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Catalog No.
Product Name
Application
Product Information
Citations
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β2-AR agonist
Higenamine (Norcoclaurine), a β2-AR agonist, is a key component of the Chinese herb aconite root that prescribes for treating symptoms of heart failure in the oriental Asian countries.- Ana Rubio, .et al. , Drug Test Anal, 2023, Jul 31 PMID: 37525530
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dopamine D2 receptor agonist
UNC 9994 hydrochloride, unique, beta-arrestin-biased functionally selective dopamine D2 receptor (D2R) agonist (Ki value 30 nM; EC50 value 50 nM in ??-arrestin-2 recruitment assay) that exhibits antipsychotic activity in vivo. UNC9994 markedly inhibited PCP-induced hyperlocomotion in wild-type mice, which effect was completely abolished in ??-arrestin-2 knockout mice.- Anika Mann, .et al. , Sci Rep, 2021, Apr 15;11(1):8288 PMID: 33859231
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MC4R agonist
Setmelanotide (RM-493; BIM-22493; IRC-022493) is a selective melanocortin 4 receptor (MC4R) agonist with EC50s of 0.27 nM and 0.28 nM for human and rat MC4R, respectively.- Dajin Cho, .et al. , J Neurosci, 2023, Sep 6;43(36):6280-6296 PMID: 37591737
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5-HT1A receptor agonist
Aripiprazole is a human 5-HT1A receptor partial agonist with a Ki of 4.2 nM.- Jaime Osuna-Luque, .et al. , J Exp Neurosci, 2018, 12: 1179069518798628 PMID: 30245571
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β1-selective adrenergic receptor agonist
Norepinephrine (Levarterenol; L-Noradrenaline) is a β1-selective adrenergic receptor agonist with EC50 of 5.37 μM.- Johanna Stenqvist, .et al. , Auton Neurosci, 2024, Jun 11:254:103194 PMID: 38875740
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α1-adrenergic receptor agonist
Phenylephrine is a selective α1-adrenergic receptor agonist used primarily as a decongestant, as an agent to dilate the pupil, and to increase blood pressure.- Johanna Stenqvist, .et al. , Auton Neurosci, 2024, Jun 11:254:103194 PMID: 38875740
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β adrenoceptor agonist
Isoprenaline or isoproterenol is a non-selective beta-adrenergic agonist and structurally similar to adrenaline.- Johanna Stenqvist, .et al. , Auton Neurosci, 2024, Jun 11:254:103194 PMID: 38875740
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GHSR agonist
Anamorelin (ONO-7643, RC-1291, ST-1291) is an orally active, high-affinity, selective agonist of the ghrelin receptor with an EC50 value of 0.74 nM in the HEK293/GRLN FLIPR assay. Anamorelin is currently under development for the management of non-small lung cancer associated cachexia/anorexia.
- Josua Jordi, .et al. , Sci Adv, 2018, Oct; 4(10): eaav1966 PMID: 30402545
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5-HT1B/1D receptor agonist
Eletriptan hydrobromide is a selective SR-1B/SR-1D agonist.- Li Li, .et al. , J Exp Med, 2022, Aug 1;219(8):e20212307 PMID: 35796804
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5-HT Receptor agonist
Almotriptan malate (Axert) is a selective 5-hydroxytryptamine1B/1D (5-HT1B/1D) receptor agonist, used for the treatment of Migraine attacks in adults.- Li Li, .et al. , J Exp Med, 2022, Aug 1;219(8):e20212307 PMID: 35796804
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GLP-1 receptor agonist
Dulaglutide is a glucagon-like peptide-1 (GLP-1) receptor agonist.- Liuqing Xi, .et al. , Peptides, 2025, Mar:185:171366 PMID: 39954860
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dopamine receptor agonist
Nalmefene hydrochloride is an opioid receptor antagonist.- Mark G Papich, .et al. , Drug Deliv Transl Res, 2022, Feb;12(2):376-383 PMID: 34817831
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SMO agonist
SAG is a chlorobenzothiophene-containing compound which acts as a SMO agonist (EC50 = 3 nM) but inhibits hedgehog signaling at high concentrations (>1 uM).- Mark van den Hurk, .et al. , NPJ Parkinsons Dis, 2022, Oct 18;8(1):134 PMID: 36258029
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Dopamine Receptor agonist
Rotigotine hydrochloride is a dopamine D2 and D3 receptor agonist. Ki values are 13 and 0.71 nM for D2 and D3 respectively.- Mattia Ferraiolo, .et al. , Neuropharmacology, 2022, 207: 108942 PMID: 35026287
- Mattia Ferraiolo, .et al. , Eur J Pharmacol, 2021, Nov 15;911:174557 PMID: 34626593
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CB2 inverse agonist
SR 144528 is a selective peripheral cannabinoid receptor inverse agonist that displays a Ki value of 0.6 nM for rat spleen and human recombinant CB2 receptors and a Ki value of 400 nM for rat brain and human recombinant CB1 receptors.- Ming Tang, .et al. , Cell Death Dis, 2018, Jun; 9(6): 601 PMID: 29789558
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5-HT Receptor agonist
Prucalopride is a selective, high affinity 5-HT4 receptor agonist which targets the impaired motility associated with chronic constipation, thus normalising bowel movements.- Pierre Meschin, .et al. , Cell Calcium, 2015, Dec;58(6):549-57 PMID: 26427584
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Adenosine A2A Receptor Agonist
CGS 21680 is a specific adenosine A2A subtype receptor agonist.- Qian Wang, .et al. , Neuropharmacology, 2019, 148: 229-243 PMID: 30659840
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5HT(1A) receptor agonist
Buspirone is a serotonergic (5HT(1A) receptor agonist) anxiolytic drug with some D(2) dopaminergic effect, used for anxiety disorders.- Reilly Taylor, .et al. , Front. Biosci. (Elite Ed), 2026, 18(1): 44075 PMID: 41914162
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MOR agonist
SR17018 is an mu-opioid-receptor (MOR) agonist with an EC50 of 97 nM.- Rob Hill, .et al. , Br J Pharmacol, 2023, Jul 24 PMID: 37489013
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Adenosine A3-R agonist
IB-MECA has been shown to act as a potent and selective Adenosine A3-R agonist with Ki values of 1.1, 54 and 56 nM for Adenosine A3-R, Adenosine A1-R and Adenosine A2A-R, respectively.- Sameshima T, .et al. , Chem Res Toxicol, 2019, Aug 28 PMID: 31461269
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Guanylate cyclase C agonist
Linaclotide is a peptide agonist of the guanylate cyclase 2C.- Tessa A Groeneweg, .et al. , Ann N Y Acad Sci, 2026, Feb;1556(1):e70152 PMID: 41400434
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GLP-1 agonist
Albiglutide is a glucagon-like peptide-1 agonist (GLP-1 agonist).- Tito Borner, .et al. , Cell Rep, 2020, Jun 16;31(11):107768 PMID: 32553160
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CB receptor agonist
WIN 55,212-2 is a potent cannabinoid receptor agonist that has been found to be a potent analgesic in a rat model of neuropathic pain. It activates p42 and p44 MAP kinase via receptor-mediated signaling.- Vida Mirzaie, .et al. , Iran J Basic Med Sci, 2025, 28(9):1171-1179 PMID: 40809175
- Vida mirzaie, .et al. , Research Square, 2024, October
- Greish K, .et al. , J Control Release, 2018, Dec 10;291:184-195 PMID: 30367922
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GPR agonist
TAK-875 is a potent, selective, and orally bioavailable GPR40 agonist.- Ying Liu, .et al. , Nucleic Acids Res, 2018, Oct 12; 46(18): 9864-9874 PMID: 30219861
- Deborah A. Goldspink, .et al. , Mol Metab, 2018, Jan; 7: 90-101 PMID: 29167062
- Hodaka Yamada, .et al. , Sci Rep, 2016, 6: 25912 PMID: 27180622
- 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.
- Zhenhuan Zheng, .et al. , Mol Metab, 2026, Mar 14;106:102340 PMID: 41833222
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GPR35/CXCR8 agonist
GPR35 agonist 1 (compound 50) is a potent and specific G protein-coupled receptor-35 (GPR35)/CXCR8 agonist with an EC50 of 5.8 nM, displays good druggability. -
Sigma-2 receptor agonist
Siramesine Hydrochloride is a selective sigma-2 receptor agonist, which has been shown to trigger cell death of cancer cells and to exhibit a potent anticancer activity in vivo. -
A2A adenosine agonist
Regadenoson was selective agonist for the A2A adenosine receptor versus the A1, A2B, and A3 receptors in binding and functional studies. Regadenoson was also found to be a full and potent agonist to cause coronary vasodilation, a response that has a very large A2A receptor reserve? -
Opioid Receptor Agonist
Cebranopadol is a potent nociceptin/orphanin FQ peptide (NOP) and opioid receptor agonist -
β3-adrenergic receptor agonist
β3-AR agonist 1 (compound 15) is a highly potent, selective, and orally available β3-adrenergic receptor (β3-AR) agonist (EC50=18 nM), being inactive to β1-, β2-, and α1A-AR (β1/β3, β2/β3, and α1A/β3>556-fold). -
beta2-adrenergic agonist
Arformoterol tartrate is a beta2-adrenergic agonist -
5-HT1A receptor agonist
Lesopitron dihydrochloride is a full and selective 5-HT1A receptor agonist with IC50 of 125 nM in rat hippocampal membranes. -
sigma 1 receptor(σ1R) agonist
SA4503 is a selective sigma 1 receptor(ς1R) agonist; high affinity for the sigma 1 receptor subtype labeled by (+)-[3H]pentazocine (IC50 = 17.4 +/- 1.9 nM); 100-fold less affinity for the sigma 2 receptor. -
α2 adrenergic agonist
AGN 192836 is a potent and selective α2 adrenergic agonist with EC50s of 8.7, 41 and 6.6 nM for α2A, α2B and α2C receptor, respectively. -
Sigma-2 receptor agonist
Anti-cancer agent siramesine is a lysosomotropic detergent that induces cytoprotective autophagosome accumulation. -
Adrenergic Receptor agonist
Tetrahydrozoline Hydrochloride is an alpha agonist which causes constriction of conjunctival blood vessels. -
D2 agonist
Naxagolide is a dopamine D2-receptor agonist which is used for the treatment of extrapyramidal disorders. -
dopamine D2-receptor agonist
ent Naxagolide Hydrochloride is a dopamine D2-receptor agonist which is used for the treatment of extrapyramidal disorders. This compound is an antiparkinsonian drug. -
ultra-long-acting β??? adrenoreceptor agonist
Vilanterol is a novel and selective agonist of Beta2-AR with a PEC50 value of 10.37??0.05. -
5-HT1B/1D receptors agonist
Donitriptan is a potent, high efficacy agonist at 5-HT1B/1D receptors with pKis of 9.4 and 9.3, respectively.
