Catalog No.
Product Name
Application
Product Information
Citations
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adenylyl cyclase inhibitor
SQ22536 is an inhibitor of adenylyl cyclase with an IC50 of 1.4 uM. It can inhibit PGE1-stimulated increases in cAMP levels in intact human platelets.- Adrian Hilman, .et al. , FASEB J, 2026, Mar 31;40(6):e71696 PMID: 41847922
- Ke Qian, .et al. , EBioMedicine, 2023, Dec:98:104863 PMID: 37950995
- Harmine, also known as telepathine, is a fluorescent harmala alkaloid belonging to the beta-carboline family of compounds. It occurs in a number of different plants, most notably the Middle Eastern plant harmal or Syrian rue (Peganum harmala) and the South American vine Banisteriopsis caapi (also known as "yage" or "ayahuasca"). Harmine reversibly inhibits monoamine oxidase A (MAO-A), an enzyme which breaks down monoamines, making it a RIMA. Harmine selectively binds to MAO-A but does not inhibit the variant MAO-B.
- Agnes P Biju, .et al. , Synapse, 2026, Mar;80(2):e70044 PMID: 41840857
- Fariha Karim, .et al. , Synapse, 2025, Jul;79(4):e70024 PMID: 40619690
- Lei Tan, .et al. , Res Vet Sci, 2022, 145: 125-134 PMID: 35190327
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S1PR1 modulators
RPC1063 is a selective sphingosine 1 phosphate receptor modulators and methods which may be useful in the treatment of S1P1-?associated diseases.- Alessia Favaron, .et al. , Eur J Pharm Sci, 2024, Sep 1:200:106845 PMID: 38971433
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DAT and SLC6A2 inhibitor
GBR-12935 is a piperazine derivative which is a potent and selective dopamine reuptake inhibitor.- Alexander D H Kingdon, .et al. , J Antibiot (Tokyo), 2025, Jan;78(1):54-63 PMID: 39402358
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dopamine re-uptake inhibitor
Vanoxerine (GBR-12909) is a piperazine derivative which is a potent and selective DRI.- Alexander D H Kingdon, .et al. , J Antibiot (Tokyo), 2025, Jan;78(1):54-63 PMID: 39402358
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human A3 adenosine receptor antagonist /Aurora inhibitor
Reversine is a potent human A3 adenosine receptor antagonist with Ki of 0.66 μM, and a pan-aurora A/B/C kinase inhibitor with IC50 of 12 nM/13 nM/20 nM, respectively. Also used for stem cell dedifferentiation.- Amy H. Ide, .et al. , Mol Biol Cell, 2023, Jun 1;34(7):ar76 PMID: 37126397
- Hazheen K, .et al. , J Biol Chem, 2020, August 20 PMID: 32820050
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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
- Reboxetine is an antidepressant compound that selectively inhibits norepinephrine uptake (IC50s = 8.2 and 1,070 nM for norepinephrine and serotonin transporters, respectively). It displays greater than 1,000-fold affinity for binding rat norepinephrine receptors compared to serotonin, histamine, acetylcholine, or dopamine receptors (Kis = 1.1, 129, 1,400, 3,900, and >10,000 nM, respectively).
- Antonia Donat, .et al. , iScience, 2023, Aug 29;26(10):107761 PMID: 37720081
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PAR-1 Antagonist
Vorapaxar (SCH 530348) is a potent and orally active thrombin receptor (PAR-1) antagonist with Ki of 8.1 nM.- Arundhasa Chandrabalan, .et al. , Am J Physiol Cell Physiol, 2023, Jul 1;325(1):C272-C285 PMID: 37273236
- Arundhasa Chandrabalan, .et al. , Sci Rep, 2023, Jan 20;13(1):1124 PMID: 36670151
- Cansu Tekin, .et al. , Cell Oncol (Dordr), 2020, Aug 18 PMID: 32809114
- Cansu Tekin, .et al. , Oncotarget, 2018, Aug 10; 9(62): 32010-32023 PMID: 30174793
- Claushuis TA, .et al. , J Thromb Haemost, 2017, Apr;15(4):744-757 PMID: 28092405
- Maaike Waasdorp, .et al. , Biochem Biophys Rep, 2017, Jul; 10: 152-156 PMID: 29114573
- Joseph C. Mudd, .et al. , J Infect Dis, 2016, Dec 15; 214(12): 1808-1816 PMID: 27703039
- Corey E. Tabit, .et al. , Circulation, 2016, Jul 12; 134(2): 141-152 PMID: 27354285
- SEP-363856, also known as SEP-856, is an orally active and CNS active psychotropic agent.
- Britto Shajan, .et al. , Genomic Psychiatry, 2026, 2(1), 42-48
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NK1 receptor antagonist
Rolapitant, also known as SCH-619734, is a selective, bioavailable, CNS penetrant neurokinin NK1 receptor antagonist that shows behavioral effects in animals models of emesis.- Bubak AN, .et al. , J Infect Dis, 2018, Sep 8;218(8):1324-1335 PMID: 29788447
- Domperidone blocks the action of dopamine. It has strong affinities for the D2 and D3 dopamine receptors, which are found in the chemoreceptor trigger zone, located just outside the blood brain barrier, which, among others, regulates nausea and vomiting (area postrema on the floor of the fourth ventricle and rhomboid fossa).
- Claudia Alvarez Baron, .et al. , Sci Rep, 2025, Aug 16;15(1):29995 PMID: 40819150
- Reiko Watanabe, .et al. , J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
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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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Smo Antagonist
LDE225 (NVP-LDE225) is a potent, selective and orally bioavailable Smoothened (SMO) antagonist that inhibits hedgehog (Hh) signaling pathway via antagonism of the Smoothened receptor (SMO).- Daniel Doheny, .et al. , Oncogene, 2020, Oct;39(42):6589-6605 PMID: 32929154
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angiotensin AT2 receptor antagonist
PD 123319 ditrifluoroacetate is a potent, selective, non-peptide angiotensin AT2 receptor antagonist. IC50 values are 34 and 210 nM in rat adrenal tissue and brain respectively.- Dao-Lai Zhang, .et al. , eLife, 2018, 7: e33432 PMID: 29393851
- Dynorphin A (1-13) Acetate is a potent, endogenous ??-agonist.
- E J Kuijer, .et al. , Neuropharmacology, 2025, Jul 1:272:110407 PMID: 40074169
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CXCR4 antagonist
Plerixafor is an immunostimulant used to multiply hematopoietic stem cells and it is a chemokine receptor-4 antagonist for mobilization of hematopoietic stem cells for transplantation.- Federico Antoniciello, .et al. , Front Mol Biosci, 2023, May 11;9:887564 PMID: 35647033
- Mei Zheng, .et al. , Biomed Pharmacother, 2022, Jun;150:112996 PMID: 35462338
- Asiedu KO, .et al. , EJNMMI Res, 2018, Dec 13;8(1):109 PMID: 30547233
- Kingsley O. Asiedu, .et al. , Clin Cancer Res, 2017, Jun 1; 23(11): 2759-2768 PMID: 27965305
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DPP-4 Inhibitor
Linagliptin is a DPP-4 inhibitor, an enzyme that degrades the incretin hormones glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP).- Fen Zhuge, .et al. , Exp Neurol, 2024, Mar:373:114689 PMID: 38199510
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Androgen Receptor inhibitor
ARN-509 is an androgen receptor antagonist with potential antineoplastic activity. ARN-509 binds to AR in target tissues thereby preventing androgen-induced receptor activation and facilitating the formation of inactive complexes that cannot be translocated to the nucleus. This prevents binding to and transcription of AR-responsive genes.- Frédérique Mittler, .et al. , Front Oncol, 2017, 7: 293 PMID: 29322028
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peptide Oxytocin Receptor Inhibitor
Atosiban is a peptide Oxytocin Receptor Inhibitor.- G Perez-Hernandez, .et al. , J Dairy Sci, 2023, Dec;106(12):9855-9867 PMID: 37641323
- Nebivolol hydrochloride is t a highly selective antagonist of the β1-adrenoceptor (Ki = 0.88 nM, β2-adrenoceptor Ki = 48 nM).
- Giovanni Bocci, .et al. , ACS Pharmacol Transl Sci, 2020, Oct 14 PMID: 33330842
- Prostaglandin E1 (PGE1) is the theoretical cyclooxygenase metabolite of dihomo-γ-linolenic acid (DGLA), but it is virtually undetectable in the plasma of normal humans or other animals. The IC50 of PGE1 for the inhibition of ADP-induced human platelet aggregation is 40 nM.
- Hang Dong, .et al. , Int J Nanomedicine, 2023, 18: 3577-3593 PMID: 37409026
- Baharak Bahmani, .et al. , Nat Commun, 2021, Mar 31;12(1):1999 PMID: 33790276
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β3 adrenergic receptor activator
Mirabegron is a potent bladder relaxant and reagent for diabetes remedy.- Havard Fjelltveit, .et al. , Auton Neurosci, 2025, Apr:258:103253 PMID: 39977963
- Johanna Stenqvist, .et al. , Auton Neurosci, 2024, Jun 11:254:103194 PMID: 38875740
- Bhavik Patel, .et al. , Pharmacol Res Perspect, 2020, 8 (1), e00564 PMID: 32030913
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CXCR4 antagonist
Plerixafor is an immunostimulant used to multiply hematopoietic stem cells and it is a chemokine receptor-4 antagonist for mobilization of hematopoietic stem cells for transplantation.- Helen C Wang, .et al. , Cell Rep, 2024, Aug 27;43(8):114542 PMID: 39046877
- Hitoshi Maeda, .et al. , Int J Biol Macromol, 2022, Sep 17;221:1439-1452 PMID: 36126807
- Jingying Chen, .et al. , Development, 2022, Jul 1;149(13) PMID: 35694896
- Narubhorn Ongprakobkul, .et al. , Am J Orthod Dentofacial Orthop, 2022, Mar 2;S0889-5406(22)00107-X PMID: 35248418
- Chunliang Liu, .et al. , J Trace Elem Med Biol, 2022, Jan 10;71:126927 PMID: 35030482
- Eri Watanabe, .et al. , Angiogenesis, 2020, Jul 22 PMID: 32699964
- Alessandra Esposito, .et al. , Bone, 2020, Jul 3;139:115521 PMID: 32629173
- Kentaro Suzuki, .et al. , Sci Rep, 2019, 9: 15284
- Ichimizu S, .et al. , J Control Release, 2019, May 10;304:156-163 PMID: 31082432
- Nan Li, .et al. , Diagn Pathol, 2019, Jan 12;14(1):3 PMID: 30636642
- Thida W, .et al. , Biochem Biophys Res Commun, 2018, Nov 20. pii: S0006-291X(18)32477-X PMID: 30470571
- Henry R. Hampton, .et al. , Nat Commun, 2015, 6: 7139 PMID: 25972253
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5-HT2A receptor antagonist
Volinanserin is a highly selective 5-HT2A receptor antagonist.- Hugo R Arias, .et al. , Eur J Pharmacol, 2024, Mar 5:966:176329 PMID: 38253116
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somatostatin receptor antagonist
Octreotide is a peptide agonist for sst2, sst3 and sst5 somatostatin receptors. IC50/Kd values (nM) at cloned human somatostatin receptors are: 290 - 1140 (sst1), 0.4 - 2.1 (sst2), 4.4 - 34.5 (sst3), > 1000 (sst4), and 5.6 - 32 (sst5).- Ida Vang Andersen, .et al. , Nucl Med Biol, 2024, May-Jun:132-133:108905 PMID: 38555651
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OX1 receptor antagonist
SB 334867 is a selective non-peptide orexin OX1 receptor antagonist. pKb values are 7.2 and < 5 for inhibition of intracellular Ca2+ release in CHO cells expressing human OX1 and OX2 receptors respectively. Blocks orexin-A induced grooming and feeding following systemic administration in vivo.- Ines M Amaral, .et al. , Psychopharmacology (Berl), 2024, Sep 20 PMID: 39302438
- Tony Ngo, .et al. , Nat Chem Biol, 2017, Feb; 13(2): 235-242 PMID: 27992882
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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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Adenosine kinase inhibitor
5-Iodotubercidin is a potent adenosine kinase inhibitor with IC50 of 26 nM.- Jing-Yu Lin, .et al. , Cell Discov, 2020, 6: 20 PMID: 32284878
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β-adrenergic blocker
S(-)-Propranolol Hydrochloride is a nonselective β-adrenergic receptor (βAR) antagonist, has high affinity for the β1AR and β2AR with Ki values of 1.8 nM and 0.8 nM, respectively. Propranolol hydrochloride inhibits [3H]-DHA binding to rat brain membrane preparation with an IC50 of 12 nM.- Jingyeong Shin, .et al. , Chemical Engineering Journal, 2023, December
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Histamine H2-receptor antagonist
Ranitidine is a potent, selective and orally active histamine H2-receptor antagonist with an IC50 of 3.3 μM that inhibits gastric secretion.- Jingyeong Shin, .et al. , Chemical Engineering Journal, 2023, December
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H2-receptor antagonist
Cimetidine is a histamine H2-receptor antagonist that inhibits stomach acid production.- Jingyeong Shin, .et al. , Chemical Engineering Journal, 2023, December
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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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α2C antagonist
JP 1302 2HCl is a potent and selective α2C antagonist.- Junya Maruoka, .et al. , Int J Neuropsychopharmacol, 2026, Apr 6;29(4):pyag007 PMID: 41717785
- Ciproxifan is an extremely potent histamine H3 inverse agonist/antagonist.
- K Yamamoto, .et al. , Naunyn-Schmiedeberg's Arch Pharmacol, 2019, pp 1-12 PMID: 30919010
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Histamine Antagonist
JNJ7777120 is a potent, selective non-imidazole H4?histamine receptor antagonist.- K Yamamoto, .et al. , Naunyn-Schmiedeberg's Arch Pharmacol, 2019, pp 1-12 PMID: 30919010
- Yamamoto K, .et al. , Neurosci Lett, 2018, May 29;676:103-107 PMID: 29655943
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CysLT1 receptor antagonist
MK-571 is a potent CysLT1 (LTD4) leukotriene receptor inverse agonist with EC50 value of 1.3 nM.- Kaito Yamashiro, .et al. , J Toxicol Sci, 2026, 51(2):141-147 PMID: 41621859
- Jung-Hung Chen, .et al. , Biomed Pharmacother, 2022, Oct;154:113613 PMID: 36058146
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5-HT1C receptor antagonist
Clozapine N-oxide is a major metabolite of Clozapine noted to decrease SR-2A (5-HT2 serotonin receptor) density in vitro.- Kazuhei Niitani, .et al. , J Pharmacol Sci, 2025, Sep;159(1):1-7 PMID: 40713343
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H1 antagonist
Asenapine shows high affinity (pKi) for numerous receptors, including the serotonin 5-HT1A (8.6), 5-HT1B (8.4), 5-HT2A (10.2), 5-HT2B (9.8), 5-HT2C (10.5), 5-HT5A (8.8), 5-HT6 (9.5), and 5-HT7 (9.9) receptors, the adrenergic α1 (8.9), α2A (8.9), α2B (9.5), and α2C (8.9) receptors, the dopamine D1 (8.9), D2 (8.9), D3 (9.4), and D4 (9.0) receptors, and the histamine H1 (9.0) and H2 (8.2) receptors.- Keisuke Obara, .et al. , Biol Pharm Bull, 2021, 44, 1140-1150 PMID: 34334499
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CXCR4 antagonist
AMD 3465 is a potent, selective CXCR4 antagonist.- Kentaro Suzuki, .et al. , Sci Rep, 2019, 9: 15284
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orexin receptor antagonist
Nemorexant (ACT-541468) is a potent orexin receptor antagonist extracted from patent WO2015083094A1, compound example 7, has IC50s of 2 nM and 3 nM for Ox1 receptor and Ox2 receptor, respectively.- Koichi Aoyama, .et al. , Forensic Toxicol, 2026, Jan;44(1):130-140 PMID: 41396382
- Doxazosin mesylate, a quinazoline compound, is an α1-selective alpha blocker used to treat high blood pressure and urinary retention associated with benign prostatic hyperplasia (BPH).
- L Klem, .et al. , Psychopharmacology (Berl), 2023, Aug;240(8):1629-1650 PMID: 37329343
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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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Opioid Receptor antagonist
JTC-801 is a selective antagonist for the nociceptin receptor, also known as the ORL-1 receptor.- Lihao Gu, .et al. , Cosmetics, 2017, 4(4), 48
- Toshio Yawata, .et al. , Mol Cell Biochem, 2016, Jan;411(1-2):201-11 PMID: 26427671
