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Catalog No.
Product Name
Application
Product Information
Product Citation
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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. -
A2A Receptor Antagonist
SCH 442416 is a selective adenosine A2A receptor antagonist; binds to human and rat A2A receptors with high affinity (Ki values are 0.048 and 0.5 nM respectively). Displays > 23000-fold selectivity for hA2A over hA1 in vitro with minimal affinity for hA2B and hA3 receptors (IC50 > 10 μM). -
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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Smoothened Inhibitor
LDE225 is an orally bioavailable small-molecule Smoothened (Smo) antagonist with potential antineoplastic activity. -
Smoothened Inhibitor
PF-5274857 is a novel Smo antagonist that specifically binds to Smo with a K(i) of 4.6 ?? 1.1 nmol/L and completely blocks the transcriptional activity of the downstream gene Gli1 with an IC(50) of 2.7 ?? 1.4 nmol/L in cells. -
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). -
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). -
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.- Tony Ngo, .et al. , Nat Chem Biol, 2017, Feb; 13(2): 235-242 PMID: 27992882
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NK1 receptor antagonist
GR 205171 is a selective neurokinin-1 receptor antagonist -
beta2-adrenergic agonist
Arformoterol tartrate is a beta2-adrenergic agonist -
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. , 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
- Bepotastine is a non-sedating, selective antagonist of the histamine 1 (H1) receptor.
- Tamsulosin hydrochloride is an antagonist of alpha1A adrenoceptors in the prostate.
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β3 adrenergic receptor activator
Mirabegron is a potent bladder relaxant and reagent for diabetes remedy.- Bhavik Patel, .et al. , Pharmacol Res Perspect, 2020, 8 (1), e00564 PMID: 32030913
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EP2 Receptor antagonist
PF-04418948 is a potent and selective prostaglandin EP2 receptor antagonist with IC50 of 16 nM. Phase 1. -
S1PR1/S1PR5 inhibitor
BAF312 is a next-generation potent sphingosine 1-phosphate (S1P) receptor agonist, selective for S1P1 and S1P5. -
CB1 receptor antagonist
AM251 is a potent CB1 receptor antagonist (IC50 = 8 nM, Ki = 7.49 nM) that displays 306-fold selectivity over CB2 receptors. -
5-HT1A receptor agonist
Lesopitron dihydrochloride is a full and selective 5-HT1A receptor agonist with IC50 of 125 nM in rat hippocampal membranes. -
5-HT3 receptor antagonist
Pancopride is a new potent and selective 5-HT3 receptor antagonist. -
prostaglandin F2α (PGF2α) analogue
(+)-Cloprostenol is a prostaglandin F2α (PGF2α) analogue, and shows selective agonistic activity at the prostaglandin receptor. -
5-HT2A and 5-HT2C receptors antagonist
Deramciclane has a high affinity for 5-HT2A and 5-HT2C receptors; it acts as an antagonist at both receptor subtypes and has inverse agonist properties at the 5-HT2C receptors without direct stimulatory agonist. -
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. -
endothelin receptor modulator
Endothelin Mordulator 1 is a endothelin receptor modulator, used for the research of endothelin-mediated disorders. -
D1/D5 receptor antagonist
SCH 23390 hydrochloride is a potent dopamine receptor antagonist (Ki values are 0.2 nM and 0.3 nM at D1 and D5 receptor sub-types, respectively). -
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.- 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-HT1B receptor agonist
Eletriptan is a selective 5-hydroxytryptamine 1B/1D (5-HT1B) receptor agonist -
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. -
5-HT1A receptor antagonist
NAD 299 hydrochloride (Robalzotan) is a selective, high affinity 5-HT1A receptor antagonist (Ki = 0.6 nM in vitro). -
CGRP receptor antagonist
BMS-927711 is a potent, selective, competitive human calcitonin gene-related peptide (CGRP) receptor antagonist that has shown in vivo efficacy without vasoconstrictor effect.
