Glucocorticoid Receptor Modulator

Avicin D is a plant triterpenoid. Avicin D induces Autophagy by activation of AMPK. Avicin D inhibits mTOR and S6 kinase activity. Avicin D selectively induces Apoptosis and downregulates p-STAT-3, bcl-2, and Survivin. Avicin D has properties of being a selective Glucocorticoid receptor modulator. Avicin D inhibits NF-κB activation. Avicin D shows anti-tumor effects against cutaneous T-cell lymphomas.

Mirodenafil-d₇ (SK3530-d₇) is the deuterium labeled Mirodenafil (HY-14930). Mirodenafil (SK3530) is an orally active, potent, reversible, and selective?phosphodiesterase?5 (PDE5)?inhibitor. Mirodenafil is a?glucocorticoid receptor?(GR)?modulator Mirodenafil activates the?Wnt/β-catenin?signaling pathway by downregulating Dkk1 expression. Mirodenafil can be used for the research of erectile dysfunction (ED), Alzheimer’s disease (AD) and systemic sclerosis (SSc).

Mirodenafil (SK3530) dihydrochloride is an orally active, potent, reversible, and selective phosphodiesterase 5 (PDE5) inhibitor. Mirodenafil dihydrochloride is a glucocorticoid receptor (GR) modulator Mirodenafil dihydrochloride activates the Wnt/β-catenin signaling pathway by downregulating Dkk1 expression. Mirodenafil dihydrochloride can be used for the research of erectile dysfunction (ED), Alzheimer’s disease (AD) and systemic sclerosis (SSc).

Desisobutyryl-ciclesonide is the active metabolite of Ciclesonide. Desisobutyryl-ciclesonide has affinity for the glucocorticoid receptor.

Betamethasone dipropionate is a glucocorticoid steroid with anti-inflammatory and immunosuppressive abilities.

Mizacorat (AZD9567; compound 15) is a potent, oral active, non-steroidal and selective glucocorticoid receptor modulator (SGRM), with an IC₅₀ of 3.8 nM. Exhibits excellent efficacy in the streptococcal cell wall (SCW) reactivation model of joint inflammation.

AZD7594 is a potent selective nonsteroidal glucocorticoid receptor modulator, with an IC₅₀ of 0.9 nM.

AZD5423 is an inhaled, potent, selective, and non-steroidal glucocorticoid receptor (GR) modulator (SGRM). AZD5423 effectively reduces allergen-induced responses in subjects with mild allergic asthma.

Mirodenafil (SK3530) is an orally active, potent, reversible, and selective phosphodiesterase 5 (PDE5) inhibitor. Mirodenafil is a glucocorticoid receptor (GR) modulator Mirodenafil activates the Wnt/β-catenin signaling pathway by downregulating Dkk1 expression. Mirodenafil can be used for the research of erectile dysfunction (ED), Alzheimer’s disease (AD) and systemic sclerosis (SSc).

Dazucorilant (CORT113176) is a selective and high affinity non-steroidal glucocorticoid receptor (GR) modulator with a K_i value ＜1 nM in vitro. Dazucorilant can be used for the research of neurological disorders.

Glucocorticoid receptor modulator 1 is a highly potent and orally active non-steroidal selective glucocorticoid receptor modulator with an IC₅₀ value of 9 nM and 130 nM for NF-κB and AP-1, respectively. Glucocorticoid receptor modulator 1 can effectively reduce the expression of inflammatory factors IL-6, IL-1β, TNF-α, also can relieve dermatitis in mice.

C108297 is a selective glucocorticoid receptor (GR) modulator (GR binding K_i 0.7 nM; GR reporter gene functional K_i 0.6 nM). C108297 attenuates obesity by reducing caloric intake and increasing lipolysis and fat oxidation, and in addition attenuates inflammation.

HP210 is a selective glucocorticoid receptor modulator (SGRM). HP210 can inhibit the mRNA expression of IL-1β and IL-6. HP210 has the potential to study inflammation-related diseases.

Prednisolone tebutate is a synthetic glucocorticoid used as an antiinflammatory and immunosuppressant.

Amebucort is a synthetic glucocorticoid corticosteroid, may used for the research of inflammatory disorders.

Betamethasone dipropionate-d₅ (Betamethasone 17,21-dipropionate-d₅) is deuterium-labeled Betamethasone dipropionate (HY-13571).

Zavacorilant is capable of modulating glucocorticoid receptor (GR).

S-HP210 is a potent and selective glucocorticoid receptor (GR) with an IC₅₀ value of 1.92 μM for NF-κB transrepression (TR). S-HP210 represses the LPS-induced transcription of a variety of proinflammatory genes such as IL-1β, IL-6 and COX-2. S-HP210 is nontoxic at effective doses against mouse fibroblasts 3T3 cells.

Betamethasone dipropionate-d₁₀ is the deuterium labeled Betamethasone dipropionate. Betamethasone dipropionate is a glucocorticoid steroid with anti-inflammatory and immunosuppressive abilities.

Glucocorticoid receptor modulator 2 (Example 1) is a glucocorticoid receptor modulator, with an IC₅₀ value less than 100 nM. Glucocorticoid receptor modulator 2 can be used for research of inflammatory and immune diseases.