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NIBR-0213

NIBR-0213
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Purity:98.87%
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NIBR-0213

Catalog No. T28169Cas No. 1233332-14-3
NIBR-0213, a potent and selective S1P(1) antagonist, has efficacy in experimental autoimmune encephalomyelitis.
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Pack SizePriceAvailabilityQuantity
1 mg$39In Stock
2 mg$54In Stock
5 mg$77In Stock
10 mg$113In Stock
25 mg$229In Stock
1 mL x 10 mM (in DMSO)$117In Stock
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Product Introduction

Bioactivity
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[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].
AliasNIBR 0213
Chemical Properties
Molecular Weight464.98
FormulaC27H29ClN2O3
Cas No.1233332-14-3
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year
Solubility Information
DMSO: 55 mg/ml (118.28 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.1506 mL10.7532 mL21.5063 mL107.5315 mL
5 mM0.4301 mL2.1506 mL4.3013 mL21.5063 mL
10 mM0.2151 mL1.0753 mL2.1506 mL10.7532 mL
20 mM0.1075 mL0.5377 mL1.0753 mL5.3766 mL
50 mM0.0430 mL0.2151 mL0.4301 mL2.1506 mL
100 mM0.0215 mL0.1075 mL0.2151 mL1.0753 mL

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