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.

For research use only. We do not sell to patients.

NIBR0213 Chemical Structure

NIBR0213 Chemical Structure

CAS No. : 1233332-14-3

Size Price Stock Quantity
1 mg USD 45 In-stock
5 mg USD 110 In-stock
10 mg USD 180 In-stock
50 mg   Get quote  
100 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

NIBR0213 Related Antibodies

Top Publications Citing Use of Products

View All LPL Receptor Isoform Specific Products:

View All Isoforms
LPAR1 LPAR2 LPAR3 LPAR5 S1PR1 S1PR2 S1PR3 S1PR4 S1PR5

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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].

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)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

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%

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
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

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

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Salutation

Applicant Name *

 

Email Address *

Phone Number *

 

Organization Name *

Department *

 

Requested quantity *

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
NIBR0213
Cat. No.:
HY-18166
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

Request for HNMR Report

We have received your request and will respond to you as soon as possible.