NIBR0213

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NIBR0213

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Cat No: 21513

Biochemicals - Receptor Pharmacology

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 S1P...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

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

Correlated keywords:

NIBR-0213 S1P-1 2 3 4 PBL

Product Overview:
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}

Size	1 mg
Shipping	dry ice
CAS Number	1233332-14-3
Molecular Formula	C₂₇H₂₉ClN₂O₃
SMILES	CC1=C(Cl)C=CC([C@@H](C)NC2=CC(C3=CC(C)=C(C(N[C@@H](C)C(O)=O)=O)C(C)=C3)=CC=C2)=C1
Molecular Weight	465
Formulation	A crystalline solid
Purity	≥98%
Custom Code	2903.99
UNSPSC code	12352100

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MSDS

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Cayman Chemical's mission is to help make research possible by supplying scientists worldwide with the basic research tools necessary for advancing human and animal health. Our utmost commitment to healthcare researchers is to offer the highest quality products with an affordable pricing policy.

Our scientists are experts in the synthesis, purification, and characterization of biochemicals ranging from small drug-like heterocycles to complex biolipids, fatty acids, and many others. We are also highly skilled in all aspects of assay and antibody development, protein expression, crystallization, and structure determination.

Over the past thirty years, Cayman developed a deep knowledge base in lipid biochemistry, including research involving the arachidonic acid cascade, inositol phosphates, and cannabinoids. This knowledge enabled the production of reagents of exceptional quality for cancer, oxidative injury, epigenetics, neuroscience, inflammation, metabolism, and many additional lines of research.

Our organic and analytical chemists specialize in the rapid development of manufacturing processes and analytical methods to carry out clinical and commercial GMP-API production. Pre-clinical drug discovery efforts are currently underway in the areas of bone restoration and repair, muscular dystrophy, oncology, and inflammation. A separate group of Ph.D.-level scientists are dedicated to offering Hit-to-Lead Discovery and Profiling Services for epigenetic targets. Our knowledgeable chemists can be contracted to perform complete sample analysis for analytes measured by the majority of our assays. We also offer a wide range of analytical services using LC-MS/MS, HPLC, GC, and many other techniques.

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ISO/IEC 17025:2005
ISO Guide 34:2009

Cayman is a leader in the field of emerging drugs of abuse, providing high-purity Schedule I-V Controlled Substances to federally-licensed laboratories and qualified academic research institutions for forensic analyses. We are certified by ACLASS Accreditation Services with dual accreditation to ISO/IEC 17025:2005 and ISO Guide 34:2009.