Seltorexant hydrochloride (JNJ-42847922 hydrochloride) is an orally active, high-affinity, and selective OX2R antagonist (pKi values of 8.0 and 8.1 for human and rat OX2R). Seltorexant hydrochloride crosses the blood-brain barrier and quickly occupies OX2R binding sites in the rat brain.

Montelukast is a potent, selective and orally active antagonist of cysteinyl leukotriene receptor 1 (CysLT1). Montelukast can be used for the reseach of asthma and liver injury. Montelukast also has an antioxidant effect in intestinal ischemia-reperfusion injury, and could reduce cardiac damage.

Zafirlukast(Accolate)

alpha-NETA (α-NETA) is a small molecule antagonist of chemerin receptor chemokine-like receptor 1 (CMKLR1), inhibits chemerin-stimulated β-arrestin2 association with CMKLR1 with IC50 of 4.9 uM.

LY-3502970 (Orforglipron) is a potent, selective, orally active non-peptide agonist of glucagon-like peptide-1 (GLP-1) receptor.LY3502970 is a partial agonist, biased toward G protein activation over β-arrestin recruitment at the GLP-1R.

(R)-YNT-3708 is a potent, selective orexin 1 receptor (OX1R) agonist with EC50 of 7.48 nM and Emax 101%, 22-fold selectivity over OX2R (IC50=168 nM).

TRV045 is a selective Sphingosine-1-phosphate subtype 1 receptor agonist with no effect on lymphocyte transport. TRV045 has antiepileptic activity.

KRO-105714 is the antagonist for sphingosine phosphocholine receptor (SPC Receptor) and sphingosine-1-phosphate receptor 1 (S1P1 Receptor) (IC50=79.2 nM). KRO-105714 inhibits SPC-induced proliferation of NIH3T3 (IC50=5.6 nM), inhibits SPC-induced cell migration (IC50=0.59 μM) and tube formation in HUVECs. KRO-105714 inhibits SPC-induced generation of IL-4 and IL-5, exhibits anti-inflammtory efficacy in mouse atopic dermatitis models.

(Rac)-1-Oleoyl lysophosphatidic acid is an isomer of 1-Oleoyl lysophosphatidic acid sodium.

Elsovaptan is the antagonist for vasopressin receptor that can be used in researchs of Alzheimer disease.

DM-4111, one of the major monohydroxyl metabolites of Tolvaptan. Obeticholic acid is a potent, selective and orally active FXR agonist.

A-49816 is an orally active diuretic that increases urine volume and sodium and chloride excretion. A-49816 at high doses (12.5, 15, and 20 mg) caused significant salt and chloride excretion and diuresis in experimental animals.

(R)-(+)-Tolvaptan ((R)-(+)-OPC-41061) is the (R)-(+) enantiomer of Tolvaptan.

ZH8965 is an orally active TAAR1-Gs/Gq agonist (EC50: 6.1/14.8 nM). ZH8965 improves antipsychotic-like phenotypes and cognitive impairment in the MK-801-induced mouse psychosis model. ZH8965 can be used in schizophrenia research.

N-Methylphenethylamine (NMPEA) hydrochloride is a potent TAAR1 agonist. N-Methylphenethylamine hydrochloride also is a trace amine neuromodulator.

MMC(TMZ)-TOC TFA has high binding affinity and selectivity for somatostatin receptor subtype-2 (SSTR2). MMC(TMZ)-TOC TFA targets delivery of TMZ to SSTR2-positive tumor cells. MMC(TMZ)-TOC TFA can be used for the research of cancer.

SSTR4 agonist-1 (Compound 47) is a selective agonist for somatostatin receptor subtype 4 (SSTR4) with an EC50 of 4.7 nM. SSTR4 agonist-1 reveals a half-life > 130 minutes in human liver microsomes.

L-796778 acetate is a selective agonist of the sst3 receptor. In CHO-K1 cells expressing the hsst3 receptor, L-796778 acetate is a partial agonist that inhibits Forskolin

BN-81674 is a somatostatin analogue and a selective antagonist of the non-peptide human somatostatin sst3 receptor (Ki=0.92 nM). In addition, BN-81674 reversed the inhibition of cyclic AMP accumulation induced by 1 nM somatostatin through the sst3 receptor with an IC50 value of 0.84 nM. BN-81674 can be used in cancer research.

SW43 is a Sigma-2 selective ligand and agonist. SW43 is an ideal molecule for the development of cancer-targeted drug compounds. SW43 conjugated with DOX-L-NETA (89Y) exhibits antitumor activity in a VX2 cancer liver tumor allograft rabbit model. SW 43 conjugated with SW IV-52s to form SW III-123 activates the NF-κB pathway, has potent cytotoxicity against ovarian cancer cell lines, and induces apoptosis.

Opipramol (Ensidon) is an atypical tricyclic antidepressant (TCA). Opipramol acts primarily as a sigma (σ) receptor agonist and can potently interact with sigma recognition sites with a Ki value of 50 nM. Opipramol can be used for the research of generalized anxiety disorder (GAD).

Igmesine hydrochloride (JO 1784) is an orally active σ-receptor ligand capable of blocking the increase in colonic electromechanical activity induced by emotional stress. Igmesine hydrochloride also eliminates the colonic motility stimulation induced by dopamine, as well as the stimulation induced by centrally injected D1 or D2 receptor agonists. Furthermore, Igmesine hydrochloride can block the colonic motility responses induced by corticotropin-releasing factor (CRF) and ES through central cholecystokinin (CCK) release and/or activation of supraspinal CCK pathways.

CM699 is a potent Dopamine Transporter (DAT) and Sigma-receptor (σR) dual inhibitor with IC50s of 311 and 14.1 nM, respectively.

CM304 is a potent S1R inhibitor that can inhibit drug-induced convulsions in rats.

AD353 is a selective sigma-1 receptor ligand with antiallodynic activity. AD353 exhibits high potency both in a model of Capsaicin. Silodosin is a potent, selective and orally active α1A-adrenergic receptor (α1A-AR) blocker.

U-46619 serinol amide is a derivative of U-46619. U-46619 serinol amide is a stable analog of Thromboxane A2 (TXA2). U-46619 serinol amide is a potent TXA2 agonist that can induce platelet shape change and aggregation.

U-44069 serinol amide is a derivative of U-44069. U-44069 serinol amide is a stable analog of the endoperoxide prostaglandin H2. U-44069 serinol amide is a vasoconstrictor that can induce preglomerular Ca2+ influx.

tetranor-Prostaglandin E1 is metabolite of Prostaglandin E1 and Prostaglandin E2 that is formed by β-oxidation.

tetranor-PGFM is the major urinary metabolite of Dinoprost, acts as an inhibitor of DNA primase ATP and GTP polymerization activities, with IC50 values of 35 µM and 28 µM for the human enzyme, respectively. Purine riboside-5'-O-triphosphate sodium inhibits calmodulin-dependent protein kinase II (CaMKII) with a Ki value of 590 µM.

Taprostene sodium is a partial agonist at prostanoid prostacyclin (IP) receptors. Taprostene sodium interacts additively with Prostaglandin E2 (PGE2).