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Darusentan
CAS No. 171714-84-4
Darusentan( Lu-135252 )
Catalog No. M20203 CAS No. 171714-84-4
Darusentan is a potent inhibitor of endothelin signaling and function in both large and small arteries.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 2MG | 57 | In Stock |
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| 5MG | 95 | In Stock |
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| 10MG | 160 | In Stock |
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| 25MG | 290 | In Stock |
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| 50MG | 478 | In Stock |
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| 100MG | 691 | In Stock |
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| 200MG | Get Quote | In Stock |
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| 500MG | Get Quote | In Stock |
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| 1G | Get Quote | In Stock |
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Biological Information
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Product NameDarusentan
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NoteResearch use only, not for human use.
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Brief DescriptionDarusentan is a potent inhibitor of endothelin signaling and function in both large and small arteries.
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DescriptionDarusentan is a potent inhibitor of endothelin signaling and function in both large and small arteries.(In Vitro):Darusentan ((S)-Darusentan) competes for radiolabeled endothelin binding in rat aortic vascular smooth muscle cells (RAVSMs) membranes with single-site kinetics, exhibiting a Ki=13 nM. In isolated endothelium-denuded rat aortic rings, Darusentan inhibits endothelin-induced vascular contractility with a pA2=8.1±0.14. Darusentan ( 0.001-1μM) inhibits ET-1-induced signaling in cultured RAVSMs.(In Vivo):Darusentan (30 mg/kg per day orally for weeks 3 and 4) reverses aortic alterations produced by infusion of Norepinephrine (2.5 μg/kg per min subcutaneously for 2 and 4 weeks) in male Sprague Dawley rats.
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In VitroDarusentan ((S)-Darusentan) competes for radiolabeled endothelin binding in rat aortic vascular smooth muscle cells (RAVSMs) membranes with single-site kinetics, exhibiting a Ki=13 nM. In isolated endothelium-denuded rat aortic rings, Darusentan inhibits endothelin-induced vascular contractility with a pA2=8.1±0.14. Darusentan ( 0.001-1μM) inhibits ET-1-induced signaling in cultured RAVSMs.
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In VivoDarusentan (30 mg/kg per day orally for weeks 3 and 4) reverses aortic alterations produced by infusion of Norepinephrine (2.5 μg/kg per min subcutaneously for 2 and 4 weeks) in male Sprague Dawley rats. Animal Model:Twenty-four (eight per group) male Sprague Dawley rats weighing 175±200 g Dosage:30 mg/kg Administration:Administered orally in rat food for weeks 3 and 4 Result:Reversed aortic alterations produced by infusion of Norepinephrine (2.5 μg/kg).
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SynonymsLu-135252
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PathwayProteasome/Ubiquitin
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TargetEndogenous Metabolite
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RecptorEndothelin A receptor
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Research AreaMetabolic Disease
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IndicationArrhythmias; Diabetic angiopathies; Diabetic nephropathies; Heart failure; Ischaemic heart disorders
Chemical Information
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CAS Number171714-84-4
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Formula Weight410.43
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Molecular FormulaC22H22N2O6
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Purity>98% (HPLC)
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SolubilityDMSO:125 mg/mL (304.57 mM);Water:Insoluble
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SMILESCOc1cc(OC)nc(O[C@H](C(O)=O)C(OC)(c2ccccc2)c2ccccc2)n1
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Chemical Name(S)-2-((46-Dimethoxy-2-pyrimidinyl)oxy)-3-methoxy-33-diphenylpropionic acid
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1.Liang F et al. Darusentan is a potent inhibitor of endothelin signaling and function in both large and small arteries. Can J Physiol Pharmacol. 2010 Aug;88(8):840-9.
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