Catalog No.
Product Name
Application
Product Information
Citations
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mGlu5 modulator
JNJ-46778212 (VU 0409551) is an mGlu5 positive allosteric modulator with an EC50 of 260 nM. -
GRK2 inhibitor
GSK180736A is a G protein-coupled receptor kinase 2 (GRK2) inhibitor with an IC50 of 0.77 μM. -
S1P1/S1P5 receptor agonist
GSK2018682 is an agonist for S1P1 and S1P5 receptor with pEC50s of 7.7 and 7.2, respectively, and has no agonist activity towards human S1P2, S1P3, or S1P4. GSK2018682 is used in the research of multiple sclerosis. -
5-HT1B receptor antagonist
SB-616234A is a selective and orally bioavailable 5-HT1B receptor antagonist, with anxiolytic and antidepressant activity. -
5-HT2/sigma 2 receptor antagonist
Roluperidone, also known as MIN-101, CYR-101, and MT-210, is a 5-HT2A and sigma 2 receptor antagonist potentially for the treatment of schizophrenia. -
neurokinin receptors antagonist
SSR-241586 is an antagonist of neurokinin receptors. SSR-241586 is shown to be active in the treatment of depression, schizophrenia, urinary trouble, emesis, and irritable bowel syndrome (IBS). -
β3-adrenergic receptor agonist
Solabegron (GW 427353) is a selective β3-adrenergic receptor agonist, stimulating cAMP accumulation in Chinese hamster ovary cells expressing the human β3-AR, with an EC50 value of 22 nM. -
metabotropic receptor agonist
trans-ACPD, a metabotropic receptor agonist, produces calcium mobilization and an inward current in cultured cerebellar Purkinje neurons. -
GPR40 agonist
Setogepram sodium salt (PBI-4050 sodium salt) acts as an orally active agonist for GPR40 and as an antagonist or inverse agonist for GPR84. -
dual dopamine and serotonin receptor antagonist
Deschloroclozapine is a dual dopamine and serotonin receptor antagonist with Kis of 200, 2500, 420, 39, 84, 40 nM for dopamine D1, D2,D4, and serotonin S2A, S2C, S3, respectively. -
5-HT3 receptor selective agonist
Phenylbiguanide is a 5-HT3 receptor selective agonist with an EC50 of 3.0±0.1 μM. -
vasopressin V2-receptor agonist
WAY-151932 is a vasopressin V2-receptor agonist with IC50 of 80.3 nM and 778 nM in human-V2 binding and V1a binding assay. -
angiotensin II receptor type 1 antagonist
Azilsartan medoxomil monopotassium is an orally administered angiotensin II receptor type 1 antagonist with IC50 of 0.62 nM, which used in the treatment of adults with essential hypertension. -
5-HT1A/5-HT1B/5-HT1C agonist
Eltoprazine(DU28853) is a serenic or antiaggressive agent which as an agonist at the 5-HT1A and 5-HT1B receptors and as an antagonist at the 5-HT2C receptor. -
β2-adrenergic receptor agonist
Levosalbutamol tartrate(levalbuterol) is the R-enantiomer of the short-acting β2-adrenergic receptor agonist salbutamol. -
leukotriene A4 hydrolase inhibitor
Acebilustat (CTX-4430) is a leukotriene A4 hydrolase inhibitor, used for an oral antiinflammatory drug. -
angiotensin II and endothelin A receptor antagonist
Sparsentan (RE-021) is a highly potent dual angiotensin II and endothelin A receptor antagonist with Kis of 0.8 and 9.3 nM, respectively. -
thromboxane-prostaglandin receptor antagonist
Terutroban is a thromboxane-prostaglandin receptor antagonist. -
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.
