(rel)-PRT062607 ((rel)-P505-15) is the relative configuration of PRT062607. PRT062607 is a highly selective inhibitor of Syk kinase, with an IC50 value of 1-2 nM, and is more than 80 times less potent against Fgr, Lyn, FAK, Pyk2, and Zap70.

(Rac)-GSK2973980A (Compound 215) is a DGAT1 inhibitor with an IC50 of 1.8 nM for hDGAT1. (Rac)-GSK2973980A can be used for research on obesity and obesity-related diseases.

(25R)-3Alpha,7alpha-dihydroxy-5beta-cholestanoyl-CoA is a coenzyme A derivative.

(1R,9S)-Dxd is an isomer of (Dxd). (1R,9S)-Dxd is an ADC payload that can be used in the synthesis of ADCs (antibody-drug conjugates).

Org 6582 is a competitive, selective, and long-acting 5-HT (Ki = 89 nM) uptake inhibitor. Org 6582’s inhibitory effect on 5-HT uptake can last for more than 48 hours. Org 6582 can be used for research on depressive disorders.

Ipratropium bromide (Atrovent, Sch 1000) monohydrate is an antagonist of muscarinic acetylcholine receptors (mAChR) with IC50 of 2.9 nM, 2.0 nM, and 1.7 nM for M1, M2, and M3 receptors, respectively.

Upacicalcet (sodium) is an intravenous calcimimetic agent. Upacicalcet suppresses excessive parathyroid hormone (PTH) secretion, thereby lowering blood PTH levels, by acting directly on parathyroid cell membrane calcium-sensing receptors. Upacicalcet can be used for researching the disease of secondary hyperparathyroidism (SHPT).

Clazosentan (Ro 61-1790) is a selective endothelin A (ETA) receptor antagonist. Clazosentan inhibits ET-1-mediated vasoconstriction. Clazosentan prevents cerebral vasospasm, vasospasm-related cerebral infarction.

MKP10241 is an orally active GPR119 agonist. MKP10241 elevates cAMP levels in the GPR119 expressing cell line (EC50: 3.7 nM). MKP10241 reduces blood glucose levels and HbA1c in acute models and a chronic diabetic mouse model. MKP10241 also demonstrates excellent preclinical efficacy in acute as well as chronic rodent models of obesity, and MASH.

Clozapine N-oxide is a major metabolite of Clozapine noted to decrease SR-2A (5-HT2 serotonin receptor) density in vitro.

T26A is a competitive prostaglandin transporter (PGT) inhibitor (Ki=378 nM). T26A is promising for research of prostaglandin signaling and inflammatory diseases (e.g., glaucoma, pulmonary hypertension) .

CCR7 inhibitor Cmp1205 is an allosteric ligand and antagonist for human CC chemokine receptor 7 (CCR7) with Kd of 3 nM, suppresses arrestin binding in response to activation by CCL19 with IC50 of 7.3 uM.Cmp1205 binds to a pocket at the intracellular part of CCR7 between the ends of TM1, TM2, TM3, and TM6 and the loop between TM7 and H8.Cmp1205 allosterically inhibits binding of the native chemokine CCL19 ligand in a membrane-based competition binding experiment with IC50 of 35 nM.

S26131 (compound 5) is a potent and selective MT1 melatoninergic ligand, and the Ki values are 0.5 and 112 nM for MT1 and MT2, respectively. S26131 behaves as an MT1 and MT2 antagonist.

Etrasimod (APD334) is a potent, selective and orally available antagonist of the sphingosine-1-phosphate-1(S1P1) receptor with an IC50 value of 1.88 nM in CHO cells.

RAP-103 is an orally active, stabilized pentapeptide analog of DAPTA (D-ala-peptide T-amide), and multi-chemokine receptor antagonist.

8-Hydroxy-DPAT hydrobromide (8-OH-DPAT hydrobromide) is a potent and selective 5-HT1A agonist with a pIC50 of 8.19. 8-Hydroxy-DPAT hydrobromide has selectivity of almost 1000 fold for a subtype of the 5-HT1 binding site.

Anamorelin(RC1291; ONO-7643) is a synthetic orally active ghrelin receptor agonist which is under development for the management of non-small lung cancer associated cachexia/anorexia.

α-MSH (11-13) acetate is the 11-13 amino acid (lysine-proline-valine) sequence of α-MSH, which reduces fever in rabbits.

MEN 10207 (acetate) is a selective antagonist of the NK-2 tachykinin receptor. MEN 10207 (acetate) induces tachykinin-induced contractions in rat bladder and guinea pig airways in vivo. MEN 10207 (acetate) inhibits [β-Ala 8 ]-NKA (4-10)-induced enhancement of bladder motility in anesthetized rats and [β-Ala 8 ]-NKA (4-10)-induced enhancement of bronchoconstriction in anesthetized guinea pigs.

XEN-2174 is a noradrenaline transporter (NET) inhibitor. XEN-2174 inhibits the reuptake of noradrenaline through non-competitive inhibition, increasing the concentration of noradrenaline in the synaptic cleft, thereby activating α2-adrenergic receptor at the spinal level and exerting analgesic effects. XEN-2174 exhibits long-lasting analgesic effects in models of neuropathic pain and postoperative pain in rats. XEN-2174 can be used in pain research.

BPR-890 is a potent agonist of CB1. BPR-890 exhibits excellent CB2/1 selectivity and has in vivo efficacy in diet-induced obese mouse model.

pro-FTY, a FTY720 anticancer prodrug, is a sphingosine-1-phosphate (S1P) inhibitor. pro-FTY specifically inhibits S1P signaling in cancer cells using a drug delivery system (DDS) that reacts with acrolein. pro-FTY significantly inhibits the survival of breast cancer cells, including multidrug-resistant cells and its organoids resistant to Paclitaxel or Doxorubicin. pro-FTY potently suppresses tumor growth in 4T1 cells or organoids xenograft tumors mice model while avoiding lymphocytopenia.

RU-24213 hydrochloride is a selective D-2 dopamine receptor agonist. RU-24213 hydrochloride is also a KAPPA-opioid receptor antagonist. RU-24213 hydrochloride induces stereotyped behaviors.

7-Hydroxy-DPAT (7-OH-DPAT) is a selective D3 dopamine receptor agonist. 7-Hydroxy-DPAT exhibits significant pharmacological activity in modulating locomotor behavior and dopamine metabolism within the brain. 7-Hydroxy-DPAT can be used for the research of neurological disease .

RK-851 is a highly selective and orally active δ-opioid receptor antagonist, with a negative logarithm of the antagonist concentration (pA2) of 8.84. TRK-851 exhibits the selectivity for the δ receptor of more than 100 times higher than that for the μ or κ receptors. TRK-851 exhibits a potent antitussive effect in a rat model of capsaicin-induced cough. TRK-851 can be used for research on antitussive effects.

Vilanterol (GW642444) acetate is a long-acting β2 adrenergic receptor agonist. Vilanterol acetate has pEC50 values for β2-AR, β1-AR, and β3-AR of 9.4, 6.4, and 6.1, respectively. Vilanterol acetate selectively activates airway β2 adrenergic receptors, increases cAMP and thus relaxes bronchial smooth muscle. Vilanterol acetate can be used in asthma research[1][2].

LM-189, a G protein alpha subunit I (Gαi)-biased agonist, is a Gαi-biased ligand of β2-adrenergic receptor (β2AR). LM-189 stabilizes a distinct conformation in TM6 and increases the dynamics of ICL2. LM-189 can be used to develop the Gαi-biased β2AR agonists.

LM-189 free base, a G protein alpha subunit I (Gαi)-biased agonist, is a Gαi-biased ligand of β2-adrenergic receptor (β2AR). LM-189 free base stabilizes a distinct conformation in TM6 and increases the dynamics of ICL2. LM-189 free base can be used to develop the Gαi-biased β2AR agonists.

CNV-dopamine is a photoreleasable D2 receptor-selective agonist. CNV-dopamine activates D2 receptors and induces G protein-coupled inwardly rectifying potassium (GIRK) currents. CNV-dopamine is promising for research of disorders like Parkinson’s disease and addiction.

5-Hydroxy-6-methoxy (S)-duloxetine maleate is an orally active and brain-penetrant serotonin (5-HT) and norepinephrine (NE) reuptake inhibitor with antidepressant and analgesic activities. 5-Hydroxy-6-methoxy (S)-duloxetine maleate is promising for research of psychiatric and neurological disorders such as depression, diabetic neuropathic pain, generalized anxiety disorder, and fibromyalgia.