inverse

CB1 inverse agonist 1 (MRL-650) is an orally active and selective CB1 agonist. The IC50s for CB1 and CB2 are 7.5 nM and 4100 nM, respectively. CB1 inverse agonist 1 shows anorexigenic effects.

ERRγ Inverse Agonist 1 (Compound 12) is a potent, selective, and orally bioavailable estrogen-related receptor gamma (ERRγ) inverse agonist with an IC50 of 40 nM [1].

RORγt Inverse Agonist 3 is a potent, selective, and orally active inverse agonist of RORγ with EC50 values of 0.22 μM for hRORγ and 0.15 μM for RORγt (human IL-17 cells), respectively.

RORγt Inverse agonist 6 is an agonist of RORγt inverse. RORγt Inverse agonist 6 can be used in research on Th17-driven autoimmune diseases.

RORγt Inverse agonist 8 is a potent, selective, orally bioavailable RORγt inverse agonist (human RORγt-LBD) with an IC50 of 19 nM.

RORγt Inverse agonist 2 is a selective, orally active inverse agonist of RORγt, with an EC50 of 119 nM.

RORγt inverse agonist 23, an orally available novel retinoic acid receptor-related orphan receptor γt inverse agonist, is a potent and selective RORγt inverse agonist.

RORγt Inverse agonist 10 is a highly potent, orally bioavailable compound that acts as an antagonist for the retinoic acid receptor-related orphan nuclear receptor gamma t (RORγt). With an IC50 of 51 nM, it effectively inhibits RORγt activity, a key transcription factor regulating genes linked to psoriasis pathogenesis, including [IL-17A], [IL-22], and [IL-23R].

RORγt inverse agonist 13 (Compound 3i) is a potent, orally active, and selective inverse agonist for RORγt with an IC50 of 63.8 nM, exhibiting improved drug-like properties[1].

SB 258719 is a selective antagonist of 5-HT7 receptor(pKi of 7.5).

Cimetidine (SKF-92334) is a histamine congener, it competitively inhibits HISTAMINE binding to HISTAMINE H2 RECEPTORS. Cimetidine has a range of pharmacological actions. It inhibits GASTRIC ACID secretion, as well as PEPSIN and GASTRIN output.

GSK2981278 (ROR gama modulator 1) is a highly potent and selective inverse agonist of retinoic acid receptor-related orphan receptor gamma (ROR gamma).

Clobenpropit dihydrobromide is a potent antagonist and inverse agonist of histamine H3R (histamine H3LR,pEC50 of 8.07)

ML179 is a potent and selective inverse agonist of liver receptor homolog-1 (LRH1, NR5A2) with IC50 of 320 nM.

Cedirogant (ABBV-157) is an orally active, retinoid-related orphan receptor-γt (RORγt) inverse agonist used in psoriasis studies.

FG 7142 (LSU-65) also modulates GABA-induced chloride flux at GABAA receptors expressing the α1 subunit (EC50= 137 nM). FG 7142 can increase tyrosine hydroxylation and cause upregulation of β-adrenoceptors in mouse cerebral cortex. FG 7142 , a non-selectively benzodiazepine inverse agonist, has high affinity for the α1 subunit-containing GABAA receptor (Ki=91 nM).

RORγ inverse agonist 1 has anti-inflammatory activity and can be used to treat rheumatism and psoriasis.

RORγt inverse agonist 32 (compound b14) exhibits oral activity and can be utilized in inflammatory research studies.

5-HT6 inverse agonist 1 (Compound 33) is an antagonist of the 5-HT6 receptor with a Ki of 23 nM and a Kb of 6.62 nM. This compound can inhibit 5-HT6R-mediated Cdk5 and mTOR signaling pathways and reduce tactile allodynia induced by spinal nerve ligation (SNL) in rat models.

RORγt inverse agonist 34 (compound 5a) is an inverse agonist for RORγt, exhibiting an IC50 of 0.094 μM for the inhibition of RORγt-LBD. This compound is utilized in psoriasis research.

RORγt inverse agonist 33 (compound (R)-D4) is an orally bioavailable RORγt inverse agonist with an IC50 of 21 nM, playing a significant role in rheumatoid arthritis research.

RORγt inverse agonist 35 (Compound 22) is an RORγt inverse agonist with an IC50 of 1.51 μM. It significantly inhibits Th17 differentiation and pro-inflammatory characteristics in human CD4+ T cells. This compound can be utilized for research on Th17-driven autoimmune diseases, such as psoriasis, multiple sclerosis, and inflammatory bowel disease (IBD).

RORγinverse agonist 2 (Compound 15) is a potent inverse agonist of the retinoic acid receptor-related orphan receptor RORγ, with IC50 values of 0.4 μM for Gal4-RORγ and 0.9 μM for full-length RORγ. This compound is useful for researching autoimmune diseases.

GPR183 inverse agonist-1 (Compound 78) is an inverse agonist of GPR183. It inhibits GPR183-mediated Gi activation and β-arrestin2 recruitment while blocking PBMC migration. This compound is utilized in research concerning inflammation, autoimmune, and cancer-related diseases.