Tegacorat (GRM-01) | GR agonist | Probechem Biochemicals

Chemical Structure : Tegacorat

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Tegacorat (GRM-01, GRM01)

货号: PC-25100Not For Human Use, Lab Use Only.

Tegacorat (GR modulator-01, GRM-01) is a potent, selective selective glucocorticoid receptor (GR) agonist and modulator (SEGRAM) with Ki/IC50 of 12/24 nM respectively.

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生物&药学活性

Tegacorat (GR modulator-01, GRM-01) is a potent, selective selective glucocorticoid receptor (GR) agonist and modulator (SEGRAM) with Ki/IC50 of 12/24 nM respectively.

GRM-01 shows little to no low affinity for Progesterone receptor (PR) and very low affinity for Mineralocorticoid receptor (MR).

GRM-01 produces transactivation at the GR receptor with EC50 of 60.2 nM in in vitro functional reporter gene assays, does not produce detectable transactivation of either the PR or the MR up to 10 uM.

GRM-01 inhibits LPS-induced TNF-α release with IC50 of 79 nM in an ex vivo rat whole blood assay.

exhibits complete inhibition of the LPS-induced IFN-γ release of 97.2% ± 4.0% and an IC50 of 238 nM in human whole blood ex vivo assays.

GRM-01 strongly inhibites IL-1β–induced release of IL-6 from immortalized A549 cells by 93% ± 3.8% with an IC50 of 6.1 nM.

GRM-01 partially inhibits the TNF-α–induced release of IL-6 from primary FLS cells by 62.8% ± 8.8% with an IC50 of 19.1 nM.

GRM-01 inhibits osteoprotegerin (OPG) release in the immortalized human osteoblast cell line MG-63 in a concentration dependent manner.

GRM-01 (0.3 and 1 mg/kg) displayed anti-inflammatory effects in the rat SCW model.

GRM-01 (0.01-1 mg/kg) produced dose-dependent reductions in plasma corticosterone levels in the rat SCW model with ED50 of 0.094 mg/kg.

物理化学性质&存储条件

分子量	475.49
分子式	C22H20F3N5O2S
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	6,7-difluoro-8-(6-fluoro-1-(methylsulfonyl)-1H-indol-4-yl)-1,4,4,9-tetramethyl-4,5-dihydro-[1,2,4]triazolo[4,3-a]quinoxaline

参考文献

1. Patent WO2020016452 A1. 2. Florian Jakob, et al. Front Pharmacol. 2025 Mar 5:16:1542351.

Tegacorat (GRM-01, GRM01)

生物&药学活性

物理化学性质&存储条件

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Tegacorat (GRM-01, GRM01)

生物&药学活性

物理化学性质&存储条件

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