Catalog No.
Product Name
Application
Product Information
Citations
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monoamine reuptake inhibitor
Diclofensine hydrochloride (Ro-8-4650 hydrochloride) is a potent inhibitor of monoamine reuptake, blocking the uptake of dopamine, noradrenaline, and serotonin by rat brain synaptosomes with IC50 values of 0.74, 2.3, and 3.7 nM, respectively. -
histamine 1 receptor antagonist
Decloxizine(UCB-1402; NSC289116) is a histamine 1 receptor antagonist. -
A1 receptor agonist
N6-Cyclohexyladenosine is a selective A1 receptor agonist (EC50 = 8.2 nM). -
CysLT1/CysLT2 antagonist
Gemilukast is an orally active and potent dual cysteinyl leukotriene 1 and 2 receptors (CysLT1 and CysLT2) antagonist, with IC50s of 1.7, 25 nM for human CysLT1 and CysLT2, respectively. -
guanylate cyclase stimulator
Vericiguat (BAY1021189) is a potent, orally available and soluble guanylate cyclase stimulator. -
DP1/EP2 agonist
Treprostinil sodium is a potent DP1 and EP2 agonist with EC50 values of 0.6??0.1 and 6.2??1.2 nM, respectively. -
histamine H4 receptor antagonist
Toreforant is a potent and selective histamine H4 receptor (H4R) antagonist, with a Ki at the human receptor of 8.4 nM. -
A2AR/ENT1 agonist
A2AR-agonist-1 is a potent A2AR and ENT1 agonist with Ki of 4.39 and 3.47 for A2AR and ENT1. -
Sigma-1 receptor agonist/muscarinic M1 agonist
Blarcamesine, also known as AVex-73 and AE-37, is a muscarinic M1 agonist potentially for the treatment of Alzheimer's disease. It is an ς receptor ligand. -
dual NE/DA transporter inhibitor
Centanafadine is dual norepinephrine (NE)/dopamine (DA) transporter inhibitor, also inhibits serotonin transporter, with IC50s of 6 nM, 38 nM and 83 nM for human NE, DA and serotonin transporter , respectively. -
endothelin (ET) receptor antagonist
Tezosentan (RO 610612) is an endothelin (ET) receptor antagonist, with pA2s of 9.5, 7.7 for ETA and ETB receptors, respectively. -
sigma 1 receptor agonist
Cutamesine (SA4503; AGY-94806) is a selective sigma 1 receptor(??1R) 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. -
FFAR1/GPR40 activator
GPR40 Activator 1 is a potent GPR40 activator for treatment of type 2 diabetes. -
group III mGluR receptors agonist
O-Phospho-L-serine is the immediate precursor to L-serine in the serine synthesis pathway, and an agonist at the group III mGluR receptors (mGluR4, mGluR6, mGluR7, and mGluR8); O-Phospho-L-serine also acts as a weak antagonist for mGluR1 and a potent antagonist for mGluR2. -
NK3R antagonist
Pavinetant (MLE-4901) is a neurokinin-3 receptor (NK3R) antagonist. -
NPY Y5 receptor antagonist
Velneperit (S-2367) is a novel neuropeptide Y (NPY) Y5 receptor antagonist. -
D3 receptor and D2 receptor partial agonist
Cariprazine is a novel antipsychotic drug candidate that exhibits high affinity for the D3 (Ki=0.085 nM) and D2 (Ki=0.49 nM) receptors, and moderate affinity for the 5-HT1A receptor (Ki=2.6 nM). -
B1 receptor antagonist
ELN-441958 is a potent, neutral antagonist of B1 receptor, inhibits the binding of the B1 agonist ligand [3H]DAKD to IMR-90 cells with Ki of 0.26 nM. -
OT-R antagonist
OT-R antagonist 1 is a new potent and selective nonpeptide low molecular weight OT-R antagonist. -
mGlu5 receptor antagonist
Mavoglurant is a structurally novel, non-competitive mGlu5 receptor antagonist, has an IC50 of 30 nM in a functional assay with human mGluR5. -
mGlu5 negative allosteric modulator
Basimglurant (RG7090) is a potent, selective and orally available mGlu5 negative allosteric modulator with a Kd of 1.1 nM. -
GHSR agonist
Capromorelin Tartrate is an orally active, potent growth hormone secretagogue receptor (GHSR) agonist, with Ki of 7 nM for hGHS-R1a. -
leukotriene receptor antagonist
Tipelukast (KCA 757) is a sulfidopeptide leukotriene receptor antagonist, an orally bioavailable anti-inflammatory agent and used for the treatment of asthma. -
5-HT2B receptor antagonist
RS 127445 is a novel high affinity, selective 5-HT2B receptor antagonist with pKi of 9.5. -
5-HT1A/5-HT1B/5-HT3A/5-HT7 receptor/SERT inhibitor
Vortioxetine is a inhibitor of 5-HT1A, 5-HT1B, 5-HT3A, 5-HT7 receptor and SERT, with Ki values of 15 nM, 33 nM, 3.7 nM, 19 nM and 1.6 nM, respectively. -
Sigma receptor agonist
Ditolylguanidine (1,3-Di-o-tolylguanidine) is an agonist of sigma receptor (??1/??2 receptor).
