Catalog No.
Product Name
Application
Product Information
Citations
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D2 receptor antagonist
Pipamperone (Floropipamide; McN-JR 3345; R 3345) is a high-affinity antagonist of 5-HT2A receptor (pKi=8.2) and D4 receptor (pKi=8.0) and a low-affinity antagonist of D2 receptor (pKi=6.7). - KW-8232 free base is an anti-osteoporotic agent, and can reduces the biosynthesis of PGE2.
- Melanotan II is a high affinity melanocortin receptor agonist (Ki values are 0.67, 6.6, 34 and 46 nM for MC1, MC4, MC3 and MC5 receptors respectively).
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CXCR2 antagonists
CXCR2-IN-1 is a central nervous system penetrant CXCR2 antagonists with a pIC50 of 9.3. -
alpha-1A/alpha-1B-adrenoceptor antagonist
Tamsulosin is an alpha1a-selective alpha blocker used in the symptomatic treatment of benign prostatic hyperplasia (BPH). -
Adenosine receptor inhibitor
N-[(4-Aminophenyl)methyl]adenosine is a adenosine receptor inhibitor, with Ki of 29 nM for Rat ecto-5??-Nucleotidase. IC50 value: 29.0 ± 1.7 nM (Ki) Target: Adenosine Receptor -
GluR modulator
VU 0364439 is a positive allosteric modulator (PAM) of mGlu4 receptors (EC50 = 19.8 nM in vitro for human mGlu4). -
Opioid Receptor Agonist
Cebranopadol is a potent nociceptin/orphanin FQ peptide (NOP) and opioid receptor agonist -
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). -
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). -
NK1 receptor antagonist
GR 205171 is a selective neurokinin-1 receptor antagonist -
beta2-adrenergic agonist
Arformoterol tartrate is a beta2-adrenergic agonist - 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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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. -
5-HT1A receptor agonist
Lesopitron dihydrochloride is a full and selective 5-HT1A receptor agonist with IC50 of 125 nM in rat hippocampal membranes. -
nonpeptide bradykinin receptor B2 antagonist
FR167344 free base is an orally active, nonpeptide bradykinin receptor B2 antagonist. -
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. -
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. -
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). -
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.
