glucocorticoid receptor

Glucocorticoid receptor agonist-1 is a potent glucocorticoid receptor agonist with an IC50 of 2.8 nM[1].

Glucocorticoid receptor agonist-2 Ala-Ala-Mal (compound 79) serves as a precursor for synthesizing anti-inflammatory antibody-drug conjugate (ADC) molecules and acts as an active reference for ABBV-3373 [1].

Glucocorticoid Receptor Agonist-1 Phosphate Gly-Glu (TFA) serves as a cleavable linker for the synthesis of Antibody-Drug Conjugates (ADCs).

Glucocorticoid receptor modulator 1 is a potent, orally active, non-steroidal selective glucocorticoid receptor modulator, exhibiting IC50 values of 9 nM and 130 nM against NF-κB and AP-1, respectively. It effectively reduces the expression of inflammatory factors such as IL-6, IL-1β, and TNF-α, and alleviates dermatitis in mice.

Glucocorticoid receptor agonist-2 (compound 21), a glucocorticoid receptor agonist exhibiting an IC50 value of 6.6 nM, serves as an active reference for ABBV-3373 [1]. This compound is instrumental in the synthesis of anti-inflammatory ADC molecules.

Glucocorticoid receptor agonist-1 Ala-Ala-Mal (compound 88), a glucocorticosteroid and glucocorticoid receptor agonist, can be conjugated with Adalimumab to formulate an ADC [1].

Glucocorticoid receptor-IN-1 is a selective regulator of the glucocorticoid receptor (GR) and exhibits anti-inflammatory activity. glucocorticoid receptor-IN-1 has good transcriptional repression, acting on hMMP1 ( IC50: 2.11 nM) and also has a transcriptional activating effect on MMTV (EC50: 5.59 nM).

Glucocorticoid Receptor Agonist-1 Phosphate (Gly-Glu-Br) is an antibody-drug conjugate (ADC) linker utilized in the synthesis of ABBV-154, ABBV-927, ABBV-368, and related analogs [1].

Glucocorticoid Receptor Agonist-1 Phosphate Ala-Ala-Mal functions as a glucocorticoid receptor agonist, utilized in the formulation of anti-CD40 antibody agent conjugates (ADC). It serves as a research tool for exploring inflammation and immune regulation [1].

Glucocorticoid receptor-IN-2 is a selective regulator of the glucocorticoid receptor (GR) and exhibits anti-inflammatory activity. IC50: 0.171 nM) and also has some transcriptional activating effect on MMTV (EC50: 0.94 nM).

Glucocorticoid Receptor Agonist-1 Phosphate Ala-Ala-Br is a drug-linker conjugate for antibody-drug conjugates (ADCs), serving as a reaction reagent in the creation of anti-CD40 antibody agent conjugates [1].

Glucocorticoid receptor agonist is an effective glucocorticoid receptor agonist.

EX-A5386 (Glucocorticoid receptor modulator-1) is a potent glucocorticoid receptor modulator, IC50/EC50<100nM.

Finerenone (BAY-948862) is a third-generation, selective, and orally available nonsteroidal mineralocorticoid receptor (MR) antagonist with IC50 of 18 nM for the treatment of chronic heart failure. Finerenone (BAY-948862) displays excellent selectivity versus glucocorticoid receptor (GR), androgen receptor (AR), and progesterone receptor (>500-fold).

Dexamethasone (Hexadecadrol) is a glucocorticoid receptor agonist and an IL receptor modulator. Dexamethasone has anti-inflammatory and immunosuppressive activity and induces autophagy. Dexamethasone inhibits LPS-induced inflammatory responses in macrophages.

Medroxyprogesterone Acetate (Farlutin) is a synthetic progestin that is derived from 17-hydroxyprogesterone. It is a long-acting contraceptive that is effective both orally or by intramuscular injection and has also been used to treat breast and endometrial neoplasms.

Cortodoxone (11-Desoxycortisol) is a glucocorticoid steroid hormone that is an intermediate in the biosynthesis of cortisol in the adrenal gland.

Ciclesonide (Alvesco)(RPR251526) is a glucocorticoid used for the treatment of obstructive airway diseases.

Cortisone (17-Hydroxy-11-dehydrocorticosterone) is a corticosteroid with potent glucocorticoid activity.

Triamcinolone acetonide (Azmacort) is a Corticosteroid. The mechanism of action of triamcinolone acetonide is as a Corticosteroid Hormone Receptor Agonist. It is an anti-inflammatory glucocorticoid used topically in the treatment of various skin disorders. Intralesional, intramuscular, and intra-articular injections are also administered under certain conditions.

Mifepristone (C-1073) is a Progestin Antagonist. The mechanism of action of mifepristone is as a Progestational Hormone Receptor Antagonist.

Corticosterone (Kendall's compound B) is an adrenocortical steroid with salocorticoid and glucocorticoid activity that is orally active. Corticosterone is involved in the regulation of energy, immune responses, and stress responses in the body.

Dexamethasone Phosphate disodium (EGP437. Dex-Phos) is a water-soluble form of the synthetic glucocorticoid dexamethasone.

Ulipristal acetate (CDB-2914) is an orally bioavailable, acetate salt of ulipristal, a selective progesterone receptor modulator with anti-progesterone activity. Ulipristal binds to the progesterone receptor (PR), thereby inhibiting PR-mediated gene expression, and interfering with progesterone activity in the reproductive system. As a result, this agent may suppress the growth of uterine leiomyomatosis. Furthermore, by inhibiting or delaying ovulation and effecting endometrial tissue, ulipristal can be used as an emergency contraception.

CORT-108297 Enantiomer is an enantiomer of CORT-108297 which is an antagonist of the Glucocorticoid Receptor.

OP-3633 is an effective and selective steroidal glucocorticoid receptor (GR) antagonist (IC50: 29 nM). OP-3633 shows low progesterone receptor (PR) agonism and androgen receptor (AR) antagonism. It also has an inhibition of GR transcriptional activity.

Geldanamycin, an HSP90 inhibitor (Kd: 1.2 μM), specifically disrupts glucocorticoid receptor (GR)/HSP association.

Flunisolide hemihydrate is a corticosteroid, an orally active Glucocorticoid receptor activator with anti-inflammatory effects. flunisolide hemihydrate induces apoptosis in eosinophils and can be used in asthma or rhinitis, inflammatory diseases. Can be used in studies related to asthma or rhinitis, inflammation.

Hydrocortisone (Cortisol) is a glucocorticoid hormone secreted by the adrenocortex. Hydrocortisone agonizes the glucocorticoid receptor, which promotes proteolytic metabolism, gluconeogenesis, capillary wall stabilization, and renal calcium excretion, as well as suppressing immune and inflammatory responses.

Amcinonide (CL-34699) is a Corticosteroid. The mechanism of action of amcinonide is as a Corticosteroid Hormone Receptor Agonist.

AL-438 is a non-steroidal selective glucocorticoid receptor modulator.

Rac-Finerenone, also known as (Rac)-BAY 94-8862, is the racemate derivative of Finerenone, a selective third-generation nonsteroidal mineralocorticoid receptor antagonist (MR) that is taken orally. With an IC50 value of 18 nM, Finerenone exhibits exceptional selectivity against the glucocorticoid receptor (GR), androgen receptor (AR), and progesterone receptor (>500-fold).

Cortisone Acetate is a synthetic or semisynthetic analog of the naturally occurring cortisone hormone produced by the adrenal glands with anti-inflammatory and immunomodulating properties. Cortisone acetate (NSC-49420) diffuses through the cell membrane and binds to nuclear glucocorticoid receptors. The receptor-ligand complex binds to promotor regions of certain genes and initiates RNA transcription. This results in an induction of synthesis of certain anti-inflammatory proteins while inhibiting the synthesis of certain inflammatory mediators.

BAY 1003803 is a glucocorticoid receptor agonist for the topical treatment of psoriasis or severe atopic dermatitis.

Norgestomet is a steroidal progestin of the 19-norprogesterone group used in veterinary medicine to control estrus and ovulation in cattle. In addition to the progesterone receptor, norgestomet possesses a weak (micromolar) affinity for the glucocorticoid

N-Demethyl Mifepristone (RU 42633), an active metabolite of Mifepristone, exhibits 61% of the affinity for the glucocorticoid receptor relative to Mifepristone's 100% [1].

Mirodenafil dihydrochloride is a PDE-5 inhibitor developed for the treatment of erectile dysfunction.

LEO 134310, a selective, non-steroidal glucocorticoid receptor (GR) agonist, is optimized for topical treatment. Demonstrating high affinity (EC50 of 14 nM) in GR binding assays, it is suitable for treating skin diseases.

ZK 216348 also binds to Progesterone and mineralocorticoid receptors (IC50s: 20.4 nM and 79.9 nM, respectively). ZK 216348 is a nonsteroidal selective glucocorticoid receptor agonist (IC50: 20.3 nM). ZK 216348 has an anti-inflammatory activity similar to

AZD2906, a selective glucocorticoid receptor (GR) agonist, demonstrates inhibitory concentrations (IC50s) of 2.2 nM in human GR, 0.3 nM in rat peripheral blood mononuclear cells (PBMC), 41.6 nM in human whole blood, and 7.5 nM in rat whole blood, respectively[1]. Additionally, it induces an increase in micronucleated immature erythrocytes within rat bone marrow.

Zavacorilant is capable of modulating glucocorticoid receptor (GR).

Diflorasone is a synthetic glucocorticoid with anti-inflammatory and immunosuppressive properties. Like other glucocorticoids, diflorasone enters the cell by diffusion across the cell membrane and binds to the glucocorticoid receptor (GR) in the cytoplasm

Betapar(Meprednisone (Betapar)) is a glucocorticoid and a methylated derivative of prednisone.

Braylin has anti-inflammatory, antinociceptive and immunomodulatory effects, which possibly act through the glucocorticoid receptor activation and by inhibition of the transcriptional activity of NF-κB. Braylin is also a phosphodiesterase-4 inhibitor, it could represent an ideal prototype of glucocorticoid receptor ligand, able to induce synergic immunomodulatory effects.

Mometasone furoate (Sch32088) is a pregnadienediol derivative ANTI-ALLERGIC AGENT and ANTI-INFLAMMATORY AGENT that is used in the management of ASTHMA and ALLERGIC RHINITIS. It is also used as a topical treatment for skin disorders.

Dexamethasone acetate (NSC 39471) is the acetate salt form of Dexamethasone, a synthetic adrenal corticosteroid with potent anti-inflammatory properties. In addition to binding to specific nuclear steroid receptors, dexamethasone also interferes with NF-kB activation and apoptotic pathways. This agent lacks the salt-retaining properties of other related adrenal hormones.

Prednisolone disodium phosphate, a synthetic glucocorticoid, has immunomodulating and anti-inflammatory properties.

Mirodenafil is a PDE-5 inhibitor developed for the treatment of erectile dysfunction.

GW-870086 is an effective anti-inflammatory agent. GW-870086 also plays a role in a glucocorticoid receptor agonist (pIC50: 10.1 in A549 cells expressing NF-κB).

Methylprednisolone succinate (Methylprednisolone hemisuccinate) is a synthetic glucocorticoid and is widely used as an anti-inflammatory agent.