dual antagonist

BMS-813160 is the first dual CCR2/CCR5 antagonist to enter Clinical development for cardiovascular.

Cyclodrine hydrochloride is a dual cholinergic muscarinic receptor (mAChR) and nicotinic receptor (nAChR) antagonist that can be used in the study of neurologically related diseases.

Oxatomide (Oxatomida) is a potent and orally active dual H1 histamine receptor and P2X7 receptor antagonist with antihistamine and antiallergic activity.Oxatomide can be used to block ATP-induced currents in the human P2X7 receptor with an IC50 value of 0.95 μM.Oxatomide has an inhibitory effect on ATP-induced Ca2+ inward currents with an IC50 value of 0.43 μM.Oxatomide inhibits 5-hydroxytryptamine. Oxatomide inhibits 5-hydroxytryptamine with an IC50 of 0.43 μM.Oxatomide is used in the treatment of immune system diseases and in the study of hypersensitivity reactions.

RO0270608, the active metabolite of R411, is an orally active dual α4β1/α4β7 integrin antagonist with anti-inflammatory properties, useful for studying allergic inflammatory responses.

Viloxazine (Viloxazin) (Viloxazin) is a dual-action compound that functions as a norepinephrine reuptake inhibitor and exhibits potent agonistic activity towards 5-HT 2C receptors while acting as an antagonist for 5-HT 2B receptors, with respective potency values of EC 50 = 32 μM and IC 50 = 27 μM. Its primary mechanism of action involves the modulation of serotonergic and noradrenergic pathways. Viloxazine is commonly employed in depression research [1] [2].

5-HT6/7 antagonist 1 is a dual 5-HT6/7/2A and D2 receptor antagonist used in the study of dementia and Alzheimer's disease.

mTOR/HDAC-IN-1 (Compound 50) is a dual inhibitor of mTOR and HDAC, with IC50 values of 0.49 nM and 0.91 nM, respectively, holding potential as an anti-cancer agent [1].

β2AR/M-receptor agonist-2 is a dual-function compound acting as a muscarinic antagonist and β2 adrenoceptor agonist (MABA). It demonstrates significant activity towards the β2 adrenoceptor with an EC50 of 3.7 nM and exhibits affinity for the human cloned M3 receptor with a Ki of 0.73 nM. This potent bronchodilator holds potential for research in chronic obstructive pulmonary disease (COPD) treatment.

KSK68 is a potent dual sigma-1 and histamine H3 receptor antagonist with potential analgesic activity and high affinity for H3 receptors, sigma-1, sigma-2 receptors.KSK68 can be used in the study of pain related diseases.

Rupatadine Fumarate (Rinialer) (UR-12592 Fumarate) is a potent dual PAF/H1 antagonist with Ki of 0.55/0.1 uM.

Bosentan hydrate (Ro 47-0203) is a competitive and dual antagonist of endothelin-1 at the endothelin-A (ET-A) and endothelin-B (ET-B) receptors.

SCH-37370 is an effective and orally active dual antagonist of platelet-activating factor and histamine. Sch 37370 blocks the binding of [3H]pyrilamine to histamine-H1 receptors in rat brain membranes. Sch 37370 selectively inhibits PAF-induced aggregation of human platelets (IC50 : 0.6 mM) and also competes with PAF binding to specific sites in membrane preparations from human lungs (IC50 : 1.2 mM).

Aprocitentan D4 (ACT-132577 D4) is a deuterium-labeled Aprocitentan. Aprocitentan is a major and pharmacologically active metabolite of Macitentan. Aprocitentan is a dual ETA ETB antagonist (IC50s: 3.4 nM and 987 nM; pA2s: 6.7 and 5.5).

Cenicriviroc Mesylate is a dual CCR2/CCR5 antagonist, also inhibits both HIV-1 and HIV-2 with anti-inflammatory and antiinfective activity.

CMI-392 is a dual inhibitor of 5-lipoxygenase and a receptor antagonist for platelet-activating factor (PAF) with IC50 values of 100 nM and 10 nM, respectively.

FK1052 hydrochloride is a potent 5-HT3 and 5-HT4 receptor dual antagonist.

Ziprasidone, an antipsychotic agent, functions as a dual antagonist of 5-HT (serotonin) and dopamine receptors. Keto Ziprasidone represents an impurity found within Ziprasidone.

KP496 is a selective, dual antagonist for the Thromboxane A2 receptor (TP) and the Leukotriene D4 receptor (cysLT1).

Macitentan-d4 (ACT-064992 D4) is a deuterated substitute for Macitentan and can be used as a dual antagonist of the non-peptides ETA and ETB (endothelin receptor).Macitentan-d4 is less toxic than Macitentan, has a longer half-life, and can be used to study endothelin receptor-mediated diseases.

Macitentan n-butyl analogue, a derivative of Macitentan, functions as an orally active dual antagonist targeting both endothelin ETA and ETB receptors. This compound shows promise for treating idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH), leveraging its non-peptide structure for potential therapeutic applications.

PF-0463481 succinate is a potent and orally active dual antagonist of CCR2/CCR5, exhibiting comparable human and rodent CCR2 potency with an IC50 of 20.8 nM.

PF-0463481 is safe and well-tolerated and has the potential for the study of diabetic nephropathy. PF-0463481 is an effective and orally active dual CCR2/CCR5 antagonist. It also has comparable human and rodent CCR2 potency (rat IC50=20.8 nM). PF-0463481

(4E)-SUN9221 is a potent dual α1-adrenergic receptor and 5-HT2 receptor antagonist, exhibiting antihypertensive and antiplatelet aggregation activities in hypertensive rats.

TD-0212 is an orally active dual pharmacology antagonist of angiotensin II type 1 receptor (AT1) and inhibitor of neprilysin (NEP)(pKi of 8.9 for AT1 and a pIC50 of 9.2 for NEP).