Search Result
Results for "
dual antagonist
" in MedChemExpress (MCE) Product Catalog:
7
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-109593
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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-U00253
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- HY-A0013A
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- HY-A0013
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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-17621
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- HY-113555
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- HY-145862
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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-173491
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CXCR
CCR
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Inflammation/Immunology
Cancer
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CXCR2/CCR7 antagonist-1 (compound 6) is a potent CXCR2 and CCR7 dual antagonist with IC50s of 0.0046 and 0.0014 μM, respectively. CXCR2/CCR7 antagonist-1 can be used in the study of cancer metastasis and autoimmune diseases .
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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-19205A
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LDP-392
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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-19880
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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-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-19519A
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DF 2156A
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CXCR
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Infection
Inflammation/Immunology
Cancer
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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-U00072
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- HY-78096
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Endogenous Metabolite
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Metabolic Disease
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O-Deshydroxyethyl bosentan is a metabolite of Bosentan (HY-A0013), which is a competitive and dual antagonist of endothelin-1 (ET) for the ETA and ETB receptors .
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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-101638A
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(±)-FK1052 free base
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5-HT Receptor
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Neurological Disease
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(±)-Fabesetron ((±)-FK1052 free base) is the racemate of Fabesetron, which is a potent 5-HT3 and 5-HT4 receptor dual antagonist .
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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-158318
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DNA/RNA Synthesis
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Cancer
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NUDT5/14 antagonist 1 (Compound 9) is a selective, dual antagonist for nucleotide diphosphate kinase NUDT5 and NUDT14, with IC50 of 0.27 and 0.16 μM, respectively. NUDT5/14 antagonist 1 binds to Bruton’s tyrosine kinase (BTK) with an IC50 of 0.377 μM .
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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-117965
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-
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- HY-100570
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-
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- HY-19519
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DF 2156A free base
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CXCR
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Inflammation/Immunology
Cancer
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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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-
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- HY-101260
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-
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- HY-115417
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-
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- HY-115871
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-
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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-170951
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Androgen Receptor
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Cancer
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AR antagonist 10 (Compound Y5) is potent and orally active androgen receptor (AR) antagonist with an IC50 of 0.04 μM. AR antagonist 10 demonstrates dual mechanisms of action, antagonizes AR by disrupting AR dimerization, and induces AR degradation via the ubiquitin-proteasome pathway. AR antagonist 10 exhibits excellent activity against variant drug-resistant AR mutants. AR antagonist 10 effectively suppresses the tumor growth of the LNCaP xenograft. AR antagonist 10 is potential to be used for drug-resistant prostate cancer .
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- HY-17621S
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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-14184
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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-A0013AR
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Endothelin Receptor
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Cardiovascular Disease
Endocrinology
Cancer
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Bosentan (hydrate) (Standard) is the analytical standard of Bosentan (hydrate). This product is intended for research and analytical applications. Bosentan hydrate 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.
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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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-
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- HY-10900
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-
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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-131479A
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Drug Metabolite
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Neurological Disease
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Threo-dihydrobupropion is a major metabolite of Bupropion, formed via oxidation and reduction exhibit pharmacological activity. Bupropion, a dual dopamine-norepinephrine uptake inhibitor and a nicotine receptor antagonist, is widely used in the management of depression and as a smoking cessation aid .
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- HY-B0358
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-
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- HY-114412A
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- HY-B0358A
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- HY-114412
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- HY-P990706
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ALPN-303
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TNF Receptor
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Inflammation/Immunology
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Povetacicept (ALPN-303), an Fc fusion protein of an engineered TACI domain, is a dual APRIL/BAFF antagonist. Povetacicept modulates B lymphocytes and pathogenic autoantibodies for the study of Lupus and other B cell-related autoimmune diseases .
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- HY-14184S
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- HY-119658
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INCB10820
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CCR
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Inflammation/Immunology
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PF-4178903 (INCB10820) is an orally active, potent dual CCR2 and CCR5 antagonist with IC50 values of 3 nM and 5.3 nM, respectively. PF-4178903 is promising for research of chronic inflammatory and autoimmune diseases .
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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-124290A
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AJM300 hydrochloride
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Integrin
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Inflammation/Immunology
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Carotegrast methyl (AJM300) hydrochloride is an orally active and selective α4 integrin antagonist. HCA2969, an active metabolite of Carotegrast methyl hydrochloride, is a specific and dual α4β1/α4β7 integrin antagonist. Carotegrast methyl hydrochloride prevents the development of colitis in mice .
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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-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-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-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-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-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-168742
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Vasopressin Receptor
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Neurological Disease
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V1a/V2 antagonist 1 (Compound 18j) is an orally active dual V1a and V2 receptor antagonist with high binding affinity for both receptors (Ki: 0.13 nM for hV1a, 0.53 nM for hV2 and 0.5 nM for mV1a; IC50: 2.2 nM for hV1a). V1a/V2 antagonist 1 inhibits Oxytocin (HY-17571)-induced scratching behavior in mice .
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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-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-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 an orally active dual ETA/ETB antagonist with IC50s of 3.4 nM and 987 nM, and pA2 valus of 6.7 and 5.5, respectively. Aprocitentan is an antihypertensive agent .
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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-129808
-
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LPL Receptor
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Cardiovascular Disease
Cancer
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VPC12249 is a competitive dual LPA1/LPA3 antagonist with Ki values of 137nM and 428 nM, respectively. VPC12249 inhibits calcium mobilization in HEK293T cells with a Ki value of ~130 nM. VPC12249 is promising for research of ovarian cancer and hypertensive diseases .
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- HY-161311
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- HY-141411B
-
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(R)-MRI-1867
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Drug Isomer
Cannabinoid Receptor
NO Synthase
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Others
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(R)-Zevaquenabant ((R)-MRI-1867) is the enantiomer of Zevaquenabant (HY-141411A). 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-14184R
-
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Endothelin Receptor
Apoptosis
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Cardiovascular Disease
Endocrinology
Cancer
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Macitentan (Standard) is the analytical standard of Macitentan. This product is intended for research and analytical applications. Macitentan (ACT-064992) 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) .
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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-106056
-
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D 16726
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Estrogen Receptor/ERR
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Cancer
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Zindoxifene is a partial anti-estrogen. Zindoxifene works primarily by binding to estrogen receptors, thereby inhibiting the growth of estrogen-dependent tumor cells. Zindoxifene is able to exhibit the dual properties of estrogen agonists and antagonists and can be used in research and development to target estrogen-dependent tumors, such as prostate and breast cancer .
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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-10805S
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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-B0358AR
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Calcium Channel
Sodium Channel
Dopamine Receptor
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Neurological Disease
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Flunarizine (dihydrochloride) (Standard) is the analytical standard of Flunarizine (dihydrochloride). This product is intended for research and analytical applications. 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-B0358R
-
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Calcium Channel
Sodium Channel
Dopamine Receptor
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Neurological Disease
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Flunarizine (Standard) is the analytical standard of Flunarizine. This product is intended for research and analytical applications. 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-15895S
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ACT-132577 d4
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Isotope-Labeled Compounds
Endothelin Receptor
|
Cardiovascular Disease
Endocrinology
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Aprocitentan-d4 is a deuterium labeled Aprocitentan. Aprocitentan is a major and pharmacologically active metabolite of Macitentan. Aprocitentan is an orally active dual ETA/ETB antagonist with IC50s of 3.4 nM and 987 nM, and pA2 valus of 6.7 and 5.5, respectively. Aprocitentan is an antihypertensive agent .
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- HY-123205
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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-B0358AS
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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-15895R
-
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Endothelin Receptor
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Cardiovascular Disease
Endocrinology
|
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Aprocitentan (Standard) is the analytical standard of Aprocitentan. This product is intended for research and analytical applications. 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-13511R
-
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Histamine Receptor
Autophagy
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Inflammation/Immunology
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Rupatadine (Standard) is the analytical standard of Rupatadine. This product is intended for research and analytical applications. 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-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-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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mAChR
Phosphodiesterase (PDE)
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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-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-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-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-13511S
-
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UR-12592-d6
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Histamine Receptor
Autophagy
Isotope-Labeled Compounds
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Inflammation/Immunology
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Rupatadine-d6 (D-tartrate) is deuterated labeled Rupatadine (HY-13511). 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-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-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-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-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
|
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-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
|
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-15770
-
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Integrin
|
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
-
|
ACT 078573
|
Orexin Receptor (OX Receptor)
Calcium Channel
Caspase
Apoptosis
|
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-111313
-
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Cholecystokinin Receptor
|
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-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-173474
-
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Estrogen Receptor/ERR
Androgen Receptor
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Cancer
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ERβ agonist-1 (Compound 8) is a dual-active selective ERβ agonist (EC50: 46.8 nM) and AR antagonist (IC50: 1555 nM). ERβ agonist-1 activates ERβ signaling by binding to ERβ and inhibits AR activity. ERβ agonist-1 retains selective ERβ agonist activity in mouse models and can be used to study prostate cancer .
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- HY-123205R
-
|
KW-4354 (Standard)
|
Reference Standards
Histamine Receptor
P2X Receptor
5-HT Receptor
Apoptosis
PERK
p38 MAPK
COX
|
Inflammation/Immunology
|
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Oxatomide (Standard) (KW-4354 (Standard)) is the analytical standard of Oxatomide (HY-123205). This product is intended for research and analytical applications. Oxatomide (KW-4354) is an orally active dual antagonist of the H1-histamine receptor and the P2X7 receptor, as well as an inhibitor of serotonin. Oxatomide possesses antihistaminic, antiallergic and anti-inflammatory activities. Oxatomide can be used in the research of allergic diseases .
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- HY-117621A
-
|
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CCR
|
Metabolic Disease
|
|
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-162412
-
|
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PROTACs
Adrenergic Receptor
Apoptosis
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Cancer
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PROTAC AR/AR-V7 degrader-1 (27c) is a PROTAC-based and dual AR, AR-V7 degrader, with DC50 values of 2.67 and 2.64 μM for AR and AR-V7, respectively. PROTAC AR/AR-V7 degrader-1 (27c) induces apoptosis (Red: AR antagonist; Blue: E3 ligase ligand; Black: linker) .
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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-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-12706
-
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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-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-162812
-
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Apoptosis
Cholinesterase (ChE)
Tau Protein
Ferroptosis
Histamine Receptor
|
Neurological Disease
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H3R antagonist 4 (compound 11L) was a dual inhibitor of cholinesterase and histamine receptor (H3R), with corresponding IC50 of 7.04 μM (eeAChE), 9.73 μM (hAChE)(reversible) and 1.09 nM (H3R) , respectively. H3R antagonist 4 inhibited the aggregation of Aβ1-42 induced by itself and Cu 2+ (95.48% and 88.63%) , and degraded the Aβ1-42 fibrils induced by itself and Cu 2+ (80.16% and 89.30%) . H3R antagonist 4 chelate biometals such as Cu 2+, Zn 2+, Al 3+, and Fe 2+. H3R antagonist 4 significantly reduced tau protein hyperphosphorylation induced by Aβ1-42 and inhibited RSL-3-induced apoptosis and ferroptosis in PC12 cells. H3R antagonist 4 had the best blood-brain barrier permeability and intestinal absorption in hCMEC/D3 and hPepT1-MDCK cells.H3R antagonist 4 ameliorates learning and memory impairment in a mouse model of Alzheimer's disease induced by scopolamine (HY-N0296) .
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- HY-14863
-
|
CTA-018
|
VD/VDR
Cytochrome P450
|
Others
Endocrinology
|
|
Lunacalcipol (CTA-018), as a vitamin D analogue, has a dual role in the pathogenesis of Chronic Kidney Disease (CKD), as an agonist of vitamin D receptor and an antagonist of cytochrome P450 enzyme 24-hydroxylase. Lunacalcipol binds to VDR and regulates transcriptional activity of VDR by influencing ligand binding affinity, ligand-dependent coactivator recruitment or inhibitory factor dissociation, efficiency of ligand entry into target cells, tissue specificity and different metabolism of ligand. Lunacalcipol can be used in the study of CKD, especially Secondary Hyperparathyroidism (sHPT) .
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- HY-123468
-
|
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Cyclic GMP-AMP Synthase
PKA
ERK
Calcium Channel
|
Cardiovascular Disease
Metabolic Disease
|
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HA-1004 is a selective inhibitor of PKA, which can inhibit lipolysis and induce vascular relaxation. HA-1004 is also a dual inhibitor of cyclic GMP-dependent protein kinase and cyclic AMP-dependent protein, and is involved in smooth muscle, second messenger, cyclic AMP and cyclic GMP regulation mechanisms. HA-1004 is an antagonist for calcium, that can be used as a vasodilator to inhibit the contraction of rabbit aortic strips, or to antagonize ERK and tyrosine hydroxylase (TH) phosphorylation in morphine abstinence rat models .
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- HY-123468A
-
|
|
Cyclic GMP-AMP Synthase
PKA
ERK
Calcium Channel
|
Cardiovascular Disease
Metabolic Disease
|
|
HA-1004 dihydrochloride is a selective inhibitor of PKA, which can inhibit lipolysis and induce vascular relaxation. HA-1004 dihydrochloride is also a dual inhibitor of cyclic GMP-dependent protein kinase and cyclic AMP-dependent protein, and is involved in smooth muscle, second messenger, cyclic AMP and cyclic GMP regulation mechanisms. HA-1004 dihydrochloride is an antagonist for calcium, that can be used as a vasodilator to inhibit the contraction of rabbit aortic strips, or to antagonize ERK and tyrosine hydroxylase (TH) phosphorylation in morphine abstinence rat models .
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-
- HY-120802
-
|
AZD-8871; LAS191351
|
mAChR
Adrenergic Receptor
|
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
-
|
|
CXCR
|
Inflammation/Immunology
|
|
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-112348
-
|
|
Cyclic GMP-AMP Synthase
PKA
ERK
Calcium Channel
|
Cardiovascular Disease
Metabolic Disease
|
|
HA-1004 hydrochloride is a selective inhibitor of PKA, which can inhibit lipolysis and induce vascular relaxation. HA-1004 hydrochloride is also a dual inhibitor of cyclic GMP-dependent protein kinase and cyclic AMP-dependent protein (Cyclic GMP-AMP Synthase), and is involved in smooth muscle, second messenger, cyclic AMP and cyclic GMP regulation mechanisms. HA-1004 hydrochloride an antagonist for calcium, that can be used as a vasodilator to inhibit the contraction of rabbit aortic strips, or to antagonize ERK and tyrosine hydroxylase (TH) phosphorylation in morphine abstinence rat models .
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-
- HY-120802A
-
|
AZD-8871 saccharinate; LAS191351 saccharinate
|
mAChR
Adrenergic Receptor
|
Infection
Inflammation/Immunology
|
|
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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-
- HY-121465
-
|
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Stearoyl serotonin is a hybrid molecule patterned after arachidonoyl serotonin. Arachidonoyl serotonin is a dual antagonist of fatty acid amide hydrolase (FAAH) and the transient receptor potential vanilloid-type 1 (TRPV1) channel, reducing both acute and chronic peripheral pain. The effects of replacing the arachidonoyl portion with the saturated 18-carbon stearoyl moiety have not been studied. However, replacement of arachidonate with saturated 11- or 12-carbon fatty acids produces compounds that potently inhibit capsaicin-induced TRPV1 channel activation (IC50=0.76 μM) without blocking FAAH-mediated hydrolysis of arachidonoyl ethanolamine (IC50 > 50 μM).
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-
- HY-121562
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
SB 714786 is a potent and selective 5-hydroxytryptamine 1D (5-HT1D) receptor antagonist. It was developed from the previously reported series of dual 5-HT1 selective 5-hydroxytryptamine reuptake inhibitors (5HT1-SSRIs). SB 714786 is the first reported highly potent and selective 5-HT1D receptor antagonist, providing an extremely useful pharmacological tool for further understanding the role of 5-HT1 receptor subtypes. It has no or very low intrinsic activity against all three receptors. SB 714786 has pKi values of 6.5, 6.7, 9.1 and 6.5 for 5-HT1A, 5-HT1B, 5-HT1D and SerT receptors, respectively, showing high selectivity for 5-HT1D receptors. These properties make SB 714786 a potential tool compound for studying the function of 5-HT1D receptors and the treatment of related diseases.
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| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-W104304
-
|
|
Vasopressin Receptor
|
Cardiovascular Disease
|
|
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 |
-
- HY-P99420
-
|
ALPN-101
|
CD28
|
Inflammation/Immunology
|
|
Acazicolcept (ALPN-101), an Fc fusion protein, is a dual inducible T cell costimulator (ICOS)/CD28 antagonist. Acazicolcept has anti-inflammatory activities .
|
-
- HY-P990706
-
|
ALPN-303
|
TNF Receptor
|
Inflammation/Immunology
|
|
Povetacicept (ALPN-303), an Fc fusion protein of an engineered TACI domain, is a dual APRIL/BAFF antagonist. Povetacicept modulates B lymphocytes and pathogenic autoantibodies for the study of Lupus and other B cell-related autoimmune diseases .
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| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-14184S
-
|
|
|
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) .
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-
-
- HY-15895S
-
|
|
|
Aprocitentan-d4 is a deuterium labeled Aprocitentan. Aprocitentan is a major and pharmacologically active metabolite of Macitentan. Aprocitentan is an orally active dual ETA/ETB antagonist with IC50s of 3.4 nM and 987 nM, and pA2 valus of 6.7 and 5.5, respectively. Aprocitentan is an antihypertensive agent .
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-
-
- HY-17621S
-
|
|
|
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 .
|
-
-
- HY-13511AS
-
|
|
|
Rupatadine-d4 fumarate is a deuterium labeled Rupatadine fumarate. Rupatadine Fumarate (UR-12592 Fumarate) is a potent dual PAF/H1 antagonist with Ki values of 0.55/0.1 μM (rabbit platelet membranes/guinea pig cerebellum membranes) .
|
-
-
- HY-10805S
-
|
|
|
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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-
-
- HY-B0358AS
-
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|
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Flunarizine-d8 dihydrochloride is deuterated labeled Flunarizine dihydrochloride (HY-B0358A). 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-13511S
-
|
|
|
Rupatadine-d6 (D-tartrate) is deuterated labeled Rupatadine (HY-13511). 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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