Catalog No.
Product Name
Application
Product Information
Citations
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PAFR inhibitor/H1 receptor inhibitor
Rupatadine is an inhibitor of PAFR and histamine (H1) receptor with Ki of 550 and 102 nM, respectively. -
antagonist of melanin concentrating hormone receptor 1
MCHr1 antagonist 2 is an antagonist of melanin concentrating hormone receptor 1, with an IC50 of 65 nM; MCHr1 antagonist 2 also inhibits hERG, with an IC50 of 4.0 nM in IMR-32 cells. -
sGC activator
YC-1 is a direct activator of soluble Guanylyl Cyclase (sGC), independent of Nitric Oxide. -
mGluR5 positive allosteric modulator
BMT-145027 is an mGluR5 positive allosteric modulator without inherent agonist activity, exhibits an EC50 of 47 nM. -
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. -
mGlu4 receptors modulator
VU 0361737 is a selective positive allosteric modulator at mGluR-4 (EC50 values are 240 and 110 nM at human and rat receptors respectively). -
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. -
OX Antagonist
Almorexant(ACT078573) is a potent and competitive dual orexin 1 receptor (OX1)/orexin 2 receptor (OX2) antagonist with Ki values of 1.3 and 0.17 nM for OX1 and OX2, respectively. -
sigma-1 receptor antagonist
S1RA is a selective sigma-1 receptor antagonist, with a reported binding affinity of Ki = 17.0 ?? 7.0 nM, selective over the sigma-2 receptor and against a panel of other 170 receptors, enzymes, transporters and ion channels. -
5-HT6R antagonist
Lu AE58054 is a potent and selective 5-HT6 receptor antagonist. - Pramipexole dihydrochloride is a dopamine receptor agonist exhibiting selectivity for the D3 receptor.
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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? -
adenosine A2A/A1 receptor antagonist
A2A receptor antagonist 1 (CPI-444 analog) is an antagonist of both adenosine A2A receptor and A1 receptor with Kis of 4 and 264 nM, respectively. -
CXCR4 Inhibitor
MSX-122 is an orally bioavailable inhibitor of CXCR4 (IC50 = ~10 nM) with potential antineoplastic and antiviral activities. CXCR4 inhibitor MSX-122 binds to the chemokine receptor CXCR4, preventing the binding of stromal derived factor-1 (SDF-1) to the CXCR4 receptor and receptor activation, which may result in decreased tumor cell proliferation and migration. -
5-HT Receptor modulator
Lu-AA21004 is an oral multimodal serotonergic agent, inhibits 5-HT(1A), 5-HT(1B), 5-HT(3A), 5-HT(7) and SERT with IC50 of 15 nM, 33 nM, 3.7 nM, 19 nM and 1.6 nM, respectively. -
SphK2 inhibitor
ABC294640 is an orally available, aryladamantane compound and selective inhibitor of sphingosine kinase-2 (SK2) with potential antineoplastic activity. -
serotonin/dopamine/norepinephrine reuptake inhibitior
SPD-473 citrate is a serotonin/dopamine/norepinephrine reuptake inhibitior. -
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.
