{"product_id":"act-132577-bhb21300025","title":"ACT-132577","description":"\u003ch3\u003eProduct details\u003c\/h3\u003e \u003cul\u003e\n\u003cli\u003e\n\u003cstrong\u003eChemical name:\u003c\/strong\u003e 5-(4-bromophenyl)-4-[2-(5-bromopyrimidin-2-yl)oxyethoxy]-6-(sulfamoylamino)pyrimidine.\u003c\/li\u003e\n\u003cli\u003e\n\u003cstrong\u003eAlso known as:\u003c\/strong\u003e Despropyl Macitentan\u003c\/li\u003e\n\u003cli\u003e\n\u003cstrong\u003eCAS number:\u003c\/strong\u003e 1103522-45-7\u003c\/li\u003e\n\u003cli\u003e\n\u003cstrong\u003eMolecular formula:\u003c\/strong\u003e C16H14Br2N6O4S.\u003c\/li\u003e\n\u003cli\u003e\n\u003cstrong\u003ePurity:\u003c\/strong\u003e \u0026gt;98%\u003c\/li\u003e\n\u003cli\u003e\n\u003cstrong\u003eConcentration:\u003c\/strong\u003e 1-100 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 with gentle warming. 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 with gentle warming. 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 Endothelin 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 ACT-132577, a metabolite of macitentan, is a dual antagonist of ET-A and ET-B endothelin receptors, inhibiting binding of 125I-ET-1 to recombinant ET-A and ET-B receptors with IC50 values of 3.4 nM and 987 nM, respectively1.\u003c\/li\u003e\n\u003cli\u003e\n\u003cstrong\u003eAlternative names:\u003c\/strong\u003e Despropyl Macitentan\u003c\/li\u003e\n\u003c\/ul\u003e \u003ch3\u003eScientific background\u003c\/h3\u003e \u003cp\u003eACT-132577 is an active metabolite of Macitentan that acts as an endothelin B (ET-B) and endothelin A (ET-A) receptor antagonist. ACT-132577 antagonizes the specific binding of endothelin-1 on membranes of cells overexpressing ET-A and ET-B receptors with IC50 values of 3.4 nM and 987 nM, respectively1. It also has the ability to reach full inhibition of intracellular Ca2+ increase induced by endothelin-1 on non-recombinant cells1.Endothelin receptors belong to the superfamily of G-protein coupled receptors and include two subtypes: ET-A and ET-B. ET-A receptors are predominantly expressed in peripheral tissues, especially in vascular smooth muscle tissues to mediate vasoconstriction. They are also present in several different regions of the brain. ET-B receptors play an important role in regulating renal function and blood pressure and are expressed in sensory nerves. They are mainly detected in medium- and large-sized cell bodies of human trigeminal ganglia.The ET-A receptor has high affinity for endothelin-1 and endothelin-2 and relatively low affinity for endothelin-3, while the ET-B receptor has high affinity for all endothelin isopeptides2,3.\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":53249705738605,"sku":"A-350-10MG-1","price":406.0,"currency_code":"USD","in_stock":true},{"title":"25 mg \/ 1","offer_id":53311547638125,"sku":"A-350-25MG-1","price":730.0,"currency_code":"USD","in_stock":true},{"title":"5 mg \/ 1","offer_id":53311547670893,"sku":"A-350-5MG-1","price":235.0,"currency_code":"USD","in_stock":true},{"title":"50 mg \/ 1","offer_id":53311547703661,"sku":"A-350-50MG-1","price":1148.0,"currency_code":"USD","in_stock":true}],"thumbnail_url":"\/\/cdn.shopify.com\/s\/files\/1\/0949\/7424\/7277\/files\/A-350_gr.gif?v=1778544410","url":"https:\/\/www.ebiohippo.com\/products\/act-132577-bhb21300025","provider":"BioHippo","version":"1.0","type":"link"}