Alclometasone (7a-Chloro-16a-methyl prednisolone) is a glucocorticoid and inhibits the release of pro-inflammatory mediators from leukocytes. Alclometasone can be used to relieve corticosteroid-responsive dermatoses, including atopic dermatitis, eczema, psoriasis and allergic dermatitis[1].
Betamethasone-d5-1 is deuterium labeled Betamethasone. Betamethasone is a synthetic glucocorticoid with anti-inflammatory and immunosuppressive activities. Betamethasone accelerates fetal lung maturation and induces gene expression and apoptosis[1][2][3][4].
Methylprednisolone succinate is a synthetic glucocorticoid and widely used as an anti-inflammatory agent.
Dexamethasone acetate is a glucocorticoid receptor agonist.
Vamorolone (VBP15) is a first-in-class, orally active dissociative steroidal anti-inflammatory drug and membrane-stabilizer. Vamorolone improves muscular dystrophy without side effects. Vamorolone shows potent NF-κB inhibition and substantially reduces hormonal effects[1][2].
Triamcinolone acetonide-d6 is deuterium labeled Triamcinolone acetonide.
AZD9567 (compound 15) is a potent, selective and oral active non-steroidal 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[1].
Dagrocorat (PF-00251802) hydrochloride is an orally active and selective high-affinity partial agonist of the glucocorticoid receptor. Dagrocorat hydrochloride is also a time-dependent reversible inhibitor of CYP3A (IC50=1.3 μM in human liver microsomes) and CYP2D6 (Ki=0.57 μM in human liver microsomes). Dagrocorat hydrochloride can be used for the research of rheumatoid arthritis[1].
Deflazacort is a glucocorticoid used as an anti-inflammatory and immunosuppressant.Target: Glucocorticoid ReceptorDeflazacort is an inactive prodrug which is converted rapidly to the active metabolite 21-desacetyldeflazacort. Maximum concentrations of 21-desacetyldeflazacort averaged 116 ng/ml and were observed after 1.3 h. The average area under the curve was 280 ng/ml.h, and the terminal half-life was 1.3 h. 21-Desacetyldeflazacort was cleared significantly faster than both methylprednisolone and prednisolone [1]. Two of 40 boys treated with deflazacort died at 13 and 18 years of age from cardiac failure. The treated boys were significantly shorter, did not have excessive weight gain and 22 of 40 had asymptomatic cataracts. Deflazacort has a very significant impact on health, quality of life and health care costs for boys with DMD and their families, and is associated with few side effects [2].
Flunisolide hemihydrate is a corticosteroid, which is an orally active glucocorticoid receptor activator with anti-inflammatory activity. Flunisolide hemihydrate can induce eosinophil apoptosis, and is used for the research of asthma or rhinitis, and inflammation[1][2].
Fluocinonide (Vanos) is a potent glucocorticoid steroid used topically as anti-inflammatory agent for the treatment of skin disorders.Target: Glucocorticoid ReceptorFluocinonide is a potent glucocorticoid steroid used topically as an anti-inflammatory agent for the treatment of skin disorders such as eczema and seborrhoeic dermatitis. Fluocinonide ranks as a "high-potency" topical corticosteroid. Minimal amounts should be used for a minimal length of time to avoid the occurrence of adverse effects. Fluocinonide should not be used if infection is present. Fluocinonide is used in veterinary medicine. It is a treatment for allergies in dogs. Natural systemic cortisol concentrations can be suppressed for weeks after one week of topical exposure. From Wikipedia.
Dexamethasone phosphate disodium is a glucocorticoid receptor agonist.
Glucocorticoids receptor agonist 2 is a potent anti-inflammatory, arylpyrazole-based glucocorticoid receptor agonist that does not impair insulin secretion.
Hydrocortisone hemisuccinate (Hydrocortisone 21-hemisuccinate), a physiological glucocorticoid, and is an orally active steroidal anti-inflammatory drug (SAID). Hydrocortisone hemisuccinate inhibits proinflammatory cytokine activity, with IC50s of 6.7 and 21.4 μM for IL-6 and IL-3, respectively. Hydrocortisone hemisuccinate can be used for the research of ulcerative colitis (UC)[1][2][3].
Mometasone furoate, prodrug of the free form mometasone, is a agent with high affinity for the glucocorticoid receptor.IC50 value: Target: glucocorticosteroid receptorMometasone furoate is used in the treatment of inflammatory skin disorders (such as eczema and psoriasis), allergic rhinitis (such as hay fever), asthma [1]. MF is approved for once or bid maintenance treatment of asthma (in patients previously receiving ICS or bronchodilators). Low systemic bioavailability and high relative binding affinity for the glucocorticoid receptor are properties of MF that allow for a favourable efficacy and tolerability profile. Inhaled MF has been shown to be an effective and well-tolerated controller medication for those patients with mild, moderate or severe persistent asthma [2].
Mifepristone is a progesterone receptor (PR) and glucocorticoid receptor (GR) antagonist with IC50s of 0.2 nM and 2.6 nM in in vitro assay.
Dagrocorat (PF-00251802) is a novel and dissociated glucocorticoid receptor agonist.
Fluticasone propionate is a high affinity, selective GR (glucocorticoid receptor) agonist which is derived from fluticasone used to treat asthma and allergic rhinitis.Target: Glucocorticoid ReceptorFluticasone propionate is a corticosteroid derived from fluticasone used to treat asthma and allergic rhinitis. It is also used to treat eosinophilic esophagitis. Fluticasone propionate is a synthetic trifluorinated glucocorticoid. It is highly lipophilic (logp octanol/water 3.69). In studies the topical drug has been associated with burning, stinging, skin irritation, blisters, dryness, skin infection, infected eczema, viral warts,impetigo, atopic dermatitis, pruritus, exacerbation of pruritus, exacerbation of eczema, erythema, and folliculitis.There are also numerous side effects associated with the oral version of this medication including headache, stuffy or runny nose, difficulty speaking, sore or irritated throat and painful white patches in the mouth or throat. Candidiasis of mouth and throat is reported as a "very common" side effect indicating that it occurs with a frequency greater than 1 in 10.Hoarseness is "common" indicating a frequency from 1 in 10 to 1 in 100. In both instances rinsing the mouth with water immediately after inhalation is recommended.
Beclometasone dipropionate monohydrate, the prodrug of Beclometasone, is an orally active and potent glucocorticoid recepter agonist. Beclometasone dipropionate monohydrate acts via a glucocorticoid receptor and suppresses inflammation and hyperproliferation. Beclometasone dipropionate monohydrate can be used for asthma [1][2].
OP-3633 is a potent and selective steroidal glucocorticoid receptor (GR) antagonist with an IC50 of 29 nM, with inhibition of GR transcriptional activity. OP-3633 exhibits low progesterone receptor (PR) agonism and androgen receptor (AR) antagonism[1].
Glucocorticoid receptor agonist-2 (compound 21) is an Glucocorticoid Receptor agonist with an IC50 value of 6.6 nM. Glucocorticoid receptor agonist-2 can be used to synthesize anti-inflammatory ADC molecules. Glucocorticoid receptor agonist-2 is an active reference of ABBV-3373[1].
Glucocorticoids receptor agonist 1 is a potent anti-inflammatory, arylpyrazole-based glucocorticoid receptor agonist that does not impair insulin secretion.
Relacorilant is a potent, selective and orally bioavailable glucocorticoid receptor antagonist, with a Ki of 7.2 nM in HepG2 TAT assay, and also shows Kis of 12, 81.2, 210 nM for rat, human and monkey glucocorticoid receptor in cell-based assay, respectively; Relacorilant has entered phase 2 clinical study in patients with Cushing’s syndrome.
Nenocorilant (Relacorilant) is a potent, orally activity glucocorticoid receptor (GR) antagonist with Ki value of 0.15 nM. Nenocorilant has pro-apoptotic effects and improves potency combined with cytotoxic agent. Nenocorilant can be used for cancer research[1][2][3].
AL 082D06 is a selective, nonsteroidal glucocorticoid receptor (GR) antagonist with Ki of 210 nM.
Fluticasone furoate is a topical, intranasal, enhanced-affinity synthetic trifluorinated corticosteroid with a Kd of 0.3 nM. Fluticasone furoate has potent anti-inflamatory and anti-asthmatic activity, and low systemic exposure. Fluticasone furoate has the potential for allergic rhinitis treatment[1][2].
Methylprednisolone aceponate (ZK 91588) is a glucocorticoid and anti-inflammatory agent with weak systemic effects. Methylprednisolone aceponate is a selective glucocorticoid receptor Ligand.Methylprednisolone aceponate can be used for research of eczema and other inflammatory skin disorders[1][2][3].
(S)-Mapracorat is a selective and less active glucocorticoid receptor agonist.
Glucocorticoid receptor agonist-1 Ala-Ala-Mal (compound 88) is a glucocorticosteroid, and an agonist of glucocorticoid receptor. Glucocorticoid receptor agonist-1 Ala-Ala-Mal can be conjugated with Adalimumab (HY-P9908) to prepare an ADC[1].
Prednisolone disodium phosphate is a synthetic glucocorticoid with anti-inflammatory and immunomodulating properties.Target: Glucocorticoid ReceptorPrednisolone irreversibly binds with glucocorticoid receptors (GR) alpha and beta for which they have a high affinity. Prednisolone can activate and influence biochemical behaviour of most cells. The steroid/receptor complexes dimerise and interact with cellular DNA in the nucleus, binding to steroid-response elements and modifying gene transcription. They induce synthesis of some proteins, and inhibit synthesis of others. Prednisolone exerted a delayed biphasic effect on the resistant CCRF-CEM leukemic cell line, necrotic at low doses and apoptotic at higher doses. At low doses, prednisolone exerted a pre-dominant mitogenic effect despite its induction on total cell death, while at higher doses, prednisolone's mitogenic and cell death effects were counterbalanced [1, 2].