1. Metabolic Enzyme/Protease
  2. ROR
  3. RORγt Inverse agonist 8

RORγt Inverse agonist 8 

Cat. No.: HY-122737
Handling Instructions

RORγt Inverse agonist 8 is a potent, selective, orally bioavailable RORγt inverse agonist, with an IC50 of 19 nM for human RORγt-LBD.

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

RORγt Inverse agonist 8 Chemical Structure

RORγt Inverse agonist 8 Chemical Structure

CAS No. : 2079892-79-6

Size Stock
100 mg Get quote
250 mg Get quote
500 mg Get quote

* Please select Quantity before adding items.

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

RORγt Inverse agonist 8 is a potent, selective, orally bioavailable RORγt inverse agonist, with an IC50 of 19 nM for human RORγt-LBD[1].

IC50 & Target

IC50: 19 nM (RORγt)[1]

In Vitro

RORγt Inverse agonist 8 (Cpd 1) is a potent RORγt inhibitor and binds to the ligand binding domain (LBD) of RORγt[1].
RORγt Inverse agonist 8 (0-10μM ;24 hours) results in complete attenuation of IL-17A secretion in a concentration-dependent manner with an IC50 of 60 nM in HUT78 cells[1].
RORγt Inverse agonist 8 selectively suppresses human Th17 and Tc17 cell differentiation[1].
RORγt Inverse agonist 8 polarizes Th17 cells also blocks IL-17A production in a concentration-dependent manner with an IC50 of 92 nM[1].
RORγt Inverse agonist 8 reduces Th17 cell-associated mRNA expression including IL17A, IL17F, IL26, IL23R and CCR6 in a concentration-dependent fashion[1].
RORγt Inverse agonist 8 alters epigenetic regulation at the IL17A and IL23R gene promoters without impairing the DNA binding activity of RORγt[1].

In Vivo

RORγt Inverse agonist 8 (15 mg/kg, 45 mg/kg ; i.g.; twice daily; for 7 days) ameliorates antigen-induced arthritis (AiA) responses in Lewis rats[1].

Animal Model: Female Lewis rats (190–220 g)[1]
Dosage: 15 mg/kg, 45 mg/kg
Administration: Oral gavage; twice daily; for 7 days
Result: Ameliorates antigen-induced arthritis (AiA) responses in Lewis rats.
Molecular Weight

475.59

Formula

C₂₆H₃₃N₇O₂

CAS No.

2079892-79-6

SMILES

O=C(C1=CN=C(C)N=C1)NC2=CN3C(C(CN4C[[email protected]H](C)N(C(C5CCCC5)=O)CC4)=C2C)=NC=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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.
  • 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

Keywords:

RORγt Inverse agonist 8RORγt Inverse agonist8RORγt Inverse agonist-8RORRAR-related orphan receptorRORγtinverseagonistInhibitorinhibitorinhibit

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 *

Country or Region *

 

Requested quantity *

Remarks

Bulk Inquiry

Inquiry Information

Product name:
RORγt Inverse agonist 8
Cat. No.:
HY-122737
Quantity:
MCE Japan Authorized Agent: