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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
66 Results for "
vasopressin receptor antagonist
" in MedChemExpress (MCE) Product Catalog:
Products (66)
66 Results for "vasopressin receptor antagonist" in MCE Product Catalog:
20
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Tolvaptan is a selective, competitive and orally active vasopressin receptor 2 (V2R) antagonist with an IC50 of 1.28 μM for the inhibition of arginine vasopressin (AVP)-induced platelet aggregation. Tolvaptan induces cell apoposis and affects cell cycle. Tolvaptan can be used for the research of hyponatremia .
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 .
7
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7
7 Cited Publications
Cat. No.: HY-17572A
CAS No.: 914453-95-5
Synonyms: RW22164 acetate; RWJ22164 acetate
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4
4 Cited Publications
Synonyms: VPA-985; WAY-VPA 985
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Lixivaptan (VPA-985, WAY-VPA 985) is an orally active and selective vasopressin receptor V2 antagonist, with IC50 values of 1.2 and 2.3 nM for human and rat V2, respectively.
2
2 Cited Publications
Cat. No.: HY-15522
CAS No.: 847375-16-0
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WAY-267464 is a non-peptide oxytocin receptor (OTR) agonist. WAY-267464 can impair social recognition memory in rats through a vasopressin 1A receptor antagonist action. WAY-267464 can be used for the research of psychiatric disorders, such disorders include autism spectrum disorder, schizophrenia, and social anxiety disorder .
2
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Cardiovascular Disease Metabolic Disease Endocrinology Cancer
Mozavaptan (OPC-31260) is a benzazepine derivative and a potent, selective, competitive and orally active vasopressin V2 receptor antagonist with an IC50 of 14 nM. Mozavaptan shows ~85-fold selectivity for V2 receptor over V1 receptor (IC50 of 1.2 μM), and can antagonize the antidiuretic action of arginine vasopressin (AVP) in vivo. Mozavaptan has the potential for hyponatremia, syndrome of inappropriate antidiuretic hormone (SIADH), and congestive heart failure treatment .
2
2 Cited Publications
Synonyms: OPC-31260 hydrochloride
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Cardiovascular Disease Metabolic Disease Endocrinology Cancer
Mozavaptan hydrochloride (OPC-31260 hydrochloride) is a benzazepine derivative and a potent, selective, competitive and orally active vasopressin V2 receptor antagonist with an IC50 of 14 nM. Mozavaptan hydrochloride shows ~85-fold selectivity for V2 receptor over V1 receptor (IC50 of 1.2 μM), and can antagonize the antidiuretic action of arginine vasopressin (AVP) in vivo. Mozavaptan hydrochloride has the potential for hyponatremia, syndrome of inappropriate antidiuretic hormone (SIADH), and congestive heart failure treatment .
2
2 Cited Publications
Cat. No.: HY-108679
CAS No.: 1432043-31-6
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WAY-267464 (hydrochloride) is a non-peptide oxytocin receptor (OTR) agonist. WAY-267464 (hydrochloride) can impair social recognition memory in rats through a vasopressin 1A receptor antagonist action. WAY-267464 (hydrochloride) can be used for the research of psychiatric disorders, such disorders include autism spectrum disorder, schizophrenia, and social anxiety disorder .
2
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Cardiovascular Disease Neurological Disease Metabolic Disease
RG7713 (RO5028442) is a highly potent, selective and brain-penetrant Vasopressin 1a (V1a) receptor antagonist with Kis of 1 nM (hV1a) and 39 nM (mV1a).
1
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Nelivaptan (SSR-149415) is a selective and orally active vasopressin V1b receptor antagonist (Ki: 3.7 and 1.3 nM for native and recombinant rat V1b receptors, respectively). Nelivaptan inhibits arginine vasopressin (AVP)-induced Ca 2+ increase and corticotropin secretion. Nelivaptan can be used for research of stress, anxiety and depression .
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Fuscoside (OPC-21268) is an orally effective, nonpeptide, vasopressin V1 receptor antagonist with an IC50 of 0.4 μM.
1
1 Cited Publications
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L-371,257 is an orally bioavailable, non-blood-brain barrier penetrant, selective and competitive antagonist of oxytocin receptor (pA2=8.4) with high affinity at both the oxytocin receptor (Ki=19 nM) and vasopressin V1a receptor (Ki=3.7 nM) .
Synonyms: RG7314
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Balovaptan (RG7314) is an orally available, selective brain-penetrant vasopressin 1a (hV1a) receptor antagonist, with Kis of 1 and 39 nM for human (hV1a) and mouse (mV1a) receptors, and is used for the research of autism.
Synonyms: GSK 221149; GSK 221149A
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Retosiban (GSK221149A) is a potent, selective, and orally active oxytocin receptor antagonist (Ki (hOT) = 0.65 nM, Ki (rOT) = 4.1 nM) with no detectable agonist activity. Retosiban has nanomolar affinity for the oxytocin receptor with >1400-fold selectivity over the closely related vasopressin receptors. Retosiban inhibits spontaneous and induces uterine contractions. Retosiban can be studied in research for preterm labour .
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SRX246 is a potent, BBB-penetrant, highly selective vasopressin 1a (V1a) receptor antagonist (Ki=0.3 nM for human V1a). SRX246 has no interaction at V1b and V2 receptors. SRX246 also displays negligible binding at 64 others receptors classes, including 35 G-proteincoupled receptors. SRX246 can be used for treatment of stress-related disorders .
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TASP0390325 is a high affinity and orally active arginine vasopressin receptor 1B (V1B receptor) antagonist with antidepressant and anxiolytic activities .
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TC OT 39 is a synthetic oxytocin analog, as well as a selective agonist of oxytocin receptor (OXTR, EC50=180 nM). TC OT 39 is also an Avprla vasopressin receptor antagonist with an Ki value of 330 nM. TC OT 39 exhibits sedative effects in mouse models .
Cat. No.: HY-146272
CAS No.: 2648650-50-2
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Vasopressin V2 receptor antagonist 1 is a vasopressin V2 receptor (V2R) antagonist with a Ki value of 3.8 nM. Vasopressin V2 receptor antagonist 1 inhibits renal cyst formation in embryonic renal cyst models and mouse models. Vasopressin V2 receptor antagonist 1 can be used in research related to autosomal dominant polycystic kidney disease .
Cat. No.: HY-159507
CAS No.: 1370444-22-6
Synonyms: Brezivaptanum; TH1773; TS-121
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Brezivaptan (Brezivaptanum; TH1773; TS-121) is a vasopressin receptor antagonist .
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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
