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NIBR-0213

Catalog No. T28169Cas No. 1233332-14-3
Alias NIBR 0213

NIBR-0213 is a potent and selective competitive S1P1 antagonist with activity against experimental autoimmune encephalomyelitis. In the GTPγ35S assay, it has IC50 values ​​of 2.0 nM and 2.3 nM for human and rat S1P1, respectively.

NIBR-0213

NIBR-0213

Purity: 98.87%
Catalog No. T28169Alias NIBR 0213Cas No. 1233332-14-3
NIBR-0213 is a potent and selective competitive S1P1 antagonist with activity against experimental autoimmune encephalomyelitis. In the GTPγ35S assay, it has IC50 values ​​of 2.0 nM and 2.3 nM for human and rat S1P1, respectively.
Pack SizePriceAvailabilityQuantity
1 mg$35In Stock
5 mg$77In Stock
10 mg$113In Stock
25 mg$229In Stock
1 mL x 10 mM (in DMSO)$108In Stock
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Purity:98.87%
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Product Introduction

Bioactivity
Description
NIBR-0213 is a potent and selective competitive S1P1 antagonist with activity against experimental autoimmune encephalomyelitis. In the GTPγ35S assay, it has IC50 values ​​of 2.0 nM and 2.3 nM for human and rat S1P1, respectively.
Targets&IC50
S1P1:2.0 nM(GTPγ35S,human), S1P1:8.5 nM(GTPγ35S,mouse), S1P1:2.5 nM(Ca2+ mobilization), S1P1:2.3 nM(GTPγ35S,rat)
In vitro
In the Ca2+ assay, NIBR-0213 showed inhibitory activity against hS1P1 with an IC50 of 2.5 nM, but was inactive against S1P2, S1P3, and S1P4 (IC50 > 10 μM); in the GTPγ35S assay, NIBR-0213 showed potent and comparable potency against human and rat S1P1 (IC50 of 2.0 nM and 2.3 nM, respectively), while the IC50 for mouse S1P1 was slightly lower at 8.5 nM. [1]
In vivo
METHODS: NIBR-0213 (30, 100, 300 mg/kg, oral, once daily, for two weeks) was used to treat the rat adjuvant-induced arthritis (AiA) model to explore the functional/pathophysiological consequences of the disruption of S1P1-dependent vascular permeability homeostasis caused by its competitive antagonism.
RESULTS An effective oral dose of 30 mg/kg BID was tolerated without signs of dyspnea but induced dose-dependent acute vascular lung leak and pleural effusion, which completely resolved within 3-4 days; at a supramaximal oral dose of 300 mg/kg QD, NIBR-0213 impaired lung function (increased respiratory rate and decreased tidal volume) within the first 24 hours; NIBR-0213 at doses of 30, 100, and 300 mg/kg induced moderate lung changes after two weeks, characterized by alveolar wall thickening, macrophage accumulation, fibrosis, microhemorrhage, edema, and necrosis.[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 | Shipping with blue ice.
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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