A potent and selective S1P1 antagonist (IC50s = 2.5 and 2.0 nM for hS1P1 Ca2+ mobilization and in a GTPγS assay); inactive at S1P2

NIBR0213 – 5 mg

Brand:
Cayman
CAS:
1233332-14-3
Storage:
-20
UN-No:
Non-Hazardous - /

NIBR0213 is an orally bioavailable, potent, and selective antagonist of sphingosine-1-phosphate receptor-1 (S1P1) with IC50 values of 2.5 and 2.0 nM for the hS1P1 in a Ca2+ mobilization assay and GTPγS assay, respectively.{34640} It is inactive at S1P2, S1P3, and S1P4 receptors (IC50s = >20, >10, and >10 µM, respectively in a Ca2+ mobilization assay). S1P1 plays a key role in the immune system, regulating lymphocyte egress from lymphoid tissues into the circulation.{15122} In rats, NIBR0213 (30 mg/kg) reduces peripheral blood lymphocytes by 75-85% for up to 24 hours.{34640} In a mouse model of experimental autoimmune encephalitis (EAE), it significantly reduces disease severity up to 26 days, when administered at 30 mg/kg twice per day for three days, then 60 mg/kg twice per day. However, in a rat model of adjuvant-induced arthritis, chronic administration of 30 mg/kg induces pulmonary damage and chronic lung inflammation.{34639}  

 

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Description

A potent and selective S1P1 antagonist (IC50s = 2.5 and 2.0 nM for hS1P1 Ca2+ mobilization and in a GTPγS assay); inactive at S1P2, S1P3, and S1P4 receptors (IC50s = >20, >10, and >10 µM, respectively in a Ca2+ mobilization assay); reduces EAE disease severity in mice up to 26 days; induces pulmonary damage in rats when administered chronically

Formal name: N-[[3′-[[(1R)-1-(4-chloro-3-methylphenyl)ethyl]amino]-3,5-dimethyl[1,1′-biphenyl]-4-yl]carbonyl]-L-alanine

Synonyms: 

Molecular weight: 465

CAS: 1233332-14-3

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Immunology & Inflammation|Adaptive Immunity||Research Area|Immunology & Inflammation|Autoimmunity

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