{"product_id":"darusentan-bhb21300126","title":"Darusentan","description":"\u003ch3\u003eProduct details\u003c\/h3\u003e \u003cul\u003e\n\u003cli\u003e\n\u003cstrong\u003eChemical name:\u003c\/strong\u003e (2S)-2-(4,6-dimethoxypyrimidin-2-yl)oxy-3-methoxy-3,3-diphenylpropanoic acid.\u003c\/li\u003e\n\u003cli\u003e\n\u003cstrong\u003eAlso known as:\u003c\/strong\u003e LU 135252\u003c\/li\u003e\n\u003cli\u003e\n\u003cstrong\u003eCAS number:\u003c\/strong\u003e 171714-84-4\u003c\/li\u003e\n\u003cli\u003e\n\u003cstrong\u003eMolecular formula:\u003c\/strong\u003e C22H22N2O6.\u003c\/li\u003e\n\u003cli\u003e\n\u003cstrong\u003ePurity:\u003c\/strong\u003e \u0026gt;99%\u003c\/li\u003e\n\u003cli\u003e\n\u003cstrong\u003eConcentration:\u003c\/strong\u003e 1 nM - 1 µM.\u003c\/li\u003e\n\u003cli\u003e\n\u003cstrong\u003eForm:\u003c\/strong\u003e Lyophilized powder.\u003c\/li\u003e\n\u003cli\u003e\n\u003cstrong\u003eSolubility:\u003c\/strong\u003e Soluble in DMSO. Centrifuge all products before use (10000 x g 5 min).\u003c\/li\u003e\n\u003cli\u003e\n\u003cstrong\u003eReconstitution:\u003c\/strong\u003e Soluble in DMSO. Centrifuge all products before use (10000 x g 5 min).\u003c\/li\u003e\n\u003cli\u003e\n\u003cstrong\u003eShipping:\u003c\/strong\u003e Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.\u003c\/li\u003e\n\u003cli\u003e\n\u003cstrong\u003eTarget:\u003c\/strong\u003e ET-A receptors\u003c\/li\u003e\n\u003cli\u003e\n\u003cstrong\u003eSource:\u003c\/strong\u003e Synthetic\u003c\/li\u003e\n\u003cli\u003e\n\u003cstrong\u003eActivity:\u003c\/strong\u003e Darusentan is a selective antagonist of ET-A Endothelin receptors, inhibiting Endothelin-1 radioligand binding to ET-A and ET-B receptors with Ki of 6 nM and 371 nM, respectively1. in vitro Darusentan inhibits Endothelin-induced vascular contractility in isolated endothelium-denuded rat aortic rings with pA2 of 8.12. Darusentan is orally bioavailable and active in vivo3.\u003c\/li\u003e\n\u003cli\u003e\n\u003cstrong\u003eAlternative names:\u003c\/strong\u003e LU 135252\u003c\/li\u003e\n\u003c\/ul\u003e \u003ch3\u003eScientific background\u003c\/h3\u003e \u003cp\u003eDarusentan, (LU 135252), is a synthetic compound that acts as a selective antagonist of endothelin A (ET-A) receptors. Darusentan is orally bioavailable and is a potent inhibitor of vasoconstriction in large and small arteries. The compound is a propanoic acid based antagonist that consist of two enantiomers - (R) and (S). The (R) enantiomer shows no binding activity, indicating that the (S) enantiomer is the active drug1,2.in vitro, Darusentan inhibits endothelin-induced vascular contractility in isolated endothelium-denuded rat aortic rings with pA2 value of 8.11,2.Endothelin receptors include two subtypes: ET-A and ET-B. They are widely distributed in vascular and nonvascular tissues. ET-A receptors are predominantly expressed in peripheral tissues, especially in vascular smooth muscle tissues to mediate vasoconstriction. They are also detected in several different regions of the brain3.\u003c\/p\u003e \u003cp\u003e\u003cstrong\u003eLead time:\u003c\/strong\u003e 1-2 Business Days\u003c\/p\u003e \u003cp\u003e\u003cstrong\u003eCountry of origin:\u003c\/strong\u003e Israel\/IL\u003c\/p\u003e \u003ch3\u003eApplications key\u003c\/h3\u003e \u003cp\u003eApplication key: FC- Flow cytometry, IFC- Indirect flow cytometry, IHC- Immunohistochemistry,LCI- Live cell imaging, Calcium imaging assay,Cell survival assay, Electrophysiology, Neurite outgrowth assay.\u003c\/p\u003e \u003cp\u003e\u003cstrong\u003eBioassay tested:\u003c\/strong\u003e Yes\u003c\/p\u003e","brand":"Alomone Labs","offers":[{"title":"10 mg \/ 1","offer_id":53249706459501,"sku":"D-265-10MG-1","price":337.0,"currency_code":"USD","in_stock":true},{"title":"25 mg \/ 1","offer_id":53311549833581,"sku":"D-265-25MG-1","price":595.0,"currency_code":"USD","in_stock":true},{"title":"5 mg \/ 1","offer_id":53311549866349,"sku":"D-265-5MG-1","price":235.0,"currency_code":"USD","in_stock":true},{"title":"50 mg \/ 1","offer_id":53311549899117,"sku":"D-265-50MG-1","price":917.0,"currency_code":"USD","in_stock":true}],"thumbnail_url":"\/\/cdn.shopify.com\/s\/files\/1\/0949\/7424\/7277\/files\/D-265_gr-1.gif?v=1778544415","url":"https:\/\/www.ebiohippo.com\/products\/darusentan-bhb21300126","provider":"BioHippo","version":"1.0","type":"link"}