NIBR-0213

CAS No. 1233332-14-3

NIBR-0213( NIBR 0213 | NIBR0213 )

Catalog No. M27904 CAS No. 1233332-14-3

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

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    NIBR-0213
  • Note
    Research use only, not for human use.
  • Brief Description
    NIBR-0213, a potent and selective S1P(1) antagonist, has efficacy in experimental autoimmune encephalomyelitis.
  • Description
    NIBR-0213, a potent and selective S1P(1) antagonist, has efficacy in experimental autoimmune encephalomyelitis.(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.(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. 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.
  • In Vitro
    NIBR-0213 displays an inhibitory activity on hS1P1?with an IC50?of 2.5?nM whereas it is inactive (IC50?>10?μM) on S1P2, S1P3, and S1P4?in Ca2+?mobilization assays.NIBR-0213 displays potent and comparable potency on human and rat S1P1?(IC50?of 2.0?nM and 2.3?nM, respectively) in GTPγ35S assays, whereas on mouse S1P1?with an IC50?of 8.5?nM.NIBR-0213 shows an ~3,000-fold selectivity against human S1P5?in the GTPγ35S assay. NIBR-0213 is a competitive S1P1?antagonist with a calculated Kd?of 0.37±0.031?nM.
  • In Vivo
    NIBR-0213 (given orally at 30?mg/kg to rats) reduces the peripheral blood lymphocyte?(PBL) counts by 75%-85% within 14?hr and maintained this effect up to 24?hr posttreatment.NIBR-0213 (30?mg/kg and 60?mg/kg) is efficacious when given therapeutically in a mouse experimental autoimmune encephalomyelitis (EAE) model.The PK properties of NIBR-0213 shows a moderate clearance (26?mL/min/kg) and a high oral bioavailability (69%), leading to significant exposure after oral dosing. Animal Model:Lewis or Wistar rats (220-250 g, males)Dosage:30?mg/kg Administration:Orally Result:Reduced the PBL counts by 75%-85% within 14?hr and maintained this effect up to 24?hr posttreatment.Animal Model:C57BL/6 mice bearing EAE model Dosage:30?mg/kg and 60?mg/kg Administration:30?mg/kg twice per day (BID) for 3?days and then increased to 60?mg/kg BID until the remainder of the experiment. In total, the treatment lasted 26?days Result:Resulted in a gradual reduction in disease-scores, with a divergence from vehicle controls that became significant after 5?days.
  • Synonyms
    NIBR 0213 | NIBR0213
  • Pathway
    Others
  • Target
    Other Targets
  • Recptor
    ——
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    1233332-14-3
  • Formula Weight
    464.99
  • Molecular Formula
    C27H29ClN2O3
  • Purity
    >98% (HPLC)
  • Solubility
    ——
  • SMILES
    C[C@H](NC(=O)c1c(C)cc(cc1C)-c1cccc(N[C@H](C)c2ccc(Cl)c(C)c2)c1)C(O)=O
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1.Harroun SG, et al. Biomarkers of cigarette smoking and DNA methylating agents: Raman, SERS and DFT study of 3-methyladenine and 7-methyladenine. Spectrochim Acta A Mol Biomol Spectrosc. 2017 Apr 5;176:1-7.
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