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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
175 Results for "
dual antagonist
" in MedChemExpress (MCE) Product Catalog:
Products (175)
175 Results for "dual antagonist" in MCE Product Catalog:
32
32 Publications Verification
Cat. No.: HY-A0013
CAS No.: 147536-97-8
Target:
Research Areas:
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.
32
32 Publications Verification
Cat. No.: HY-A0013A
CAS No.: 157212-55-0
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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.
14
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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) .
14
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Conivaptan hydrochloride (YM 087) is an orally active dual vasopressin V1a/V2 receptor antagonist with Ki values of 0.48 nM and 3.04 nM for vasopressin V1a receptor and V2 receptor, respectively. Conivaptan hydrochloride competitively and reversibly blocks vasopressin-mediated antidiuresis, vasoconstriction, and cellular hypertrophy, while inhibiting CYP3A4. Conivaptan hydrochloride inhibits vasopressin-induced intracellular calcium, cAMP, and mitogen-activated kinase activation in vascular smooth muscle cells and cardiomyocytes. Conivaptan hydrochloride induces water diuresis while improving hemodynamics in heart failure models, reducing left ventricular end-diastolic pressure, vascular resistance, and organ weight. Conivaptan hydrochloride is used for research on hyponatremia and congestive heart failure .
9
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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 .
9
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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 .
9
9 Cited Publications
Synonyms: ACT 078573 hydrochloride
Research Areas:
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 .
7
7 Cited Publications
Synonyms: TAK-652; TBR-652
Research Areas:
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 .
7
7 Cited Publications
Synonyms: TAK-652 Mesylate; TBR-652 Mesylate
Research Areas:
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.
6
6 Cited Publications
Cat. No.: HY-B0358
CAS No.: 52468-60-7
Research Areas:
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 .
6
6 Cited Publications
Cat. No.: HY-B0358A
CAS No.: 30484-77-6
Research Areas:
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 .
6
6 Cited Publications
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Research Areas:
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 .
3
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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 .
2
2 Cited Publications
Synonyms: UR-12592 Fumarate
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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 .
2
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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 .
1
1 Cited Publications
Target:
Research Areas:
Cardiovascular Disease Inflammation/Immunology Endocrinology Cancer
BMS-813160 is a potent and selective CCR2/5 dual antagonist. BMS-813160 binds with CCR2 and CCR5 with IC50s of 6.2 and 3.6 nM, respectively. BMS-813160 can be used for the research of inflammation .
1
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1
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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 .
1
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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 .
1
1 Cited Publications
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Research Areas:
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 .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
