HL-43 (EP4 antagonist HL-43) is a selective prostaglandin E receptor 4 (EP4) antagonist, promotes chondrocyte differentiation/cartilage regeneration and anabolism with low toxicity; HL-43 exhibits the highest potency in inducing Col2a1 expression and reducing Mmp3 expression in presence of IL-1β. HL-43 downregulats Mmp3/13 expression in a dose-dependent manner. HL-43 induces anabolic factors (ACAN and SOX9), and suppresses catabolic factor (MMP13), and hypertrophic marker (COLX), inhibits the STAT3 catabolic pathway;. HL-43 promotes chondrocyte differentiation and ECM generation, and inhibits matrix degradation in both human and mouse articular cartilage explants. HL-43 enhances cartilage repair and regeneration in different artilage defect (CD) animal models.

Tavapadon is a potent, orally-bioavailable, selective partial agonist of the dopamine D1 and D5 receptors.

TUG-469 is a selective free fatty acid receptor 1 (FFA1/GPR40) agonist with an EC50 value of 19 nM. TUG-469 is >200-fold selective for FFA1 over FFA4. TUG-469 significantly improves glucose tolerance in pre-diabetic mice. TUG-469 can be used for the research of diabetes.

MR120 (CCR6 antagonist 1b) is a potent, selective CCR6 antagonist, disrupts the CCL20-induced chemotaxis of CCR6+CD4+ T cells.

SB699551 is a potent, selective 5-HT5A receptor antagonist with pKi of 8.3, >100-fold selectivity over 5-HT1B/D, 5-HT2A, 5-HT2C, 5-HT1A and 5-HT7 receptors. SB699551 also is a novel PSMD4/Rpn10 inhibitor, decreases cell viability in MM cell lines.

J-2156 TFA is a high potent, selective somatostatin receptor type 4 (SST4 receptor) agonist with IC50s of 0.05 nM and 0.07 nM for human and rat SST4 receptors, respectively. J-2156 TFA is used for the relief of mechanical allodynia and mechanical hyperalg

VU0238441 is a pan muscarinic acetylcholine receptor (mAChR) positive allosteric modulator (PAM) with EC50s of 3.2 μM, 2.8 μM, 2.2 μM, 2.1 μM, >10 μM for M1, M2, M3, M5 and M4, respectively.

Pregnenolone-d4-1 (3β-Hydroxy-5-pregnen-20-one-d4-1) is the deuterium labeled Pregnenolone. Pregnenolone (3β-Hydroxy-5-pregnen-20-one) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone can protect the brain from cannabis intoxication. Pregnenolone is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels.

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.

RS 67333 hydrochloride is a potent and selective 5-HT4 receptor (5-HT4R) partial agonist with a pKi of 8.7 in guinea-pig striatum. RS 67333 hydrochloride exhibits lower affinities at several other receptors including 5-HT1A, 5-HT1D, 5-HT2A, 5-HT2C, dopamine D1, D2 and muscarinic M1-M3 receptors. RS 67333 hydrochloride has neuroprotective effects, and can be used for Alzheimer's disease research.

corticotropin releasing factor (CRF) antagonist.

Sufugolix(TAK-013) is a non-peptide, orally-active, selective antagonist of the gonadotropin-releasing hormone receptor (GnRHR) (IC50 = 0.1 and 0.06 nM for affinity and in vitro inhibition, respectively).

AT-56 is a selective, competitive, and highly bioavailable inhibitor of lipocalin-type prostaglandin D synthase (L-PGDS) with a Ki value of 75 µM.

​​JNJ-5207787​​ represents a breakthrough in neuropeptide Y receptor modulation as a brain-penetrant, selective Y2 receptor antagonist.

ATI-2341, pepducin targeting the C-X-C chemokine receptor type 4 (CXCR4), is an allosteric agonist activating the inhibitory heterotrimeric G protein (Gi) to promote inhibition of cAMP production and induce calcium mobilization.

MK-571 is a selective, orally active CysLT1 receptor antagonist.

BL5923 (BL-5923) is a potent, highly specific, orally available inhibitor of CCR1 with IC50 of 20.4 and 22.8 nM for human and mouse CCR1, resepctively.

GSK682753A is a selective and highly potent inverse agonist of the epstein-barr virus-induced receptor 2 (EBI2) with an IC50 of 53.6 nM.

Setmelanotide (RM-493, BIM-22493, CAM 4072) is a cyclic peptide full agonist of melanocortin-4 receptor (MC4R) with an EC50 of 0.27 nM and a Ki of 2.1 nM.

NPS-2143(SB 262470A ) is a selective potent calcium ion-sensing receptor antagonist with IC50 of 43 and 41 nM for cytoplasmic Ca2+ concentrations and parathyroid hormone secretion, respectively.

SHA 68 is a potent and selective non-peptide neuropeptide S receptor (NPSR) antagonist with IC50s of 22.0 and 23.8 nM for NPSR Asn107 and NPSR Ile107, respectively. SHA 68 has limited the blood-brain barrier (BBB) penetration and the activity in neuralgia.

KARI-201 is a multifunctional small molecule that demonstrates dual activity as a highly selective inhibitor of acid sphingomyelinase (ASM) and an agonist of the ghrelin receptor. It operates as a competitive inhibitor by binding directly to the active site of ASM. Studies reveal that the incorporation of KARI-201 into ASM decreases in a concentration-dependent manner with sphingomyelin, resulting in KM values of 332.5, 433.9, and 572.6 μM at KARI-201 concentrations of 1, 10, and 100 μM, respectively. In preclinical models, KARI-201 has shown efficacy in reducing amyloid pathology and reversing cognitive deficits in APP/PS1 mice. Additionally, it enhances autophagy degradation by promoting lysosomal biogenesis in neuronal cells. As a ghrelin receptor agonist, KARI-201 also supports hippocampal neurogenesis and improves synaptic plasticity, making it a promising therapeutic candidate for neurodegenerative conditions.

Ogremorphin (OGM, OGM8345) represents a pioneering small-molecule inhibitor that selectively targets GPR68, demonstrating high specificity with an IC50 value of 0.71 µM. As a first-in-class compound, it offers unique therapeutic potential by precisely modulating GPR68 activity.

RTI-7470-44 is a highly potent and selective antagonist of the human trace amine-associated receptor 1 (hTAAR1), demonstrating an IC50 of 8.4 nM in an in vitro cAMP functional assay. In radioligand binding studies, it exhibits a Ki value of 0.3 nM, highlighting its strong affinity for hTAAR1. Notably, RTI-7470-44 shows significant species selectivity, with over 90-fold preference for hTAAR1 compared to its rat and mouse counterparts. This compound also possesses favorable pharmacokinetic properties, including good blood-brain barrier penetration, moderate metabolic stability, and a promising off-target safety profile. In electrophysiological studies, RTI-7470-44 enhanced the spontaneous firing rate of dopaminergic neurons in the mouse ventral tegmental area (VTA) and effectively counteracted the effects of the TAAR1 agonist RO5166017.

Indacaterol is a potent, orally administered ultra-long-acting β2 adrenergic receptor (ADRB2) agonist, widely recognized for its therapeutic potential in respiratory and cardiovascular conditions. By selectively activating ADRB2, indacaterol not only enhances bronchodilation but also exhibits a unique mechanism of action by inhibiting NF-κB activity in a β-arrestin2-dependent manner. This dual functionality helps mitigate lung inflammation, prevent further pulmonary damage, and improve lung function in patients with chronic obstructive pulmonary disease (COPD). Beyond its respiratory applications, indacaterol has also emerged as a valuable tool in cardiovascular disease research, offering insights into its broader therapeutic effects. Its multifaceted pharmacological profile positions indacaterol as a promising candidate for addressing complex disease mechanisms and advancing treatment strategies in both respiratory and cardiovascular fields.

FSLLRY-NH2 is a protease-activated receptor 2 (PAR2) inhibitor.

Eucatropine is a synthetic anticholinergic agent that acts as a potent inhibitor of muscarinic acetylcholine receptors (mAChRs). These receptors are part of the parasympathetic nervous system and play a key role in mediating the effects of acetylcholine, a neurotransmitter involved in various physiological processes such as smooth muscle contraction, glandular secretion, and heart rate regulation.

Tirzepatide (LY3298176, GIP/GLP-1 RA, TZP) is a dual GIP/GLP-1 receptor agonist. Tirzepatide differentially induces internalization of the GIP and GLP-1 receptors with EC50 values of 18.2 nM and 18.1 nM, respectively.

Carbetocin (marketed under brand names such as Lonactene and Duratocin) is a synthetic analogue of oxytocin, specifically designed for use in obstetrics to prevent and manage postpartum hemorrhage (PPH), a leading cause of maternal mortality worldwide. It is a long-acting agonist of peripheral oxytocin receptors, making it highly effective in inducing uterine contractions and reducing bleeding after childbirth.

A peptide hormone and neuropeptide that is released into the bloodstream as a hormone in response to stretching of the cervix and uterus during labor and with stimulation of the nipples from breastfeeding.