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NIBR-0213

Catalog No. T28169 CAS 1233332-14-3

Synonyms: NIBR 0213

NIBR-0213, a potent and selective S1P(1) antagonist, has efficacy in experimental autoimmune encephalomyelitis.

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NIBR-0213, CAS 1233332-14-3

Pack Size	Availability	Price/USD
1 mg	In stock	$ 39.00
2 mg	In stock	$ 54.00
5 mg	In stock	$ 77.00
10 mg	In stock	$ 113.00
25 mg	In stock	$ 229.00
1 mL * 10 mM (in DMSO)	In stock	$ 117.00

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Purity: 98.87%

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Description	NIBR-0213, a potent and selective S1P(1) antagonist, has efficacy in experimental autoimmune encephalomyelitis.
Targets&IC50	S1P1:2.0 nM(GTPγ35S,human), S1P1:2.3 nM(GTPγ35S,rat), S1P1:2.5 nM(Ca2+ mobilization), S1P1:8.5 nM(GTPγ35S,mouse)
In vitro	In Ca2+?mobilization assays, NIBR-0213 displayed an inhibitory activity on hS1P1?with an IC50?of 2.5?nM whereas it was inactive (IC50?> 10?μM) on S1P2, S1P3, and S1P4. In GTPγ35S assays, NIBR-0213 displayed potent and comparable potency on human and rat S1P1?(IC50?of 2.0?nM and 2.3?nM, respectively), whereas on mouse S1P1?a slightly reduced IC50?of 8.5?nM was?measured. NIBR-0213 showed an ～3,000-fold selectivity against human S1P5?in the GTPγ35S assay (Figure?3A). On S1P4, a weak agonistic activity was detected with an EC50?of 245?nM. Schild plot analysis indicated that NIBR-0213 is a competitive S1P1?antagonist with a calculated Kd?of 0.37?± 0.031?nM[2].
In vivo	NIBR-0213 increased in a dose-dependent manner the leakage of?plasma proteins?into lung parenchyma, as measured by the increase in EBD in lung tissues at 6?hr posttreatment (time of Emax on PBL). A maximum of 4–5-fold EBD increase versus vehicle controls was observed with 0.3?mg/kg. An ED50?of ～0.1?mg/kg could be estimated, i.e., in the range of the ED50?for the effects on PBL counts[2]. NIBR-0213 given orally at 30 mg/kg to rats reduced the PBL counts by 75%–85% within 14 hr and maintained this effect up to 24 hr posttreatment[2].

Synonyms	NIBR 0213
Molecular Weight	464.98
Formula	C27H29ClN2O3
CAS No.	1233332-14-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 55 mg/ml (118.28 mM)

References and Literature

1. Bigaud M, Dincer Z, Bollbuck B, Dawson J, Beckmann N, Beerli C, Fishli-Cavelti G, Nahler M, Angst D, Janser P, Otto H, Rosner E, Hersperger R, Bruns C, Quancard J. Pathophysiological Consequences of a Break in S1P1-Dependent Homeostasis of Vascular Permeability Revealed by S1P1 Competitive Antagonism. PLoS One. 2016 Dec 22;11(12):e0168252. doi: 10.1371/journal.pone.0168252. eCollection 2016. PubMed PMID: 28005953; PubMed Central PMCID: PMC5179015. 2. Quancard J, Bollbuck B, Janser P, Angst D, Berst F, Buehlmayer P, Streiff M, Beerli C, Brinkmann V, Guerini D, Smith PA, Seabrook TJ, Traebert M, Seuwen K, Hersperger R, Bruns C, Bassilana F, Bigaud M. A potent and selective S1P(1) antagonist with efficacy in experimental autoimmune encephalomyelitis. Chem Biol. 2012 Sep 21;19(9):1142-51. doi: 10.1016/j.chembiol.2012.07.016. PubMed PMID: 22999882. 3. Obinata H, Hla T. Fine-tuning S1P therapeutics. Chem Biol. 2012 Sep 21;19(9):1080-2. doi: 10.1016/j.chembiol.2012.09.002. PubMed PMID: 22999874; PubMed Central PMCID: PMC3625427.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library GPCR Compound Library Bioactive Compound Library Bioactive Compounds Library Max

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Keywords

NIBR-0213 1233332-14-3 GPCR/G Protein LPL Receptor NIBR 0213 Lysophospholipid Receptor NIBR0213 S1P1 Inhibitor encephalomyelitis autoimmune inhibit inhibitor

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