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.

Compound 1, identified as a GPR61 inverse agonist, exhibits an IC50 of 11 nM, rendering it suitable for metabolism and body weight disorder research, including obesity and cachexia [1].

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

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

Nurr1 Inverse Agonist-1 is an inverse agonist for the neuroprotective transcription factor Nurr1, serving as a research tool.

RORγt inverse agonist 31 (14g) is a potent antagonist of the retinoic acid receptor-related orphan receptor γt (RORγt), exhibiting an inhibitory concentration (IC50) of 0.428 μM. It has demonstrated efficacy in mitigating Imiquimod-induced psoriasis severity in murine models [1].

RORγt inverse agonist 30 (Compound 1) is a potent RORγt inverse agonist (IC50: 46 nM). Targeting the nuclear receptor RORγt is effective in the treatment of autoimmune diseases.

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

CB1 Inverse Agonist 2, an orally active compound, serves as an inverse agonist for the Cannabinoid Receptor CB1. It effectively counteracts the hypothermia and anorexia induced by CP55940 in mouse models.

RORγt inverse agonist 28 is a potent RORγt inverse agonist. RORγt inverse agonist 28 regulates the differentiation of Th17 cells and inhibits the production of IL-17. RORγt inverse agonist 28 has shown research potential in inflammatory and autoimmune diseases.

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

RORγt inverse agonist 29 is a potent, selective, orally active RORγt inverse agonist with an IC50 value of 21 nM. RORγt inverse agonist 29 can be used in the study of autoimmune diseases such as skin inflammation and psoriasis.

ERRγ Inverse Agonist 1 (Compound 12) is a potent, selective and orally bioavailable Estrogen-related Receptor grammar (ERRγ) inverse agonist (IC 50=40 nM) [1].

RORγt Inverse agonist 10 is a highly potent and 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 the activity of RORγt, a prominent transcription factor involved in the regulation of genes associated with the pathogenesis of psoriasis, including IL-17A, IL-22, and IL-23R.

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 26, a potent reverse agonist of RORγt, effectively modulates Th17 cell differentiation and suppresses IL-17 production. This compound shows promising potential for researching inflammation and autoimmune diseases.

RORγt Inverse agonist 3 is a potent, selective and orally active inverse agonist of RORγ(EC50s of 0.22 μM and 0.15 μM for hRORγ and RORγt (human IL-17 cells), respectively).

RORγt inverse agonist 14 (8e) is a potent, selective, and orally active compound with an EC50 of 2.5 nM, exhibiting anti-inflammatory activity. It is employed in researching rheumatoid arthritis and psoriasis [1].

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

Pimavanserin tartrate (Nuplazid) is an effective and specific serotonin 5-HT2A inverse agonist (pIC50: 8.73), used in the therapy of psychosis associated with Parkinson's disease.

GSK805 is a potent, orally bioavailable retinoid-related orphan receptor gamma t (RORγt) inverse agonist that interacts with the receptor's putative ligand binding domain without exerting significant effects on DNA binding

Kaempferol (Robigenin) is a natural flavonoid and an inverse agonist of ERRα and ERRγ. Kaempferol has a wide range of antitumor, anti-inflammatory, antioxidant, antibacterial and antiviral activities.

Sarmazenil (Ro 15-3505) is a partial inverse agonist at the benzodiazepine receptor with pro-convulsant properties and is used in the study of chronic hepatic encephalopathy (HE).

Hemopressin (rat) acetate is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. Hemopressin is orally active, selective and inverse agonist of CB2 cannabinoid receptors. Hemopressin exerts antinocicep

S 38093 is a novel brain-penetrant antagonist/inverse agonist of H3 receptors.

LY-2624803 is a 5-HT2A receptor antagonist and histamine receptor inverse agonist that can be used to improve slow wave sleep.

FA16 is a selective, metabolically stable ferroptosis inducer with an IC50 value of 1.26 μM.FA16 is a derivative of 2-(trifluoromethyl)benzimidazole.FA16 inhibits the cystine/glutamate inverse transporter protein (system Xc-)-mediated exchange of intracellular glutamate for extracellular cystine.FA16 significantly inhibited tumor growth in a HepG2 xenograft tumor model. HepG2 xenograft tumor model significantly inhibited tumor growth.

Meclizine, also known as Meclozine, is a piperazine class H1 antagonist with antihistamine properties that inhibits the interaction of histamine at H1 receptors reversibly. It serves as an effective anti-motion sickness agent, able to cross the blood-brain barrier. Additionally, Meclizine acts as an agonist ligand for the mouse constitutive androstane receptor (CAR) and an inverse agonist for human CAR, making it useful in research on polyQ toxicity disorders, including Huntington's disease.

AC-90179 HCl (AC-90179 hydrochloride) is a selective inverse agonist of 5-HT2A receptor. AC-90179 HCl is an atypical antipsychotic pharmaceutical and has been shown to alleviate hallucinogen-induced vasocontriction.

[D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P acetate ([D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P acetate (96736-12-8 free base)) is a broad spectrum neuropeptide inverse agonist and antagonist. Potent full inverse agonist for the ghrelin receptor (EC50 = 5.2 nM); diminishes constitutive ghrelin receptor signaling. Also antagonist at tachykinin, bradykinin, CCK and bombesin receptors. Induces apoptosis and inhibits cancer cell growth in vitro.

Samelisant (SUVN-G3031) is a selective and inverse agonist of H3 receptor with Kis of 8.7 nM and 9.8 nM for human and rat. Samelisant has anticataplectic effects and can be used in studies about narcolepsy.

MK-0249 FA is an orally active, selective and potent histamine H3 inverse agonist for the study of attention deficit, hyperactivity disorder neurodivergent and cognitive disorders in adults.

Fezagepras (Setogepram) is an orally active GPR40 agonist and is an antagonist or inverse agonist of GPR84 with anti-inflammatory, anti-fibrotic, and anti-proliferative actions.

Hemopressin (human, mouse) acetate is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. Hemopressin is orally active, selective and inverse agonist of CB1 cannabinoid receptors. Hemopressin exerts an

(S)-2-((R)-3-(4-chlorophenyl)-N’-((4-chlorophenyl)sulfonyl)-4-phenyl-4,5-dihydro-1H-pyrazole-1-carboximidamido)-3-methylbutanamide is a cannabinoid receptor antagonist/inverse agonist.

DMCM hydrochloride is a non-selective fully inverse agonist of benzodiazepine. DMCM showed significant differences in human recombinant GABAA αxβ3γ2 receptor subtypes. For α1, α2, α3, and α5 receptors, their Kis were 10 nM, 13 nM, 7.5 nM, 2.2 nM, respectively.

Fezagepras sodium (Setogepram sodium salt) is an orally active GPR40 agonist and is an antagonist or inverse agonist for GPR84, with anti-fibrotic, anti-inflammatory and anti-proliferative actions.

Deramciclane has high affinity for 5-HT2A and 5-HT2C receptors. It acts as an antagonist in both receptor subtypes and has inverse agonist properties for 5-HT2C receptors, but no direct stimulant agonists.

XY101 is a selective, metabolically stable and orally available agonist of RORγ inverse(IC50 of 30 nM and a Kd of 380 nM).

AZD-0284 is an inverse agonist of the nuclear receptor RORγ. In development for the treatment of plaque psoriasis vulgaris and respiratory tract disorders[1].

BMS493 is an inverse agonist of the pan-retinoic acid receptor (RAR) that inhibits retinoic acid-induced differentiation, enhances the interaction of nuclear co-inhibitors with RARs, attenuates RA signaling, potentiates TPP-induced toxicity, and inhibits the increase in phospholipase A2 activity.

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

SR9243, an LXR inverse agonist, can induce LXR-corepressor interaction; shows anticancer activity and selectively targets the lipogenesis and Warburg effect.

Rimonabant (SR141716) is an inverse agonist for the cannabinoid receptor CB1. It is an anorectic anti-obesity drug produced and marketed by Sanofi-Aventis. Its main avenue of effect is a reduction in appetite. Rimonabant is the first selective CB1 receptor blocker to be approved for use anywhere in the world. Rimonabant is approved in 38 countries including the E.U., Mexico, and Brazil. It was rejected for approval for use in the United States.

Hemopressin(rat) is a bioactive endogenous peptide substrate for endopeptidase 24.15, neurolysin and ACE. Ki values are 27.76, 3.43 and 1.87 μM respectively.

11-cisRetinol is an isomer of vitamin A . It is formed from vitamin A,viaatrans-retinyl ester intermediate, by the enzyme RPE65 in the retinal pigment epithelium and then converted to 11-cis retinal as part of the visual cycle.1,211-cisRetinol is an agonist of salamander and human red rod opsins expressed in COS cells and an inverse agonist of salamander red cone opsin, as well as human red and green cone opsins expressed in COS cells.3It promotes pigment formation in cone, but not rod, photoreceptors. 1.Rando, R.R.The biochemistry of the visual cycleChem. Rev.101(7)1881-1896(2001) 2.Guignard, T.J.P., Jin, M., Pequignot, M.O., et al.FATP1 inhibits 11-cis retinol formation via interaction with the visual cycle retinoid isomerase RPE65 and lecithin: Retinol acyltransferaseJ. Biol. Chem.285(24)18759-18768(2010) 3.Ala-Laurila, P., Cornwall, M.C., Crouch, R.K., et al.The action of 11-cis-retinol on cone opsins and intact cone photoreceptorsJ. Biol. Chem.284(24)16492-16500(2009)

H4 Receptor antagonist 1 is a potent and selective histamine H4 receptor inverse agonist, with an IC50 of 19 nM.

Basmisanil (RG1662) is a negative allosteric modulator/inverse agonist of GABAAα5 receptors.Formulations containing basmisanil are in clinical trials for the treatment of cognitive impairments associated with Down syndrome.

Agouti-related Protein (AGRP) (83-132) Amide (human) is a segment derived from the agouti-related protein (AGRP), abundantly present in the hypothalamus' arcuate nucleus. It predominantly functions as an inverse agonist for the melanocortin-4 receptor (MC4R), thereby promoting food intake [1] [2].

Hemopressin(human, mouse) is a bioactive endogenous peptide substrate for endopeptidase, neurolysin and ACE. Ki values are 27.76, 3.43 and 1.87 μM respectively.