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Cat. No.: HY-147533

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RORγt inverse agonist 30

RORγt inverse agonist 30 (Compound 1) is a potent RORγt inverse agonist with the IC₅₀ of 46 nM. Targeting the nuclear receptor RORγt is effective in autoimmune disorders.

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

CAS No.: 1445901-41-6
Formula: C₂₄H₃₁N₃O₃S
Molecular Weight:441.59

Storage:

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

Data Sheet (267 KB)

RORγt inverse agonist 30 Chemical Structure

CAS No.: 1445901-41-6

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

RORγt inverse agonist 30 (Compound 1) is a potent RORγt inverse agonist with the IC₅₀ of 46 nM. Targeting the nuclear receptor RORγt is effective in autoimmune disorders^[1].

IC₅₀ & Target^[1]

RORγt

46 nM (IC₅₀)

All ROR Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
HEK-293T	EC₅₀	>10 μM Compound: 17	Agonist activity at GAL4-fused human FXR expressed in HEK293T cells assessed as activation of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay Agonist activity at GAL4-fused human FXR expressed in HEK293T cells assessed as activation of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay	[PMID: 25017032]
HEK-293T	EC₅₀	>10 μM Compound: 17	Agonist activity at GAL4-fused human LXRalpha expressed in HEK293T cells assessed as activation of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay Agonist activity at GAL4-fused human LXRalpha expressed in HEK293T cells assessed as activation of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay	[PMID: 25017032]
HEK-293T	EC₅₀	>10 μM Compound: 17	Agonist activity at GAL4-fused human LXRbeta expressed in HEK293T cells assessed as activation of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay Agonist activity at GAL4-fused human LXRbeta expressed in HEK293T cells assessed as activation of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay	[PMID: 25017032]
HEK-293T	EC₅₀	>10 μM Compound: 17	Agonist activity at GAL4-fused human PXR expressed in HEK293T cells assessed as activation of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay Agonist activity at GAL4-fused human PXR expressed in HEK293T cells assessed as activation of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay	[PMID: 25017032]
HEK-293T	EC₅₀	>10 μM Compound: 17	Agonist activity at GAL4-fused human RORb expressed in HEK293T cells assessed as suppression of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay Agonist activity at GAL4-fused human RORb expressed in HEK293T cells assessed as suppression of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay	[PMID: 25017032]
HEK-293T	EC₅₀	>10 μM Compound: 17	Inverse agonist activity at GAL4-fused human RORa expressed in HEK293T cells assessed as suppression of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay Inverse agonist activity at GAL4-fused human RORa expressed in HEK293T cells assessed as suppression of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay	[PMID: 25017032]
HEK-293T	EC₅₀	0.13 μM Compound: 17	Agonist activity at GAL4-fused human RORc expressed in HEK293T cells assessed as suppression of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay Agonist activity at GAL4-fused human RORc expressed in HEK293T cells assessed as suppression of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay	[PMID: 25017032]
PBMC	EC₅₀	>10 μM Compound: 17	Cytotoxicity against human PBMC after 48 hrs by CellTiter-Glo assay Cytotoxicity against human PBMC after 48 hrs by CellTiter-Glo assay	[PMID: 25017032]
PBMC	EC₅₀	>10 μM Compound: 17	Inhibition of IFNgamma production in human PBMC after 48 hrs by Sandwich ELISA Inhibition of IFNgamma production in human PBMC after 48 hrs by Sandwich ELISA	[PMID: 25017032]
PBMC	EC₅₀	0.8 μM Compound: 17	Antiinflammatory activity in human PBMC assessed as inhibition of IL-17 production after 48 hrs by Sandwich ELISA Antiinflammatory activity in human PBMC assessed as inhibition of IL-17 production after 48 hrs by Sandwich ELISA	[PMID: 25017032]

In Vitro

RORγt inverse agonist 30 (compound 1) inhibits mouse Th17 cell differentiation with an IC₅₀ of 0.67 μM^[1].

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

In Vivo

RORγt inverse agonist 30 exhibits favorable pharmacokinetics profiles with T_1/2 of 2.3 min, CL_int of 612 μL/min/mg and CL_int(liver) of 2423.5 mL/min/kg^[1].

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

Chemical Information

CAS No. 1445901-41-6
Molecular Weight 441.59
Formula C₂₄H₃₁N₃O₃S
SMILES

CC(N1CCN(CC1)C2=CC=C(C=C2)CN(S(=O)(CC3=CC=CC=C3)=O)C4CCC4)=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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (267 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Nannan Sun, et al. Discovery of novel N-sulfonamide-tetrahydroquinolines as potent retinoic acid receptor-related orphan receptor γt inverse agonists for the treatment of autoimmune diseases. Eur J Med Chem. 2020 Feb 1;187:111984. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References

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RORγt inverse agonist 30

All ROR Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

RORγt inverse agonist 30 Related Classifications

HY-147533 Related Classifications