AZD-7594 (AZ-13189620) is a potent, nonsteroidal, selective glucocorticoid receptor modulator (SGRM) with binding IC50 of 0.9 nM, shows no affinity for AR, PR, MR and ERα/β; demonstrates cell potentcy with IC50 of 55 nM (repression of AP-1 dependent transcription), inhibits LPS-stimulated TNF-α production in human PBMC with IC50 0.43 nM; potently inhibits lung edema in a rat model of allergic airway inflammation with inhaled EC50 of 130 uM/Kg.
Phase 2 Clinical
Mapracorat (ZK 245186) is a potent, selective and non-steroid glucocorticoid receptor (GR) agonist with binding Ki of 1.9 nM; does not show significant activity for ERα, PR, AR or MR; shows anti-inflammatory efficacy after topical application similar to the classical glucocorticoids, with a better safety profile.
Phase 1 Clinical
LLY-2707 (LLY 2707, LLY2707) is a novel potent, selective, nonsteroidal glucocorticoid receptor antagonist with Ki of 2.13 nM; shows substantially lower potency at the other steroid receptors (AR, MR and PR); suppress amphetamine-induced increases in locomotor activity, reduces atypical antipsychotic-associated weight gain in rats.
AZD-9567 monohydrate is a potent, selective, non-steroidal and orally available selective glucocorticoid receptor modulator (SGRM) for treatment of rheumatoid arthritis.
AZD-9567 (AZD9567) is a potent, selective, non-steroidal and orally available selective glucocorticoid receptor modulator (SGRM) for treatment of rheumatoid arthritis.
Loteprednol etabonate is an anti-inflammatory corticosteroid used in optometry and ophthalmology.
Cortisone acetate (Cortisone 21-acetate) is a synthetic glucocorticoid corticosteroid and corticosteroid ester; the C21 acetate ester of cortisone and acts as a prodrug of cortisone in the body.
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