Search Result
Results for "
dual antagonist
" in MedChemExpress (MCE) Product Catalog:
5
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-109593
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- HY-U00253
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- HY-A0013
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- HY-A0013A
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- HY-149096
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CXCR
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Others
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CCR7 antagonist 1 (30c) is a dual CXCR2 (IC50 of 11.02 μM) and CCR7 (IC50 of 0.43 μM) antagonist .
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- HY-109565
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ASTX660
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IAP
Apoptosis
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Cancer
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Tolinapant (ASTX660) is an orally bioavailable dual antagonist of cellular inhibitor of apoptosis protein (cIAP) and X-linked inhibitor of apoptosis protein (XIAP).
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- HY-145862
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- HY-17621
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- HY-135500
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Endothelin Receptor
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Endocrinology
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ACT-373898 is an inactive carboxylic acid metabolite of Macitentan. Macitentan is an orally active, non-peptide dual ETA and ETB (endothelin receptor) antagonist .
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- HY-145706
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Adenosine Receptor
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Neurological Disease
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A2A/A1 AR antagonist-1 (compound 1a) is dual potent A2A/A1 AR antagonist with Kis of 5.58 and 24.2 nM, respectively. A2A/A1 AR antagonist-1 has the potential for the research of ischemic stroke .
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- HY-101638
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(±)-FK1052
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5-HT Receptor
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Neurological Disease
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(±)-Fabesetron hydrochloride ((±)-FK1052) is the racemate of Fabesetron hydrochloride, which is a potent 5-HT3 and 5-HT4 receptor dual antagonist .
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- HY-19205A
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Lipoxygenase
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Inflammation/Immunology
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CMI-392 is a dual 5-lipoxygenese inhibitor and platelet-activating factor (PAF) receptor antagonist with IC50s of 100 and 10 nM, respectively.
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- HY-U00072
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- HY-19519A
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DF 2156A
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CXCR
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Infection
Inflammation/Immunology
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Ladarixin sodium (DF 2156A) is an orally active, allosteric non-competitive and dual CXCR1 and CXCR2 antagonist. Ladarixin sodium can be used for the research of COPD and asthma .
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- HY-115724
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5-HT Receptor
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Neurological Disease
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FPPQ is a dual-acting 5-HT3 (Ki = 0.9 nM) and 5-HT6 (Ki = 3 nM) receptor antagonist with antipsychotic and procognitive properties.
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- HY-157019
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Ephrin Receptor
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Cancer
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UniPR1447 is Dual EphA2 and EphB2 antagonist, with an IC50 of 6.6 μM for EphA2−ephrin-A1 binding .
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- HY-153333
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Adenosine Receptor
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Cardiovascular Disease
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A1/A3 AR antagonist 3 is an A1R/A3R dual antagonist with high affinity at low-micromolar to low-nanomolar. A1/A3 AR antagonist 3 can be used for the research of chronic heart diseases .
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- HY-19519
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DF 2156A free base
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Ladarixin (DF 2156A free base) is an orally active, allosteric non-competitive and dual CXCR1 and CXCR2 antagonist. Ladarixin can be used for the research of COPD and asthma .
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- HY-P99420
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ALPN-101
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CD28
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Inflammation/Immunology
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Acazicolcept (ALPN-101), an Fc fusion protein, is a dual inducible T cell costimulator (ICOS)/CD28 antagonist. Acazicolcept has anti-inflammatory activities .
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- HY-115417
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- HY-115871
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- HY-147541
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Adenosine Receptor
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Inflammation/Immunology
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A2A/A3 AR antagonist-1 (compound 23) is a dual A2A/A3 adenosine receptor (AR) fluorescent ligand, with Kis of 90 nM and 31.8 nM for hA2A AR and hA3 AR, respectively .
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- HY-146034
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NOD-like Receptor (NLR)
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Inflammation/Immunology
Cancer
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NOD1/2 antagonist-1 (compound 36b) is a potent NOD1/2 (nucleotide-binding
oligomerization domain-like receptor 1/2) dual antagonist, with IC50 values of 1.13 (NOD1) and 0.77 μM (NOD2), respectively. NOD1/2 antagonist-1 has a acceptable T1/2 (67.6 min). NOD1/2 antagonist-1 (compound 36b) can improve the antitumor efficacy of Paclitaxel (PTX) .
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- HY-14184
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- HY-141411A
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(S)-MRI-1867
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Cannabinoid Receptor
NO Synthase
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Metabolic Disease
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Zevaquenabant ((S)-MRI-1867) is a peripherally restricted, orally bioavailable dual cannabinoid CB1 receptor and inducible NOS antagonist. Zevaquenabant ameliorates obesity-induced chronic kidney disease (CKD) .
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- HY-148533
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mAChR
Adrenergic Receptor
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Neurological Disease
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β2AR agonist /M-receptor antagonist-1 is a potent dual muscarinic antagonist/beta 2 agonist (MABA). β2AR agonist /M-receptor antagonist-1 potently relaxes either Carbachol (HY-B1208)-induced contraction, in the absence (MABA) or presence of Propranolol (M3; HY-B1208), or Histamine (HY-B1204)-induced contraction (β2) .
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- HY-17621S
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- HY-14882A
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TAK-652 Mesylate; TBR-652 Mesylate
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CCR
HIV
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Infection
Inflammation/Immunology
Endocrinology
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Cenicriviroc Mesylate (TAK-652 Mesylate) is a dual CCR2/CCR5 antagonist, also inhibits both HIV-1 and HIV-2, and displays potent anti-inflammatory and antiinfective activity.
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- HY-116120
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- HY-10900
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- HY-B0358A
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Calcium Channel
Sodium Channel
Dopamine Receptor
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Neurological Disease
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Flunarizine dihydrochloride is a potent dual Na +/Ca 2+ channel (T-type) blocker. Flunarizine dihydrochloride is a D2 dopamine receptor antagonist. Flunarizine dihydrochloride shows anticonvulsive and antimigraine activity, and peripheral vasodilator effects .
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- HY-14184A
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Endothelin Receptor
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Cardiovascular Disease
Endocrinology
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Macitentan n-butyl analogue is a n-butyl analogue of Macitentan. Macitentan is an orally active, non-peptide dual endothelin ETA and ETB receptor antagonist for the potential treatment of idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH).
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- HY-114412A
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- HY-B0358
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Flunarizine is a potent dual Na +/Ca 2+ channel (T-type) blocker. Flunarizine is a D2 dopamine receptor antagonist. Flunarizine shows anticonvulsive and antimigraine activity, and peripheral vasodilator effects .
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- HY-15895
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ACT-132577
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Endothelin Receptor
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Cardiovascular Disease
Endocrinology
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Aprocitentan (ACT-132577) is the major and pharmacologically active metabolite of Macitentan. Aprocitentan is dual ETA/ETB antagonist with IC50s of 3.4 nM and 987 nM, and pA2 valus of 6.7 and 5.5, respectively .
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- HY-114412
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- HY-14882
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TAK-652; TBR-652
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CCR
HIV
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Infection
Endocrinology
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Cenicriviroc (TAK-652) is an orally active, dual CCR2/CCR5 antagonist, also inhibits both HIV-1 and HIV-2, and displays potent anti-inflammatory and antiinfective activity .
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- HY-14184S
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- HY-124290
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AJM300
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Integrin
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Inflammation/Immunology
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Carotegrast methyl (AJM300) is an orally active and selective α4 integrin antagonist. HCA2969, an active metabolite of Carotegrast methyl, is a specific and dual α4β1/α4β7 integrin antagonist. Carotegrast methyl prevents the development of colitis in mice .
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- HY-13511A
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UR-12592 Fumarate
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Histamine Receptor
Autophagy
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Inflammation/Immunology
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Rupatadine (UR-12592) Fumarate is a potent, orally active and long-lasting dual PAF/H1 antagonist, with Kis of 0.55 μM and 0.1 μM, respectively. Rupatadine Fumarate can be used for the research of allergic rhinitis and urticaria .
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- HY-129393
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AB928
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Adenosine Receptor
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Inflammation/Immunology
Cancer
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Etrumadenant (AB928) is an orally bioavailable, selective dual adenosine receptor (A2aR/A2bR) antagonist. Etrumadenant relieves adenosine-mediated immune suppression. Etrumadenant has immunomodulatory and antitumor activities .
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- HY-114953
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Angiotensin Receptor
Endothelin Receptor
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Cardiovascular Disease
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BMS-248360 is a potent and orally active dual antagonist of both angiotensin II receptor (AT1) and endothelin A (ETA) receptor, with Kis of 10 nM and 1.9 nM for hAT1 and hETA receptor, respectively. BMS-248360 displays hypertensive effects .
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- HY-13511
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UR-12592
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Histamine Receptor
Autophagy
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Inflammation/Immunology
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Rupatadine (UR-12592) is a potent, orally active and long-lasting dual PAF/H1 antagonist, with Kis of 0.55 μM and 0.1 μM, respectively. Rupatadine can be used for the research of allergic rhinitis and urticaria .
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- HY-14189
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R-411
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Integrin
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Inflammation/Immunology
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Valategrast hydrochloride (R-411) is a potent integrin α4β1 (VLA-4) and α4β7 dual antagonist. Valategrast hydrochloride has the potential for Chronic obstructive pulmonary disease (COPD) and asthma treatment .
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- HY-146478
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Adenosine Receptor
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Neurological Disease
Inflammation/Immunology
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A1/A3 AR antagonist 1 (compound 10) is a potent adenosine 1 (A1) and adenosine 3 (A3) receptor dual antagonist with Kis of 36.7 nM, 25.4 nM and 1.47 nM for human A1, human A3 and rat A1, respectively. A1/A3 AR antagonist 1 can be used for researching kidney failure, inflammatory pulmonary diseases, and Alzheimer’s disease .
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- HY-158057
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Adenosine Receptor
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Cancer
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A2AR/A2BR antagonist 1 (compound 7ai) has a dual antagonistic effect on A2AR/A2BR, with the IC50 values of 11.2 nM and 6.4 nM for A2AR and A2BR, respectively. A2AR/A2BR antagonist 1 promotes T cell-mediated cancer cell death .
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- HY-13511AS
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- HY-109133
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BAY 1753011
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Vasopressin Receptor
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Neurological Disease
Metabolic Disease
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Pecavaptan is an orally active and dual antagonist of V1a/V2 receptor (Ki=0.5 nM and 0.6 nM for human, respectively). Pecavaptan promotes an increase in urine production, which reduces the associated symptoms of water retention and edema .
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- HY-15895S
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- HY-139559
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ORN-0829; TS-142
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Orexin Receptor (OX Receptor)
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Neurological Disease
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Vornorexant (ORN-0829; TS-142) is a potent dual OX1R and OX2R antagonist with IC50 values of 1.05 nM and 1.27 nM, respectively. Vornorexant exhibits potent sleep-promoting effects in vivo and can be used for insomnia research research.
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- HY-149454
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P2Y Receptor
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Cancer
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P2Y1/P2Y12 antagonist-1 (compound 24w) is an orally available dual inhibitor of P2Y1 and P2Y12 with antiplatelet activity. P2Y1/P2Y12 antagonist-1 inhibits ADP-induced platelet aggregation in rabbit plasma with an IC50 of 4.23 μM. P2Y1/P2Y12 antagonist-1 exhibits potent inhibitory effects in rat thrombosis model.
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- HY-146486
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P2Y Receptor
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Inflammation/Immunology
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P2Y2R/GPR17 antagonist 1 (Compound 14m) is a dual P2Y2R and GPR17 antagonist with IC50 values of 3.17 µM and 1.67 µM against P2Y2R and GPR17, respectively. P2Y2R/GPR17 antagonist 1 shows excellent metabolic stability in human liver microsomes .
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- HY-161311
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- HY-10805S
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- HY-14190
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R-411 free base
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Integrin
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Inflammation/Immunology
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Valategrast (R-411 free base) is a potent and orally active integrin α4β1 (VLA-4) and α4β7 dual antagonist. Valategrast has the potential for Chronic obstructive pulmonary disease (COPD) and asthma treatment .
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- HY-14973
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AMG 853
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Prostaglandin Receptor
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Inflammation/Immunology
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Vidupiprant (AMG 853) is a phenylacetic acid derivative. Vidupiprant is a potent and orally active CRTH2 (DP2) and prostanoid D receptor (DP or DP1) dual antagonist with IC50s of 3 nM and 4 nM in buffer, and 8 nM and 35 nM in human plasma, respectively. Vidupiprant has the potential for asthma treatment .
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- HY-109067
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VVZ-149
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GlyT
5-HT Receptor
P2X Receptor
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Neurological Disease
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Opiranserin (VVZ-149), a non-opioid and non-NSAID analgesic candidate, is a dual antagonist of glycine transporter type 2 (GlyT2) and serotonin receptor 2A (5HT2A), with IC50s of 0.86 and 1.3 μM, respectively. Opiranserin shows antagonistic activity on rP2X3 (IC50=0.87 μM). Opiranserin is development as an injectable agent for the treatment of postoperative pain .
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- HY-109067A
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VVZ-149 hydrochloride
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GlyT
5-HT Receptor
P2X Receptor
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Neurological Disease
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Opiranserin (VVZ-149) hydrochloride, a non-opioid and non-NSAID analgesic candidate, is a dual antagonist of glycine transporter type 2 (GlyT2) and serotonin receptor 2A (5HT2A), with IC50s of 0.86 and 1.3 μM, respectively. Opiranserin hydrochloride shows antagonistic activity on rP2X3 (IC50=0.87 μM). Opiranserin hydrochloride is development as an injectable agent for the treatment of postoperative pain .
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- HY-134189
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Opioid Receptor
Sigma Receptor
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Neurological Disease
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EST73502 is a selective, orally active and blood-brain barrier (BBB) penetrant dual μ-opioid receptor (MOR) agonist and σ1 receptor (σ1R) antagonist, with Kis of 64 nM and 118 nM for MOR and σ1R, respectively. EST73502 has antinociceptive activity .
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- HY-101834
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Orexin Receptor (OX Receptor)
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Others
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ACT-462206 is an orally active and potent dual Orexin 1/Orexin 2 receptor antagonist with IC50s of 60 nM (Orexin 1) and 11 nM (Orexin 2), respectively. ACT-462206 exhibits brain penetration properties, and can be used for insomnia, stress/anxiety-related disorders and addiction research .
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- HY-148088
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Adenosine Receptor
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Cancer
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M1069 is a selective and orall active, dual A2A/A2B adenosine receptor antagonist with a selectivity of >100 fold against the A1 and A3 receptors. M1069 counteracts immune-suppressive mechanisms of adenosine, and exhibits anti-tumor activity .
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- HY-134189A
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Sigma Receptor
Opioid Receptor
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Neurological Disease
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EST73502 monohydrochloride is a selective, orally active and blood-brain barrier (BBB) penetrant dual μ-opioid receptor (MOR) agonist and σ1 receptor (σ1R) antagonist, with Kis of 64 nM and 118 nM for MOR and σ1R, respectively. EST73502 monohydrochloride has antinociceptive activity .
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- HY-115871A
-
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Others
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Others
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(Rac)-PDE4-IN-4 is the diastereomer mixture of PDE4-IN-4 (HY-115871). PDE4-IN-4 is a dual M3 (pIC50 = 10.2) antagonist-PDE4 (pIC50 = 8.8) inhibitor for the inhaled research of pulmonary diseases .
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- HY-13511AR
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UR-12592 Fumarate (Standard)
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Histamine Receptor
Autophagy
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Inflammation/Immunology
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Rupatadine (Fumarate) (Standard) is the analytical standard of Rupatadine (Fumarate). This product is intended for research and analytical applications. Rupatadine (UR-12592) Fumarate is a potent, orally active and long-lasting dual PAF/H1 antagonist, with Kis of 0.55 μM and 0.1 μM, respectively. Rupatadine Fumarate can be used for the research of allergic rhinitis and urticaria .
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- HY-155615
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Sigma Receptor
Histamine Receptor
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Neurological Disease
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KSK67 is a high-affinity dual sigma-2 and histamine H3 receptor antagonist, with Kis of 3.2, 1531, 101 nM for H3 receptor, sigma-1, sigma-2 receptor respectively. KSK67 can be used for research of nociceptive and neuropathic pain .
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- HY-148088A
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Adenosine Receptor
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Cancer
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M1069 (free base) is a selective and orall active, dual A2A/A2B adenosine receptor antagonist with a selectivity of >100 fold against the A1 and A3 receptors. M1069 (free base) counteracts immune-suppressive mechanisms of adenosine, and exhibits anti-tumor activity .
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- HY-139230
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Cannabinoid Receptor
PPAR
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Metabolic Disease
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OLHHA is a dual CB1 receptor antagonist and PPARα agonist. OLHHA also is a alcohol intake inhibitor with an EC50 value of 0.2 mg/kg. OLHHA reduces both hepatic lipid accumulation and circulating triglyceride levels. OLHHA shows anti-steatotic activity and has the potential for the research of non-alcoholic fatty liver disease (NAFLD) .
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- HY-16780
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ONO-6950
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Leukotriene Receptor
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Inflammation/Immunology
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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. Gemilukast is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-135390
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Ro 64-1056
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Drug Metabolite
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Cardiovascular Disease
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Hydroxy desmethyl Bosentan (Ro 64-105) is a Bosentan metabolism produced by the cytochrome P450 enzymes CYP2C9 and CYP3A4 in the liver . Bosentan is a competitive and dual antagonist of endothelin-1 (ET) for the ETA and ETB receptors with Ki of 4.7 nM and 95 nM in human SMC, respectively. Bosentan can be used in treatment of pulmonary arterial hypertension .
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- HY-W104304
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Vasopressin Receptor
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Cardiovascular Disease
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2-(3-Trifluoromethylphenyl)glycine hydrochloride is a precursor of substituted 2-acetamido-5-aryl-l, 2,4-triazolones. Substituted 2-acetamido-5-aryl-l, 2,4-triazolones are dual V1a/V2 receptor antagonists and can be used in cardiovascular disease research .
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- HY-14485
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P2X Receptor
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Neurological Disease
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Ro-51 is a potent and selective dual P2X3/P2X2/3 antagonist, with IC50 of 2 nM and 5 nM for P2X3 and P2X2/3, respectively. Ro-51 can be used for the research for pain .
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- HY-138542
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Integrin
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Inflammation/Immunology
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RO0270608, the active metabolite of R411, is a dual alpha4beta1-alpha4beta7 (α4β1/α4β7) integrin antagonist. Antiinflammatory activity .
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- HY-15770
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Integrin
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Inflammation/Immunology
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TR-14035 is a orally active dual α4β7/α4β1 integrin antagonist, with IC50 s of 7 nM and 87 nM for α4β7 and α4β1, respectively. TR-14035 can be used for the research of inflammation and autoimmune diseases .
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- HY-10805
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ACT 078573
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Orexin Receptor (OX Receptor)
Calcium Channel
Caspase
Apoptosis
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Neurological Disease
Endocrinology
Cancer
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Almorexant (ACT 078573) is an orally active, potent and competitive dual orexin receptor antagonist, with Kd values of 1.3 nM (OX1) and 0.17 nM (OX2), respectively. Almorexant reversibly blocks signaling of orexin-A and orexin-B peptides. Almorexant totally blocked the intracellular Ca 2+ signal pathway. Almorexant stimulates caspase-3 activity in AsPC-1 cells and induces apoptosis .
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- HY-10805A
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ACT 078573 hydrochloride
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Orexin Receptor (OX Receptor)
Calcium Channel
Caspase
Apoptosis
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Neurological Disease
Endocrinology
Cancer
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Almorexant (ACT 078573) hydrochloride is an orally active, potent and competitive dual orexin receptor antagonist, with Kd values of 1.3 nM (OX1) and 0.17 nM (OX2), respectively. Almorexant hydrochloride reversibly blocks signaling of orexin-A and orexin-B peptides. Almorexant hydrochloride totally blocked the intracellular Ca 2+ signal pathway. Almorexant hydrochloride stimulates caspase-3 activity in AsPC-1 cells and induces apoptosis .
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- HY-117621
-
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CCR
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Metabolic Disease
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PF-0463481 is a potent and orally active dual CCR2/CCR5 antagonist with comparable human and rodent CCR2 potency (rat IC50=20.8 nM), and displays 10-20 fold less rodent CCR5 potency (rat IC50=470 nM). PF-0463481 is safe and well-tolerated and has the potential for the study of diabetic nephropathy .
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- HY-111313
-
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Cholecystokinin Receptor
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Metabolic Disease
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JNJ-26070109 is a high-affinity, competitive, orally bioactive, and selective cholecystokinin 2 (CCK2) receptor antagonist with good pharmacokinetic properties, with pKis of 8.49, 7.99, and 7.70 for human, rat, and dog CCK2 receptors, respectively. The dual function of CCK2 receptors in regulating gastric acid secretion and growth of the gastrointestinal mucosa make this an attractive and novel target for the research of gastroesophageal reflux disease .
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- HY-123205
-
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Histamine Receptor
P2X Receptor
5-HT Receptor
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Inflammation/Immunology
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Oxatomide is a potent and orally active dual H1-histamine receptor and P2X7 receptor antagonist with antihistamine and anti-allergic activity. Oxatomide almost completely blocks the ATP-induced current in human P2X7 receptors (IC50 of 0.95 μM). Oxatomide inhibits ATP-induced Ca 2+ influx with an IC50 value of 0.43 μM and also inhibits serotonin .
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- HY-117621A
-
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CCR
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Metabolic Disease
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PF-0463481 succinate is a potent and orally active dual CCR2/CCR5 antagonist with comparable human and rodent CCR2 potency (rat IC50=20.8 nM), and displays 10-20 fold less rodent CCR5 potency (rat IC50=470 nM). PF-0463481 succinate is safe and well-tolerated and has the potential for the study of diabetic nephropathy .
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- HY-155614
-
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Sigma Receptor
Histamine Receptor
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Neurological Disease
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KSK68 is a high-affinity dual sigma-1 and histamine H3 receptor antagonist, with Kis of 7.7, 3.6, 22.4 nM for H3 receptor, sigma-1, sigma-2 receptor respectively. KSK68 has negligible affinity at the other histamine receptor subtypes. KSK68 can be used for research of nociceptive and neuropathic pain .
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- HY-146076
-
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5-HT Receptor
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Neurological Disease
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5-HT6/5-HT2A receptor ligand-1 (compound 33) is a dual 5-HT6/5-HT2A receptor antagonist, with a Ki of 2 nM and 11 nM, respectively. 5-HT6/5-HT2A receptor ligand-1 has the potential for neurological and psychiatric disorders research .
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- HY-146077
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5-HT Receptor
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Neurological Disease
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5-HT6/5-HT2A receptor ligand-2 (compound 42) is a brain-penetrant dual 5-HT6/5-HT2A receptor antagonist, with a Ki of 25 nM and 32 nM, respectively. 5-HT6/5-HT2A receptor ligand-2 shows pro-cognitive properties .
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- HY-12706
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- HY-D0976
-
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P2X Receptor
HIV
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Infection
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NF279 is a potent selective and reversible P2X1 receptor antagonist, with an IC50 of 19 nM. NF279 displays good selectivity over P2X2, P2X3 (IC50=1.62 μM), P2X4 (IC50>300 μM). NF279 is a dual HIV-1 coreceptor inhibitor that interferes with the functional engagement of CCR5 and CXCR4 by Env .
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- HY-163065
-
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Opioid Receptor
Sigma Receptor
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Neurological Disease
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σ1 Receptor/μ Opioid receptor modulator 2 (compound 4x) is a dual μOR agonist/σ1R antagonist, and displays picomolar μOR agonism activity (EC50: 0.6 ± 0.2 nM) and good σ1R inhibitory activity (Ki: 363.7 ± 5.6 nM). σ1 Receptor/μ Opioid receptor modulator 2 exhibits robust analgesic effects in various pain models .
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- HY-120802
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AZD-8871; LAS191351
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mAChR
Adrenergic Receptor
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Inflammation/Immunology
|
Navafenterol (AZD-8871) is an inhaled dual-acting, potent, selective, and long-lasting M3-antagonist/β2-agonist (MABA) with long-lasting effects and favorable safety profile. The pIC50 is 9.5 for human M3 receptor, and the pEC50 is 9.5 for β2-adrenoceptor. Navafenterol can be used for the research of chronic obstructive pulmonary disease (COPD). Bronchoprotective and antisialagogue effects. Favorable cardiovascular profile .
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- HY-12927
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SX-517 is a dual CXCR2/1 antagonist, containing boronic acid. SX-517 inhibits CXCL1-induced Ca 2+ flux (IC50=38 nM), and antagonizes CXCL8-induced [(35)S]GTPγS binding (IC50=60 nM) and ERK1/2 phosphorylation. SX-517 has significant ability for inflammation suppression, in both humanized polymorphonuclear (PMN) cells and in murine model .
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- HY-120802A
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AZD-8871 saccharinate; LAS191351 saccharinate
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mAChR
Adrenergic Receptor
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Infection
Inflammation/Immunology
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Navafenterol (AZD-8871) saccharinate is an inhaled dual-acting, potent, selective, and long-lasting M3-antagonist/β2-agonist (MABA) with long-lasting effects and favorable safety profile. The pIC50 is 9.5 for human M3 receptor, and the pEC50 is 9.5 for β2-adrenoceptor. Navafenterol saccharinate can be used for the research of chronic obstructive pulmonary disease (COPD). Bronchoprotective and antisialagogue effects. Favorable cardiovascular profile .
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Product Name |
Target |
Research Area |
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- HY-W104304
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Vasopressin Receptor
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Cardiovascular Disease
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2-(3-Trifluoromethylphenyl)glycine hydrochloride is a precursor of substituted 2-acetamido-5-aryl-l, 2,4-triazolones. Substituted 2-acetamido-5-aryl-l, 2,4-triazolones are dual V1a/V2 receptor antagonists and can be used in cardiovascular disease research .
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Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P99420
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ALPN-101
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CD28
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Inflammation/Immunology
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Acazicolcept (ALPN-101), an Fc fusion protein, is a dual inducible T cell costimulator (ICOS)/CD28 antagonist. Acazicolcept has anti-inflammatory activities .
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Cat. No. |
Product Name |
Chemical Structure |
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- HY-14184S
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Macitentan-d4 is a deuterium labeled Sulfamethoxazole. Macitentan is an orally active, non-peptide dual ETA and ETB (endothelin) receptor antagonist. Macitentan has the potential for idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH)[1].
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- HY-15895S
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Aprocitentan-d4 is a deuterium labeled Aprocitentan. Aprocitentan is a major and pharmacologically active metabolite of Macitentan. Aprocitentan is dual ETA/ETB antagonist with IC50s of 3.4 nM and 987 nM, and pA2 valus of 6.7 and 5.5, respectively[1].
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- HY-17621S
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Sparsentan-d5 is deuterium labeled Sparsentan. 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[1].
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- HY-13511AS
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Rupatadine-d4 (fumarate) is a deuterium labeled Rupatadine fumarate. Rupatadine Fumarate (UR-12592 Fumarate) is a potent dual PAF/H1 antagonist with Ki of 0.55/0.1 μM(rabbit platelet membranes/guinea pig cerebellum membranes)[1][2][3].
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- HY-10805S
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Almorexant- 13C,d3 is the 13C- and deuterium labeled Almorexant. Almorexant (ACT 078573) 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, respectively.
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