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

Chemical Structure : Tegacorat

Tegacorat (GRM-01, GRM01)

Catalog No.: 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.

Packing	Price	Stock	Quantity
25 mg		Get quote
50 mg		Get quote
100 mg		Get quote

Get Quotation Now

* Please select Quantity before adding items.

or Bulk Inquiry

Bulk size, bulk discount!

E-mail: sales@probechem.com

Tech Support: tech@probechem.com

Biological Activity

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.

Physicochemical Properties

M.Wt	475.49
Formula	C22H20F3N5O2S
Appearance	Solid
CAS No.
Storage	Solide Powder -20°C 12 Months; 4°C 6 Months	In Solvent -80°C 6 Months; -20°C 6 Months
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

References

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

Tegacorat (GRM-01, GRM01)

Biological Activity

Physicochemical Properties

References

Bulk Inquiry

* Indicates a Required FieldYour information is safe with us.

Get Quote

* Indicates a Required FieldYour information is safe with us.