2. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor Immunology/Inflammation
  3. ROR Interleukin Related
  4. BMS-986251

BMS-986251 is an orally active and selective RORγt inverse agonist with an EC50 of 12 nM for RORγt GAL4. BMS-986251 inhibits IL-17 with an EC50 of 24 nM in human whole blood assay. BMS-986251 demonstrates robust efficacy in mouse acanthosis and Imiquimod-induced (HY-B0180) models (preclinical models of psoriasis).

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

BMS-986251 Chemical Structure

BMS-986251 Chemical Structure

CAS No. : 2460133-35-9

Size Price Stock Quantity
1 mg USD 1040 Get quote 13 - 15 weeks 12 - 14 weeks
5 mg USD 2083 Get quote 13 - 15 weeks 12 - 14 weeks
10 mg USD 3325 Get quote 13 - 15 weeks 12 - 14 weeks
25 mg USD 6650 Get quote 13 - 15 weeks 12 - 14 weeks
50 mg USD 10325 Get quote 13 - 15 weeks 12 - 14 weeks
100 mg USD 15400 Get quote 13 - 15 weeks 12 - 14 weeks
200 mg   Get quote  
500 mg   Get quote  
Synthetic products have potential research and development risk.

* 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

BMS-986251 Related Antibodies

Top Publications Citing Use of Products

View All ROR Isoform Specific Products:

View All Isoforms
RORγ RORα RORβ

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

BMS-986251 is an orally active and selective RORγt inverse agonist with an EC50 of 12 nM for RORγt GAL4. BMS-986251 inhibits IL-17 with an EC50 of 24 nM in human whole blood assay. BMS-986251 demonstrates robust efficacy in mouse acanthosis and Imiquimod-induced (HY-B0180) models (preclinical models of psoriasis)[1].

IC50 & Target[1]

RORγt

12 nM (EC50)

IL-17

24 nM (EC50)

RORα

>10 μM (EC50)

RORβ

>10 μM (EC50)

In Vitro

BMS-986251 is against ROR family members (RORα GAL4: EC50>10 μM; RORβ GAL4: EC50>10 μM) and against other nuclear receptors (PXR: EC50>5 μM; LXRα: EC50>7.5 μM; LXRβ: EC50>7.5 μM). BMS-986251 does not inhibit any of the CYP’s[1].

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

BMS-986251 Related Antibodies
In Vivo

BMS-986251 (5-45 mg/kg; orally; twice daily until day 9) results in reduced ear thickness[1].
BMS-986251 (0.13, 0.79, 4.76 mg/kg; orally; once a day) displays a dose-dependent reduction of the IL-17F produced in naïve C57BL/6 female mice (7-9 weeks)[1].
BMS-986251 (2 mg/kg of IV and 4 mg/kg of PO) has a T1/2 of 7.7 hours, a CL of 2.7 mL/min•kg, and a Vss of 1.9 L/kg for IV in mouse[1].

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

Animal Model: C57BL/6 female mice with acanthosis[1]
Dosage: 5, 15, 45 mg/kg
Administration: Orally; twice daily until day 9
Result: Resulted in reduced ear thickness and significantly reduces imiquimod (IMQ)-induced skin thickening.
Animal Model: Mouse or rat[1]
Dosage: 2 mg/kg of IV and 4 mg/kg of PO (Pharmacokinetic Analysis)
Administration: IV or PO
Result: Had a T1/2 of 7.7 hours, a CL of 2.7 mL/min•kg, and a Vss of 1.9 L/kg for IV in mouse.
Had a Cmax of 4.8 μM and an AUC of 37 μM•h for PO in mouse.
Had a T1/2 of 11 hours, a CL of 1.3 mL/min•kg, and a Vss of 1.25 L/kg for IV in rat.
Had a Cmax of 4.7 μM and an AUC of 64 μM•h for PO in rat.
Clinical Trial
Molecular Weight

667.61

Formula

C30H29F8NO5S
CAS No.
SMILES

O=C([C@H]1C[C@H](C)[C@H](C(N2CC[C@@]3(S(=O)(C4=CC=C(F)C=C4)=O)C5=CC=C(C(C(F)(F)F)(F)C(F)(F)F)C=C5CC[C@@]23[H])=O)CC1)O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
  • 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.

BMS-986251 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
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:

BMS-9862512460133-35-9BMS986251BMS 986251RORInterleukin RelatedRAR-related orphan receptorILorallyacanthosisimiquimodpsoriasisPXRLXRαLXRβ?Inhibitorinhibitorinhibit

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:
BMS-986251
Cat. No.:
HY-136527
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.