Catalog No.
Product Name
Application
Product Information
Citations
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neuropeptide Y Y2 receptor antagonist
JNJ-31020028 is a novel, selective, brain-penetrant neuropeptide Y Y2 receptor antagonist - Capromorelin functions as a growth hormone secretagogue and ghrelin mimetic which causes the body to secrete human growth hormone in a way usually seen at puberty and in young adulthood.
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ETBR antagonist
BQ-788 sodium salt is a selective ETBR (Endothelin receptor B ) antagonist. -
5-HT3 receptor antagonist
Tropisetron is a selective 5-HT3 receptor antagonist and α7-nicotinic receptor agonist with an IC50 of 70.1 ?? 0.9 nM for 5-HT3 receptor. -
Dopamine receptor agonist
(+)-PD 128907 hydrochloride is a potent D3DR (dopamine receptor) agonist (Ki = 2.3 nM). -
serotonin/NE reuptake inhibitor
Levomilnacipran HCl is a selective serotonin and norepinephrine reuptake inhibitor. -
Adenosine A3 receptor agonist
CF-102 is an orally bioavailable, synthetic, highly selective adenosine A3 receptor (A3AR) agonist with potential antineoplastic activity. -
NK1 receptor antagonist
Netupitant is a selective neurokinin 1 (NK1) receptor antagonist. It competitively binds to and blocks the activity of the human substance P/NK1 receptors in the central nervous system (CNS), thereby inhibiting NK1-receptor binding of the endogenous tachykinin neuropeptide substance P (SP), which may result in the prevention of chemotherapy-induced nausea and vomiting (CINV). -
5-HT2A receptor agonist
Pimavanserin is a potent and selective 5-HT2A receptor inverse agonist with mean pIC50 of with 8.7 in the cell-based functional assay. -
FFA4/GPR120 agonist
GSK137647A is a selective FFA4 agonist, with pEC50 of 6.3, 6.2, and 6.1 for human, Mouse and Rat FFA4, respectively. -
5-HT1F antagonist
LY 334370 hydrochloride is a selective 5-HT1F receptor agonist (Ki values are 1.87, 16.4, > 100 (IC50)). CAS: 199673-74-0(LY 334370 hydrochloride); 182563-08-2 (LY 334370 Free Base) -
H4 receptor antagonist
JNJ-39758979 is histamine H4 receptor antagonists with a Ki of 12.5 nM. -
5-HT(2A) receptor agonist
Temanogrel, also known as APD791, is a highly selective 5-hydroxytryptamine2A receptor inverse agonist under development for the treatment of arterial thrombosis. -
opioid receptor antagonis
Bevenopran, also known as CB-5945, ADL-5945, MK-2402, OpRA III, is a peripherally selective μ- and δ-opioid receptor antagonist. - Neuronostatin-13 human is a 13-amino acid peptide hormone encoded by the somatostatin gene and plays an important role in the regulation of hormonal and cardiac function.
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OX2 receptor antagonist
TCS-OX2-29 is a selective OX2 receptor antagonist with IC50 value of 40 nM. CAS: 1610882-30-8 (HCl) 372523-75-6 (Free Base) -
IP (prostacyclin) receptor antagonist
RO-1138452 is a potent and selective IP (prostacyclin) receptor antagonist with high affinity for IP receptors. -
sigma1 receptor agonist
Anavex2-73 is a muscarinic/moderate sigma1 receptor agonist that alleviated the scopolamine- and dizocilpine-induced learning impairments. CAS: 195615-83-9 (Free base) 195615-84-0 (HCl) -
histamine H3 receptors agonist
S38093 is an inverse agonist at histamine H3 receptors. CAS: 862896-30-8 (Free base) 1222097-72-4 (HCl) -
CRTh2 receptor antagonist
Fevipiprant, also known as NVP-QAW039 or QAW039, is an oral active and potent CRTh2 receptor antagonist and potentially useful for asthma treatment. -
beta-adrenergic receptor antagonist
Nifenalol, also known as INPEA, is a new beta-adrenergic receptor antagonist. -
α-adrenoceptor agonist
Xylometazoline hydrochloride is an α-adrenoceptor agonist commonly used as nasal decongestant. -
alpha-adrenergic receptor agonist / MAO inhibitor
Amitraz, also known as Mitaban and Taktic, is an alpha-adrenergic receptor agonist and MAO inhibitor used as an insecticide in prevention of flea and tick infections. It prevents prostaglandin synthesis and may inhibit beta-cell insulin release. -
5-HT2 antagonist
Sarpogrelate hydrochloride (MCI-9042), a selective 5-HT2 antagonist, has been widely used as an anti-platelet agent for the treatment of PAD. -
D2DR and D4DR inhibitor
Loxapine Succinate is a D2DR and D4DR inhibitor and serotonergic receptor antagonist. Loxapine succinate is an antipsychotic agent used in schizophrenia. -
MT1 and MT2 receptor agonist
Tasimelteon is a melatonin MT1 and MT2 receptor agonist. -
β-adrenergic receptor antagonist
(R)-Atenolol is a beta blocker used to treat high blood pressure and chest pain (angina). It can also reduce the risk of death after a heart attack. -
β2AR agonist
Metaproterenol hemisulfate (Orciprenaline hemisulfate) is a direct-acting sympathomimetic and a β2-adrenergic receptor (β2AR) agonist with an IC50 of 68 nM. Metaproterenol hemisulfate also has anti-inflammatory activity. -
alpha-1 adrenergic agonist
Methoxamine Hydrochloride is an alpha-1 adrenergic agonist that causes prolonged peripheral vasoconstriction. -
Non-selective β antagonist
Oxprenolol is an orally bioavailable β-adrenergic receptor (β-AR) antagonist (Ki = 7.10 nM in a radioligand binding assay using rat heart tissue). It is non-selective and inhibits both β1- and β2-ARs (Kds = 2.09 and 1.35 nM in isolated rat heart and uterus, respectively). Oxprenolol is selective for β-ARs over serotonin (5-HT) receptors in rat sarcolemmal membrane preparations (IC50s = 4.13 and 23,300 nM, respectively), but it binds to 5-HT1A receptors in rat hippocampus and 5-HT1B in rat striatum (Kis = 94.2 and 642 nM, respectively). -
beta-Adrenergic agonist
Ractopamine HCl is a beta-Adrenergic agonist. It acts by being a full agonist at the TAAR1. -
H1 histamine receptor antagonist
Terfenadine ((??)-Terfenadine) is a potent open-channel blocker of hERG with an IC50 of 204 nM. Terfenadine, an H1 histamine receptor antagonist, acts as a potent apoptosis inducer in melanoma cells through modulation of Ca2+ homeostasis. Terfenadine induces ROS-dependent apoptosis, simultaneously activates Caspase-4, -2, -9 and induces p73, Noxa. - Misoprostol is a medication used to start labor, cause an abortion, prevent and treat stomach ulcers, and treat postpartum bleeding due to poor contraction of the uterus. For abortions it is often used with mifepristone or methotrexate. By itself effectiveness for this purpose is between 66% and 90%.
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5-HT3 receptor antagonist
Ondansetron hydrochloride is a serotonin 5-HT3 receptor antagonist. -
α1A-adrenoceptor antagonist
Nicergoline is an ergot derivative used to treat senile dementia and other disorders with vascular origins. It has been found to increase mental agility and enhance clarity and perception. It decreases vascular resistance and increases arterial blood flow in the brain, improving the utilization of oxygen and glucose by brain cells. It has similar vasoactive properties in other areas of the body, particularly the lungs. Nicergoline is used for vascular disorders such as cerebral thrombosis and atherosclerosis, arterial blockages in the limbs, Raynaud's disease, vascular migraines, and retinopathy. -
Histamine H1 receptor antagonist
Levocetirizine dihydrochloride is a L-isomer of cetirizine and histamine H1 receptor antagonist. It incrases levels of CD4+ CD25+ T cells and decreases levels of eosinophils, decreasing allergy symptoms. -
prostaglandin analogue
Tafluprost, also known as MK2452 and AFP-168, is a prostaglandin analogue used topically (as eye drops) to control the progression of glaucoma and in the management of ocular hypertension. -
non-peptide angiotensin II receptor antagonist
Fimasartan is a non-peptide angiotensin II receptor antagonist (ARB) used for the treatment of hypertension and heart failure. Through oral administration, fimasartan blocks angiotensin II receptor type 1 (AT1 receptors), reducing pro-hypertensive actions of angiotensin II, such as systemic vasoconstriction and water retention by the kidneys.
