QCC374 is a selective agonist of IP[1].
Rilmenidine, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine is an alpha 2-adrenoceptor agonist. Rilmenidine induces autophagy. Rilmenidine modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells[1][2][3].
Dexamethasone phosphate (Dexamethasone 21-phosphate) is a biologically inactive compound which undergoes dephosphorylation by intra-erythrocyte enzymes. The active metabolite, dexamethasone, is then released into the circulation by simple passive diffusion through cell membranes. Dexamethasone phosphate-encapsulated erythrocyte has the potential for steroid-dependent ulcerative colitis research[1].
GR 113808 is a potent and highly selective 5-HT4 receptor antagonist (pKb= 8.8). GR 113808 shows 300-fold selectivity over 5-HT1A, 5-HT1B, 5-HT2A, 5-HT2C and 5-HT3 receptors[1].
SEP-363856 （SEP-856）, an orally active and CNS active psychotropic agent with a unique, non-D2/5-HT2A mechanism of action, exerts its antipsychotic-like effects. SEP-363856 （SEP-856） has the potential for the treatment of schizophrenia[1].
Terrein is a melanogenesis inhibitor[1]. Terrein induces apoptosis in breast cancer cell lines [2]. Terrein is an inhibitor of quorum sensing and c-di-GMP in Pseudomonas aeruginosa[3].
Naloxonazine is a potent and selective opiate mu-1 antagonist that can also affect leishmania by regulating host coding function[1].
SB225002 is a potent and selective CXCR2 antagonist with an IC50 of 22 nM.
Hemokinin 1, human is a selective tachykinin neurokinin 1 (NK1) receptor full agonist. Hemokinin 1, human is a full agonist at NK2 and NK3 receptor. Hemokinin 1, human can produces an opioid-independent analgesia[1][2].
L-DOPA-13C is the 13C labeled L-DOPA[1]. L-DOPA (Levodopa) is an orally active metabolic precursor of neurotransmitters dopamine. L-DOPA can cross the blood-brain barrier and is converted into dopamine in the brain. L-DOPA has anti-allodynic effects and the potential for Parkinson's disease[2][3][4].
[D-Trp8]-γ-MSH is a potent and selective agonist of melanocortin 3 (MC3) receptor, with IC50s of 6.7 nM, 600 nM and 340 nM for hMC3, hMC4 and hMC5, respectively in CHO cells. [D-Trp8]-γ-MSH could provide protection against multiple inflammatory disorders such as rheumatoid arthritis and colitis[1][2].
5-HT2A&5-HT2C agonist-1 (Example 2) is a 5-HT2A & 5-HT2C agonist, with IC50s of 196 nM and 0.9 nM respectively. 5-HT2A&5-HT2C agonist-1 can be used for research of depression, alcoholism, tobacco and cocaine addiction, inflammation, cluster headache, PTSD, seizure disorders and other CNS disorders[1].
CB1R Allosteric modulator 2 (compound 18) is a potent CB1R allosteric modulator. CB1R Allosteric modulator 2 shows negatively affects the functional activity of orthosteric ligands (NAM) at CB1Rs[1].
Treprostinil (UT-15C) diethanolamine is a potent EP2, DP1 and IP agonist with Ki values of 3.6, 4.4, 32.1, 212, 826, 2505 and 4680 nM for EP2, DP1, IP, EP1, EP4, EP3 and FP, respectively. Treprostinil (UT-15C) diethanolamine increases upregulation of cAMP toward maintaining homeostasis within the vasculature. Treprostinil (UT-15C) diethanolamine can result in vasodilatation of human pulmonary arteries[1][2][3].
SKF83959 hydrobromide is a potent and selective dopamine D1-like receptor partial agonist. SKF83959 hydrobromide Ki values for rat D1, D5, D2 and D3 receptors are 1.18, 7.56, 920 and 399 nM, respectively. SKF83959 hydrobromide is a potent allosteric modulator of sigma (σ)-1 receptor. SKF83959 hydrobromide belongs to benzazepine family and has improvements on cognitive dysfunction. SKF83959 hydrobromide can be used for the research of Alzheimer's disease and depression[1][2][3][4].
RP101442, an active metabolite of Ozanimod, is a selective, potent S1PR1 (sphingosine-1-phosphate receptor 1) agonist, with EC50s of 2.6 nM and 171 nM for S1PR1 and S1PR5, respectively[1].
(S)-(+)-Dimethindene maleate, an enantiomer, is a potent M2-selective muscarinic receptor antagonist (pA2 = 7.86/7.74; pKi = 7.78). (S)-(+)-Dimethindene maleate shows lower affinities for the muscarinic M1 (pA2 = 6.83/6.36; pKi = 7.08), the M3 (pA2 = 6.92/6.96; pKi = 6.70) and the M4 receptors (pKi = 7.00), respectively. (S)-(+)-Dimethindene maleate also is a histamine H1 receptor antagonist (pA2 = 7.8)[1].
Cosalane (NSC 658586) is a potent inhibitor of HIV replication. Cosalane has an intrinsic ability to block human and murine CCR7 function in vitro in response to both of its natural ligands, CCL19 and CCL21, with the IC50 of 0.207/2.66 μM in human for CCL19/CCL21 and 0.193/1.98 μM in murine, respectively[1][2].
SUN B8155, a non-peptide agonist of calcitonin (CT) receptor, selectively mimics the biological actions of calcitonin. Calcitonin, a 32-amino acid peptide hormone secreted mainly from the thyroid gland, plays an important role in maintaining bone homeostasis[1].
PROTAC K-Ras Degrader-1 (Compound 518) is potent K-Ras degrader based PROTAC, exhibits ≥70% degradation efficacy in SW1573 cells[1].
Fasitibant chloride (MEN16132 free base) is a potent and selective nonpeptide bradykinin B2 receptor (B2R) antagonist. Fasitibant chloride reduces joint pain and diminishes joint oedema in Carrageenan-induced arthritis rat model[1][2][3].
Pramipexole-d5 is the deuterium labeled Pramipexole[1]. Pramipexole is a selective and blood-brain barrier (BBB) penetrant dopamine D2-type receptor agonist, with Kis of 2.2 nM, 3.9 nM, 0.5 nM and 1.3 nM for D2-type receptor, D2, D3 and D4 receptors, respectively. Pramipexole can be used for the research of Parkinson's disease (PD) and restless legs syndrome (RLS)[2][3][4].
NPC-567 is a bradykinin B2 receptor antagonist. NPC-567 is effective in inhibiting the acute response to allergen in the airways[1][2].
Scopolamine N-oxide hydrobromide is an antagonist of the muscarinic acetylcholine.
Oxprenolol (Ba 39089 free base) is an orally bioavailable β-adrenergic receptor (β-AR) antagonist with a Ki of 7.10 nM in a radioligand binding assay using rat heart muscle[1].
Tyr-(D-Dab4,Arg5,D-Trp8)-cyclo-Somatostatin-14 (4-11) is a somatostatin agonist that can be used in cancer research[1].
Carbacyclin is a PGI2 analogue, acts as a prostacyclin (PGI2) receptor agonist and vasodilator, and potently inhibits platelet aggregation.
Norbinaltorphimine dihydrochloride is a potent and selective κ opioid receptor antagonist.
MCH-1 antagonist 1 is a potent melanin concentrating hormone (MCH-1) antagonist with a Ki of 2.6 nM. MCH-1 antagonist 1 also inhibits CYP3A4 with an IC50 of 10 μM.
Adenosine receptor inhibitor 1 is a potent and selective adenosine receptor (AR) inhibitor with Ki values of >1000, 68.5, >1000, >1000 nM for A1AR, A2AAR, A2BAR, A3AR, respectively. Adenosine receptor inhibitor 1 shows antinociceptive activity, anti-inflammatory effect and peripheral analgesic effect. Adenosine receptor inhibitor 1 has the potential for the research of cancer or neurodegenerative diseases[1].