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-A0013
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-
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- HY-14184
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-
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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-109593
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- HY-17621
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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-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-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-B0358
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-
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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-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-A0013A
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-
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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-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-B0358A
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-
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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-124290
-
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AJM300
|
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-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-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-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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- HY-152843
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YZJ-1139
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Orexin Receptor (OX Receptor)
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Neurological Disease
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Fazamorexant (YZJ-1139) is an orally active dual orexin receptor antagonist, with an IC50 of 32 nM against OX1R and an IC50 of 41 nM against OX2R. Fazamorexant prolongs total sleep time and improves sleep efficiency. Fazamorexant is applicable to related research on insomnia .
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- HY-123205
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-
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- HY-10900
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-
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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-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-15895S
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ACT-132577-d4
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Isotope-Labeled Compounds
Endothelin Receptor
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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-112247
-
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PPAR
TGF-beta/Smad
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Metabolic Disease
Inflammation/Immunology
|
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SR 16832 is a dual-site covalent, orthosteric and allosteric PPARγ antagonist. SR 16832 activates the TGF-β signaling pathway and upregulates the expression of Vimentin and Fibronectin (Fibronectin). SR 16832 is toxic to bronchial epithelium. SR 16832 can be used in research related to type 2 diabetes and pulmonary fibrosis .
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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-148088
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M1069
1 Publications Verification
|
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-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-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-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-14184S
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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-14184R
-
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ACT-064992 (Standard)
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Reference Standards
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-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-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-101260
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-
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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-148954
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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-Z8176
-
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Sodium Channel
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Neurological Disease
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(Z)-Flunarizine is the (Z)-isomer of Flunarizine (HY-B0358). 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-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, a chemical probe, 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-B0358AR
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Reference Standards
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-U00253
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-
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- HY-113555
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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-U00072
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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-117965
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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?(HY-B1208), or Histamine(HY-B1204)-induced contraction (β2) .
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- HY-115417
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- HY-17621S
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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-124615
-
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p38 MAPK
PI3K
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Cancer
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ST-162 is a MAPK/PI3K dual antagonist. ST-162 exhibits antitumor activity and can increase the efficacy of immune checkpoint blockers. ST-162 can be used for the research of cancer, such as melanoma .
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- HY-128537
-
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Neurokinin Receptor
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Inflammation/Immunology
|
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DNK-333 is a potent and balanced dual NK1 and NK2 receptor antagonist with IC50 values of 4.8 nM and 5.5 nM, respectively. DNK-333 blocks the Neurokinin A (NKA) (HY-P0197)-induced bronchoconstriction in asthma .
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- HY-116120
-
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- HY-14882R
-
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TAK-652 (Standard); TBR-652 (Standard)
|
CCR
HIV
Reference Standards
|
Infection
Endocrinology
|
|
Cenicriviroc (Standard) is the analytical standard of Cenicriviroc. This product is intended for research and analytical applications. 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-B0358AS
-
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- HY-145862
-
-
- HY-173491
-
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CXCR
CCR
|
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
|
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-19880
-
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- HY-19205A
-
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LDP-392
|
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-101638
-
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(±)-FK1052
|
5-HT Receptor
|
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
|
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.
|
-
- HY-101638A
-
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(±)-FK1052 free base
|
5-HT Receptor
|
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 .
|
-
- HY-153333
-
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|
Adenosine Receptor
|
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-100570
-
-
- 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-170951
-
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Androgen Receptor
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Cancer
|
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-A0013AR
-
-
- HY-114412A
-
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- HY-131479A
-
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Drug Metabolite
|
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-119658
-
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INCB10820
|
CCR
|
Inflammation/Immunology
|
|
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-114412
-
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- HY-124290A
-
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AJM300 hydrochloride
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Integrin
|
Inflammation/Immunology
|
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-114953
-
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Angiotensin Receptor
Endothelin Receptor
|
Cardiovascular Disease
|
|
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-14189
-
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R-411
|
Integrin
|
Inflammation/Immunology
|
|
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-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
-
-
- HY-141411B
-
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(R)-MRI-1867
|
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-161311
-
-
- HY-129808
-
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LPL Receptor
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Cardiovascular Disease
Cancer
|
|
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-106056
-
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D 16726
|
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-10805S
-
-
- HY-B0358R
-
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Reference Standards
Calcium Channel
Sodium Channel
Dopamine Receptor
|
Neurological Disease
|
|
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-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-182677
-
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5-HT Receptor
Dopamine Receptor
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Neurological Disease
|
|
EF-7412 is a dual antagonist of the 5-HT1A receptor and dopamine D2 receptor, with Ki values of 27 nM and 22 nM, respectively. EF-7412 acts as an antagonist at both pre- and postsynaptic 5-HT1A receptor sites, blocking 8-OH-DPAT (HY-112061)-induced hypothermia, behavioral syndrome, and corticosterone elevation in vivo. EF-7412 increases hypothalamic 5-HIAA/5-HT and DOPAC/DA ratios, alters 5-HT and DA neuronal activity, and slightly decreases spontaneous motor activity. EF-7412 can be used for research on 5-HT1A/D2 receptor regulation and related neural pathways .
|
-
- HY-78096
-
|
|
Endogenous Metabolite
|
Metabolic Disease
|
|
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 .
|
-
- HY-182619
-
|
|
PPAR
|
Cancer
|
|
PPARα/δ antagonist-1 is an orally active, highly selective dual antagonist of PPARα/δ, with IC50 values of 0.113 μM and 0.025 μM against human PPARα and PPARδ, respectively. PPARα/δ antagonist-1 exhibits an excellent in vitro activity profile and preliminary efficacy in mouse tumor models. PPARα/δ antagonist-1 can be used in studies related to cancers (melanoma metastasis, ovarian cancer) .
|
-
- HY-101927
-
|
|
NOD-like Receptor (NLR)
|
Cancer
|
|
NOD1/2 antagonist-2 (Compound 26BH) is a dual NOD1/NOD2 antagonist (IC50s: 2.36 μM and 4.16 μM for NOD1 and NOD2, respectively). NOD1/2 antagonist-2 inhibits both NF-κB and MAPK inflammatory signaling, thereby sensitizing Paclitaxel (HY-B0015) to suppress Lewis lung carcinoma growth .
|
-
- HY-180815
-
|
|
Adrenergic Receptor
|
Endocrinology
|
|
α1A/1D-Adrenoceptor antagonist-1 (Compound 15) is a selective α1A/1D-adrenoceptor dual antagonist with IC50 values of 20.26 and 164.9 nM. α1A/1D-Adrenoceptor antagonist-1 shows an IC50 of 1912 nM for α1B-adrenoceptor.α1A/1D-Adrenoceptor antagonist-1 can be used for research of benign prostatic hyperplasia .
|
-
- HY-183239
-
|
|
Adenosine Receptor
|
Inflammation/Immunology
Cancer
|
|
A2AR/A2BR antagonist 2 is a dual A2A/A2B adenosine receptor antagonist with selectivity for the A1 receptor. A2AR/A2BR antagonist 2 reverses adenosine-mediated T-cell immunosuppression in the tumor microenvironment. A2AR/A2BR antagonist 2 can be used in cancer-related research .
|
-
- HY-179607
-
|
|
CCR
|
Inflammation/Immunology
Cancer
|
|
LUF8100 is a dual-target antagonist of CCR2/CCR5 with pKi values for CCR2 and CCR5 of 5.23 and 4.97 respectively. LUF8100 can be used for research on immune homeostasis and cancer .
|
-
- HY-116435
-
-
- HY-180370
-
|
NitroSynapsin; YQW-036; NMI-6979
|
iGluR
Drug Derivative
|
Cardiovascular Disease
Neurological Disease
|
|
Nitromemantine (NitroSynapsin) is a nitrate derivative of Memantine (HY-B0591) and is a dual-functional NMDAR antagonist. Nitromemantine exhibits significant efficacy in rodent models of cerebral infarction through a dual mechanism of blocking channels and regulating receptors via NO/redox regulation. Nitromemantine can target ischemic neurons under hypoxic conditions and enhance its activity. Nitromemantine inhibits the current induced by NMDA, with its IC50 being 2.4 μM. Nitromemantine can be used for the study of cerebral ischemic stroke .
|
-
- HY-19029
-
|
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
|
SDZ 208-912 is a dual-action 5-HT1A/2 receptor agonist and dopamine D1 receptor antagonist. SDZ 208-912 exhibits partial dopamine agonism and atypical neurosedative effects in rodent models. SDZ 208-912 can be used in research on neurological disorders such as schizophrenia .
|
-
- HY-15895R
-
|
ACT-132577 (Standard)
|
Reference Standards
Endothelin Receptor
|
Cardiovascular Disease
Endocrinology
|
|
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 .
|
-
- HY-120172
-
|
|
Lipoxygenase
Leukotriene Receptor
|
Inflammation/Immunology
|
|
WAY-126299A is an orally active dual-acting 5-1ipoxygenase inhibitor (IC50: 12.2 μM) and leukotriene D4 antagonist (pKB: 6.4). WAY-126299A inhibits antigen-induced leukotriene-dependent bronchoconstriction. WAY-126299A can be used for research of asthma .
|
-
- HY-13511R
-
|
UR-12592 (Standard)
|
Reference Standards
Histamine Receptor
Autophagy
|
Inflammation/Immunology
|
|
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 .
|
-
- HY-129448
-
|
|
Neurokinin Receptor
|
Neurological Disease
|
|
RO4583298 is a potent, orally active dual antagonist of NK1 (human and gerbil)/NK3 (human, cynomolgus monkey, gerbil and guinea-pig). RO4583298 inhibits senktide-induced potentiation of spontaneous activity of dopaminergic neurons. RO4583298 can block gerbil foot tapping response and inhibits mouse tail whips .
|
-
- HY-13511AR
-
|
UR-12592 Fumarate (Standard)
|
Reference Standards
Histamine Receptor
Autophagy
|
Inflammation/Immunology
|
|
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 .
|
-
- HY-134189A
-
|
|
Sigma Receptor
Opioid Receptor
|
Neurological Disease
|
|
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 .
|
-
- HY-115871A
-
|
|
mAChR
Phosphodiesterase (PDE)
|
Others
|
|
(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 .
|
-
- HY-139230
-
|
|
Cannabinoid Receptor
PPAR
|
Metabolic Disease
|
|
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) .
|
-
- HY-148088A
-
|
|
Adenosine Receptor
|
Cancer
|
|
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 .
|
-
- HY-10900R
-
|
|
Reference Standards
Orexin Receptor (OX Receptor)
|
Neurological Disease
Endocrinology
|
|
TCS 1102 (Standard) is the analytical standard of TCS 1102 (HY-10900). This product is intended for research and analytical applications. TCS 1102 is a potent, dual orexin receptor antagonist, with Ki values of 0.2 nM and 3 nM for OX2 and OX1 receptors, respectively. TCS 1102 demonstrates excellent blood-brain barrier penetrability and moderate bioavailability in rats .
|
-
- HY-14190A
-
|
(rac)-R-411 free base
|
Drug Isomer
|
Others
|
|
(rac)-Valategrast ((rac)-R-411 free base) is a racemic compound of Valategrast (HY-14190). Valategrast is a potent, orally active dual antagonist of integrin α4β1 (VLA-4) and α4β7. Valategrast may be used in research on chronic obstructive pulmonary disease (COPD) and asthma.
|
-
- HY-155615
-
|
|
Sigma Receptor
Histamine Receptor
|
Neurological Disease
|
|
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 .
|
-
- HY-13511S
-
|
UR-12592-d6
|
Histamine Receptor
Isotope-Labeled Compounds
Autophagy
|
Inflammation/Immunology
|
|
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 .
|
-
- HY-16780
-
|
ONO-6950
|
Leukotriene Receptor
|
Inflammation/Immunology
|
|
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.
|
-
- 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 .
|
-
- HY-176920
-
|
|
Leukotriene Receptor
|
Inflammation/Immunology
|
|
BRI-12349 (Compound 50) is a dual antagonist of CysLT1R/CysLT2R with Ki values of 1.03 and 6.46 μM. BRI-12349 can inhibit the generation of IP1 induced by LTD4 (the main ligand of CysLTs). BRI-12349 can be used for the research of immunology and inflammation, such as asthma .
|
-
- HY-135390
-
|
Ro 64-1056
|
Drug Metabolite
|
Cardiovascular Disease
|
|
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 .
|
-
- HY-109067AR
-
|
VVZ-149 hydrochloride (Standard)
|
Reference Standards
GlyT
5-HT Receptor
P2X Receptor
|
Neurological Disease
|
|
Opiranserin hydrochloride (Standard) is the analytical standard of Opiranserin (hydrochloride) (HY-109067A). This product is intended for research and analytical applications. 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 .
|
-
- HY-120321
-
|
|
Mineralocorticoid Receptor
Carbonic Anhydrase
|
Cardiovascular Disease
|
|
DSR-71167 is an orally active mineralocorticoid receptor (MR) antagonist with an IC50 of 0.26 μM. DSR-71167 exhibits weak carbonic anhydrase (CA) inhibitory activity with an IC50 of 19 μM. DSR-71167 can dose-dependently increase urinary sodium excretion in rat models and has a very low risk of hyperkalemia in potassium-loading rat models. DSR-71167 lowers systolic blood pressure in hypertensive rat models. DSR-71167 can be used for research on hypertension and heart failure .
|
-
- HY-14485
-
|
|
P2X Receptor
|
Neurological Disease
|
|
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 .
|
-
- HY-138542
-
|
|
Integrin
|
Inflammation/Immunology
|
|
RO0270608, the active metabolite of R411, is a dual alpha4beta1-alpha4beta7 (α4β1/α4β7) integrin antagonist. Antiinflammatory activity .
|
-
- HY-10805A
-
|
ACT 078573 hydrochloride
|
Orexin Receptor (OX Receptor)
Calcium Channel
Caspase
Apoptosis
|
Neurological Disease
Endocrinology
Cancer
|
|
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 .
|
-
- HY-117621
-
|
|
CCR
|
Metabolic Disease
|
|
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 .
|
-
- HY-15770
-
|
|
Integrin
|
Inflammation/Immunology
|
|
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 .
|
-
- HY-10805
-
|
ACT 078573
|
Orexin Receptor (OX Receptor)
Calcium Channel
Caspase
Apoptosis
|
Neurological Disease
Endocrinology
Cancer
|
|
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 .
|
-
- HY-111313
-
|
|
Cholecystokinin Receptor
|
Metabolic Disease
|
|
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 .
|
-
- HY-179684
-
|
|
CGRP Receptor
5-HT Receptor
ERK
Epigenetic Reader Domain
|
Neurological Disease
|
|
PCC0105005 is a dual-target CGRP Receptor antagonist (IC50 = 1.01 nM) and a partial agonist of 5-HT1F Receptor (EC50 = 77.91 nM). PCC0105005 shows significant efficacy in the rat model of migraine. PCC0105005 significantly reduces the expression of CGRP and c-Fos proteins, and inhibits the phosphorylation levels of ERK and CREB. PCC0105005 can be used for research on migraine .
|
-
- HY-163101
-
|
|
Platelet-activating Factor Receptor (PAFR)
Leukotriene Receptor
|
Inflammation/Immunology
|
|
CP-96021 is an orally active dual leukotriene D4 (LTD4) and platelet activating factor (PAF) receptor antagonist, featuring a guinea pig LTD4 receptor Ki of 34 nM and a rabbit PAF receptor Ki of 37 nM. CP-96021 blocks ligand binding to its target receptors, inhibits ligand-induced bronchoconstriction, and inhibits antigen-triggered airway obstructive effects. CP-96021 can be used for the research of asthma .
|
-
- HY-155614
-
|
|
Sigma Receptor
Histamine Receptor
|
Neurological Disease
|
|
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 .
|
-
- HY-173474
-
|
|
Estrogen Receptor/ERR
Androgen Receptor
|
Cancer
|
|
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 .
|
-
- HY-123205R
-
|
KW-4354 (Standard)
|
Reference Standards
Histamine Receptor
P2X Receptor
5-HT Receptor
Apoptosis
PERK
p38 MAPK
COX
|
Inflammation/Immunology
|
|
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 .
|
-
- HY-117621A
-
|
|
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 .
|
-
- HY-146077
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
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 .
|
-
- HY-146076
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
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 .
|
-
- HY-101834R
-
|
|
Reference Standards
Orexin Receptor (OX Receptor)
|
Others
|
|
ACT-462206 (Standard) is the analytical standard of ACT-462206 (HY-101834). This product is intended for research and analytical applications. 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 .
|
-
- HY-162412
-
|
|
PROTACs
Adrenergic Receptor
Apoptosis
|
Cancer
|
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) .
|
-
- HY-179605
-
|
|
Androgen Receptor
|
Others
|
|
AR ligand-49 (Compound 4q) is a dual ligand for the adenosine A2A receptor (A2AAR) and the A3 receptor (A3AR). Its Ki values are 15 and 4.5 nM respectively. AR ligand-49 exhibits reverse agonistic activity at hA2AAR and antagonistic activity at hA3AR. AR ligand-49 can be used for the study of the design and development of adenosine receptor ligands .
|
-
- HY-12706
-
-
- HY-181722
-
|
|
Sigma Receptor
Histamine Receptor
|
Neurological Disease
|
|
σ1R/H3R ligand-1 is a dual σ1R/H3R antagonist with a σ1R Ki of 8.8 nM and an H3R Ki of 31.2 nM. Through the dual action of simultaneously antagonizing σ1R and H3R, σ1R/H3R ligand-1 exhibits potent dose-dependent analgesic activity in mouse models of visceral pain and neuropathic pain. σ1R/H3R ligand-1 can be used for the research of visceral pain and neuropathic pain .
|
-
- HY-162812
-
|
|
Apoptosis
Cholinesterase (ChE)
Tau Protein
Ferroptosis
Histamine Receptor
|
Neurological Disease
|
|
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) .
|
-
- HY-P990706
-
|
ALPN-303
|
TNF Receptor
|
Inflammation/Immunology
|
|
Povetacicept (ALPN-303) is an engineered Fc fusion protein containing the TACI domain, and acts as a dual APRIL/BAFF antagonist. The Kd value of Povetacicept for human BAFF is 59.3 pM, while its Kd value for human APRIL is 1.00 pM. Povetacicept reduces the activation, proliferation, differentiation and survival of B cells, and inhibits the production of immunoglobulins and autoantibodies. Povetacicept can be used in research related to autoimmune hemolytic anemia, immune thrombocytopenia, systemic lupus erythematosus, lupus nephritis and myasthenia gravis .
|
-
- HY-163065
-
|
|
Opioid Receptor
Sigma Receptor
|
Neurological Disease
|
|
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 .
|
-
- HY-10805R
-
|
ACT 078573 (Standard)
|
Orexin Receptor (OX Receptor)
Calcium Channel
Caspase
Apoptosis
Reference Standards
|
Neurological Disease
Endocrinology
Cancer
|
|
Almorexant (Standard) is the analytical standard of Almorexant. This product is intended for research and analytical applications. 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 Ca2+ signal pathway. Almorexant stimulates caspase-3 activity in AsPC-1 cells and induces apoptosis .
|
-
- HY-W017463
-
|
|
Drug Intermediate
TMV
Isocitrate Dehydrogenase (IDH)
|
Infection
|
|
trans-3-(3-Pyridyl) acrylic acid is an unsaturated carboxylic acid and synthetic building block, which serves as a synthetic precursor of 3-(3-pyridyl) propanoic acid. trans-3-(3-Pyridyl) acrylic acid can be used to prepare dual mutant IDH1/NAMPT inhibitors and PGE2 antagonist analogs. In addition, trans-3-(3-Pyridyl) acrylic acid exhibits antiviral activity against tobacco mosaic virus (TMV) .
|
-
- HY-182736
-
|
|
CCR
Histamine Receptor
Calcium Channel
|
Inflammation/Immunology
|
|
YM-344484 is an orally active dual antagonist of chemokine CCR3 receptor and histamine histamine H1 receptor. YM-344484 inhibits ligand-induced Ca 2+ influx, chemotaxis of CCR3-expressing cells, histamine-induced Ca 2+ influx, increased vascular permeability and eosinophil accumulation. YM-344484 suppresses vascular permeability and inhibits eosinophil infiltration in a mouse asthma model. YM-344484 can be used in research related to asthma, allergic rhinitis and atopic dermatitis .
|
-
- HY-10805AR
-
|
ACT 078573 hydrochloride (Standard)
|
Reference Standards
Orexin Receptor (OX Receptor)
Calcium Channel
Caspase
Apoptosis
|
Neurological Disease
Endocrinology
Cancer
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Almorexant hydrochloride (Standard) is the analytical standard of Almorexant (hydrochloride) (HY-10805A). This product is intended for research and analytical applications. 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 Ca2+ signal pathway. Almorexant hydrochloride stimulates caspase-3 activity in AsPC-1 cells and induces apoptosis .
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- HY-14863
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CTA-018
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VD/VDR
Cytochrome P450
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Others
Endocrinology
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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
Tyrosine Hydroxylase
Calcium Channel
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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
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Cyclic GMP-AMP Synthase
PKA
ERK
Calcium Channel
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Cardiovascular Disease
Metabolic Disease
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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
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AZD-8871; LAS191351
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mAChR
Adrenergic Receptor
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Inflammation/Immunology
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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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CXCR
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Inflammation/Immunology
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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-112348
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Cyclic GMP-AMP Synthase
PKA
ERK
Calcium Channel
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Cardiovascular Disease
Metabolic Disease
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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-10383
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Endothelin Receptor
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Cardiovascular Disease
Metabolic Disease
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J-104132 (L-753037) is a potent, orally active, selective and competitive ETA/ETB receptor antagonist with Ki of 0.034 nM for ETA and 0.104 nM for ETB receptors. J-104132 inhibits Endothelin-1 (ET-1) (HY-P71446)-induced signaling and vascular contractions in vitro. J-104132 alleviates hypertension, vascular remodeling, and diabetic endothelial dysfunction in vivo by dual ETA/ETB blockade. J-104132 can be used for research on diabetic vascular complications [1][3].
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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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- HY-108942
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Adenosine Receptor
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Cardiovascular Disease
Neurological Disease
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ASP5854 is an orally active, blood-brain barrier permeable adenosine A1/A2a dual receptor antagonist. ASP5854 blocks receptor activity and agonist-induced intracellular calcium elevation, and exhibits the characteristic of slow dissociation from striatal A2a receptors in primates. ASP5854 reverses catalepsy, enhances cognitive ability, improves motor function and exerts neuroprotective effects, while also alleviating dyskinesia and increasing contralateral turning behavior. ASP5854 is mainly used in studies related to ischemic stroke and Parkinson's disease .
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- HY-121465
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Endogenous Metabolite
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Metabolic Disease
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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-178919
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Formyl Peptide Receptor (FPR)
Apoptosis
Bacterial
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Inflammation/Immunology
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N-19004 is a FPR1 antagonist. N-19004 shows broad-spectrum antibacterial effects against a variety of pathogens. N-19004 exhibits significant retinal protective effects in the rd10 mouse model of retinitis pigmentosa (RP). N-19004 can attenuate retinal dysfunction, mitigate rod and cone degeneration, and reduce immune cell activation, gliosis, inflammation, oxidative stress, and apoptosis. N-19004 can reduce the size of laser-induced choroidal lesions and promote edema absorption through dual anti-inflammatory and anti-angiogenic effects. N-19004 can be used for the research of retinal degenerative diseases such as retinitis pigmentosa .
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- HY-174306
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5-HT Receptor
PGC-1α
Akt
PI3K
Ras
MEK
ERK
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Metabolic Disease
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MARY1 is a selective 5-HT2BR antagonist with an IC50 of 380 nM and a Ki of 764 nM (human
5-HT2BR). MARY1 induces renal mitochondrial biogenesis (MB) and enhances renal mitochondrial function by increasing mitochondrial respiratory capacity, mitochondrial protein levels, and mitochondrial number in renal proximal tubular cells (RPTCs). MARY1 induces MB through 5-HT2BR and dual PI3K/AKT and RAS/MEK/ERK cell signaling pathways in RPTCs. MARY1 can be used to study renal diseases associated with metabolic and mitochondrial dysfunction .
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- HY-165459
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MK-056
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TRP Channel
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Infection
Inflammation/Immunology
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KJM429 (MK-056) is a high-affinity ligand for the rat vanilloid receptor rTRPV1 (Ki=30-63 nM) with a unique dual regulatory function. KJM429 acts as a competitive antagonist to inhibit TRPV1 receptor activation induced by Capsaicin (HY-10448), resiniferatoxin, thermal stimulation and weak acid (pH 6.0), and switches to a TRPV1 agonist under strong acid conditions (pH<5.5). KJM429 effectively blocks calcium influx induced by Capsaicin and partial thermal stimulation, and triggers calcium uptake under low pH conditions, with minimal effects on non-TRPV1-mediated calcium signaling. KJM429 can be used for research on the mechanisms of pain-related diseases such as postherpetic neuralgia, diabetic neuropathy, cluster headache, osteoarthritis and pruritus .
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- HY-P11490
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MDM-2/p53
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Inflammation/Immunology
Cancer
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DPMI-ω is a dual-specificity d-peptide antagonist of oncogenic proteins MDM2 and MDMX. DPMI-ω, upon fabrication on gold nanoparticles, efficiently traverses tumor cells and kills them by reactivating the p53 signaling pathway. DPMI-ω can disrupte the p53-MDM2/MDMX complex. DPMI-ω can inhibit B16 melanoma growth and induce cells G0/G1 phase arrest. DPMI-ω can augment the efficacy of immunotherapy by expanding CD3 +/CD8 + cytotoxic T cells and suppressing CD4 +/CD25 + regulatory T cells companied with anti-PD1 antibody. DPMI-ω can be used for research of melanoma .
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- HY-121562
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5-HT Receptor
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Neurological Disease
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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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- HY-165587
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Prostaglandin Receptor
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Cardiovascular Disease
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BM-573 is an orally active dual thromboxane A₂ (TXA₂) modulator with an IC50 of 1.3 nM. BM-573 possesses both thromboxane synthase (TxAS) inhibition and thromboxane receptor (TP) antagonistic effects. BM-573 can completely inhibit platelet aggregation induced by Arachidonic acid (HY-109590) or U-46619 (TXA₂ analogues). BM-573 completely blocks the generation of TXB₂ (the stable metabolite of TXA₂) in human platelets and does not inhibit cyclooxygenase (COX-1/COX-2), thus avoiding interference with other prostaglandin synthesis. BM-573 has an inhibitory effect on U-46619-induced contractions in rat gastric fundus smooth muscle (ED₅₀ = 4.2 μM), but has no effect on contractions caused by PGE₂, PGF₂α, or PGI₂. BM-573 can be used in the study of atherosclerosis, myocardial infarction, pulmonary hypertension and shock .
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- HY-183805
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5-HT Receptor
FAAH
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Neurological Disease
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5-HT6R/FAAH modulator 2 is a dual 5-HT6R antagonist and FAAH inhibitor with human 5-HT6R pKi 7.24, human FAAH pIC50 5.47, and blood-brain barrier penetration.5-HT6R/FAAH modulator 2 modulates serotonergic signaling, blocks 5-HT6R function, inhibits endocannabinoid degradation via FAAH catalytic activity suppression.5-HT6R/FAAH modulator 2 exhibits neuroprotective effects against mitochondrial dysfunction, amyloid-β, and glutamate-induced toxicity, reverses memory deficits.5-HT6R/FAAH modulator 2 shows reduced cytotoxicity relative to oxygen-containing lead compounds.5-HT6R/FAAH modulator 2 can be used for the research of Alzheimer's disease .
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| Cat. No. |
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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- HY-P11490
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MDM-2/p53
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Inflammation/Immunology
Cancer
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DPMI-ω is a dual-specificity d-peptide antagonist of oncogenic proteins MDM2 and MDMX. DPMI-ω, upon fabrication on gold nanoparticles, efficiently traverses tumor cells and kills them by reactivating the p53 signaling pathway. DPMI-ω can disrupte the p53-MDM2/MDMX complex. DPMI-ω can inhibit B16 melanoma growth and induce cells G0/G1 phase arrest. DPMI-ω can augment the efficacy of immunotherapy by expanding CD3 +/CD8 + cytotoxic T cells and suppressing CD4 +/CD25 + regulatory T cells companied with anti-PD1 antibody. DPMI-ω can be used for research of melanoma .
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| Cat. No. |
Product Name |
Target |
Research Area |
Image |
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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) is an engineered Fc fusion protein containing the TACI domain, and acts as a dual APRIL/BAFF antagonist. The Kd value of Povetacicept for human BAFF is 59.3 pM, while its Kd value for human APRIL is 1.00 pM. Povetacicept reduces the activation, proliferation, differentiation and survival of B cells, and inhibits the production of immunoglobulins and autoantibodies. Povetacicept can be used in research related to autoimmune hemolytic anemia, immune thrombocytopenia, systemic lupus erythematosus, lupus nephritis and myasthenia gravis .
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(5)
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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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(5)
| Cat. No. |
Product Name |
Chemical Structure |
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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 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-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) .
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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 .
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- HY-B0358AS
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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-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 values of 0.55/0.1 μM (rabbit platelet membranes/guinea pig cerebellum membranes) .
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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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- HY-13511S
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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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