2. GPCR/G Protein
  3. LPL Receptor
  4. NIBR0213

NIBR-0213 is a potent, orally active and selective S1P1 antagonist with efficacy in experimental autoimmune encephalomyelitis. 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.

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NIBR0213 Chemical Structure

NIBR0213 Chemical Structure

CAS No. : 1233332-14-3

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Based on 1 publication(s) in Google Scholar

NIBR0213 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

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Description

NIBR-0213 is a potent, orally active and selective S1P1 antagonist with efficacy in experimental autoimmune encephalomyelitis. 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[1].

Cellular Effect
Cell Line Type Value Description References
CHO IC50
> 10 μM
Compound: 38, NIBR-0213
Antagonist activity at human S1P5 receptor expressed in CHO cells after 120 mins by [35S]GTPgammaS binding assay
Antagonist activity at human S1P5 receptor expressed in CHO cells after 120 mins by [35S]GTPgammaS binding assay
[PMID: 24125884]
CHO IC50
> 10 μM
Compound: 38, NIBR-0213
Antagonist activity at human S1P4 receptor expressed in CHO cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 20 mins by Fluo-4/FLIPR method
Antagonist activity at human S1P4 receptor expressed in CHO cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 20 mins by Fluo-4/FLIPR method
[PMID: 24125884]
CHO IC50
> 10 μM
Compound: 38, NIBR-0213
Antagonist activity at human S1P3 receptor expressed in CHO cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 20 mins by Fluo-4/FLIPR method
Antagonist activity at human S1P3 receptor expressed in CHO cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 20 mins by Fluo-4/FLIPR method
[PMID: 24125884]
CHO IC50
> 10 μM
Compound: 38, NIBR-0213
Antagonist activity at human S1P2 receptor expressed in CHO cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 20 mins by Fluo-4/FLIPR method
Antagonist activity at human S1P2 receptor expressed in CHO cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 20 mins by Fluo-4/FLIPR method
[PMID: 24125884]
CHO IC50
2 nM
Compound: 38, NIBR-0213
Antagonist activity at human S1P1 receptor expressed in CHO cells after 120 mins by [35S]GTPgammaS binding assay
Antagonist activity at human S1P1 receptor expressed in CHO cells after 120 mins by [35S]GTPgammaS binding assay
[PMID: 24125884]
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[1].
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[1].
NIBR-0213 shows an about 3,000-fold selectivity against human S1P5 in the GTPγ35S assay[1].
NIBR-0213 is a competitive S1P1 antagonist with a calculated Kd of 0.37±0.031 nM[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

NIBR0213 Related Antibodies
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[1].
NIBR-0213 (30 mg/kg and 60 mg/kg) is efficacious when given therapeutically in a mouse experimental autoimmune encephalomyelitis (EAE) model[1].
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[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Lewis or Wistar rats (220-250 g, males)[1]
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[1]
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.
Molecular Weight

464.98

Formula

C27H29ClN2O3
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

ClC1=CC=C([C@@H](C)NC2=CC=CC(C3=CC(C)=C(C(N[C@@H](C)C(O)=O)=O)C(C)=C3)=C2)C=C1C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (268.83 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Ethanol : ≥ 25 mg/mL (53.77 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1506 mL 10.7532 mL 21.5063 mL
5 mM 0.4301 mL 2.1506 mL 4.3013 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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g

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.38%

SDS (252 KB)

COA (245 KB) HNMR (269 KB) LCMS (90 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
Ethanol / DMSO 1 mM 2.1506 mL 10.7532 mL 21.5063 mL 53.7658 mL
5 mM 0.4301 mL 2.1506 mL 4.3013 mL 10.7532 mL
10 mM 0.2151 mL 1.0753 mL 2.1506 mL 5.3766 mL
15 mM 0.1434 mL 0.7169 mL 1.4338 mL 3.5844 mL
20 mM 0.1075 mL 0.5377 mL 1.0753 mL 2.6883 mL
25 mM 0.0860 mL 0.4301 mL 0.8603 mL 2.1506 mL
30 mM 0.0717 mL 0.3584 mL 0.7169 mL 1.7922 mL
40 mM 0.0538 mL 0.2688 mL 0.5377 mL 1.3441 mL
50 mM 0.0430 mL 0.2151 mL 0.4301 mL 1.0753 mL
DMSO 60 mM 0.0358 mL 0.1792 mL 0.3584 mL 0.8961 mL
80 mM 0.0269 mL 0.1344 mL 0.2688 mL 0.6721 mL
100 mM 0.0215 mL 0.1075 mL 0.2151 mL 0.5377 mL
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NIBR0213 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

NIBR02131233332-14-3NIBR 0213NIBR-0213LPL ReceptorLysophospholipid ReceptorS1P1autoimmuneencephalomyelitisInhibitorinhibitorinhibit

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