat model of experimental autoimmune neuritis at a chronic dose of 10 mg/kg per day

Formal name: N-[[2-[2-(trifluoromethyl)[1,1′-biphenyl]-4-yl]benzo[b]thien-5-yl]methyl]-β-alanine

Synonyms: 

Molecular weight: 455.5

CAS: 820240-77-5

Purity: ≥98%

Formulation: A crystalline solid

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