RORγt inverse agonist 30

製品番号: HY-147533: Data Sheet 取扱説明書
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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.

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RORγt inverse agonist 30 構造式

CAS 番号 : 1445901-41-6

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RORγ RORα RORβ

生物活性
純度とドキュメンテーション
参考文献
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製品説明

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)

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]

体外実験

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.

体内実験

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.

分子量

441.59

分子式

C₂₄H₃₁N₃O₃S

CAS 番号

1445901-41-6

SMILES

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

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

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

純度とドキュメンテーション

取扱説明書 (2659 KB)

参考文献

[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]