{"product_id":"aprocitentan-bhb21902323","title":"Aprocitentan","description":"\u003cdiv class=\"bhp-desc\"\u003e\n\u003cstyle\u003e.bhp-desc{font-size:16px;color:#1a1a1a;line-height:1.7}.bhp-desc h2{font-size:18px;font-weight:700;color:#003366;margin:24px 0 10px;padding-bottom:6px;border-bottom:2px solid #003366}.bhp-desc p{margin:0 0 12px}.bhp-desc .bhp-spec-table{width:100%;border-collapse:collapse;margin:12px 0 18px}.bhp-desc .bhp-spec-table th{width:36%;text-align:left;padding:8px 12px;background:#e8f0fb;color:#003366;font-weight:600;vertical-align:top;border:1px solid #ccd9f0}.bhp-desc .bhp-spec-table td{padding:8px 12px;vertical-align:top;border:1px solid #ccd9f0}.bhp-desc .bhp-warning-box{background:#fff8e6;border-left:4px solid #e6a817;padding:10px 14px;margin:10px 0 14px;border-radius:0 4px 4px 0}.bhp-desc .bhp-cat-pill{display:inline-block;background:#003366;color:#fff;border-radius:20px;padding:3px 12px;font-size:13px;margin-bottom:10px}\u003c\/style\u003e\n\u003cspan class=\"bhp-cat-pill\"\u003eAntagonists\u003c\/span\u003e\u003ch2\u003eCompound Overview\u003c\/h2\u003e\n\u003cp\u003eAprocitentan, also known as ACT-132577, is the major, pharmacologically active metabolite of macitentan. It is an orally active dual ETA\/ETB antagonist with IC\u003csub\u003e50\u003c\/sub\u003e values of 3.4 nM and 987 nM and pA2 values of 6.7 and 5.5, respectively, and it functions as an antihypertensive agent\u003csup\u003e[1]\u003c\/sup\u003e. It is supplied as a white to off-white solid (C16H14Br2N6O4S, MW 546.19) at 99.55% purity.\u003c\/p\u003e\n\u003ch2\u003ePhysical \u0026amp; Chemical Properties\u003c\/h2\u003e\n\u003ctable class=\"bhp-spec-table\"\u003e\u003ctbody\u003e\n\u003ctr\u003e\n\u003cth\u003eCAS Number\u003c\/th\u003e\n\u003ctd\u003e1103522-45-7\u003c\/td\u003e\n\u003c\/tr\u003e\n\u003ctr\u003e\n\u003cth\u003eMolecular Formula\u003c\/th\u003e\n\u003ctd\u003eC16H14Br2N6O4S\u003c\/td\u003e\n\u003c\/tr\u003e\n\u003ctr\u003e\n\u003cth\u003eMolecular Weight\u003c\/th\u003e\n\u003ctd\u003e546.19 g\/mol\u003c\/td\u003e\n\u003c\/tr\u003e\n\u003ctr\u003e\n\u003cth\u003ePurity\u003c\/th\u003e\n\u003ctd\u003e99.55%\u003c\/td\u003e\n\u003c\/tr\u003e\n\u003ctr\u003e\n\u003cth\u003eAppearance\u003c\/th\u003e\n\u003ctd\u003eSolid\u003c\/td\u003e\n\u003c\/tr\u003e\n\u003ctr\u003e\n\u003cth\u003eColor\u003c\/th\u003e\n\u003ctd\u003eWhite to off-white\u003c\/td\u003e\n\u003c\/tr\u003e\n\u003ctr\u003e\n\u003cth\u003eSMILES\u003c\/th\u003e\n\u003ctd\u003eO=S(N)(NC1=NC=NC(OCCOC2=NC=C(Br)C=N2)=C1C3=CC=C(Br)C=C3)=O\u003c\/td\u003e\n\u003c\/tr\u003e\n\u003ctr\u003e\n\u003cth\u003eTarget\u003c\/th\u003e\n\u003ctd\u003eET A, ET A 6.7 (pA2), ET B, ET B 5.5 (pA2)\u003c\/td\u003e\n\u003c\/tr\u003e\n\u003ctr\u003e\n\u003cth\u003eSignaling Pathway\u003c\/th\u003e\n\u003ctd\u003eGPCR\/G Protein\u003c\/td\u003e\n\u003c\/tr\u003e\n\u003ctr\u003e\n\u003cth\u003eSolubility\u003c\/th\u003e\n\u003ctd\u003eIn Vitro: DMSO: 25 mg\/mL (45.77 mM; Requires sonication and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)\u003c\/td\u003e\n\u003c\/tr\u003e\n\u003ctr\u003e\n\u003cth\u003eStorage\u003c\/th\u003e\n\u003ctd\u003ePowder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 2 years; -20°C, 1 year.\u003c\/td\u003e\n\u003c\/tr\u003e\n\u003ctr\u003e\n\u003cth\u003eShipping\u003c\/th\u003e\n\u003ctd\u003eRoom temperature in continental US; may vary elsewhere.\u003c\/td\u003e\n\u003c\/tr\u003e\n\u003c\/tbody\u003e\u003c\/table\u003e\n\u003ch2\u003eBiological Activity\u003c\/h2\u003e\n\u003ch3 style=\"font-size:16px;font-weight:700;color:#003366;margin:16px 0 8px\"\u003eIC50 \u0026amp; Target\u003csup\u003e[1]\u003c\/sup\u003e\n\u003c\/h3\u003e\n\u003cp\u003e\u003c\/p\u003e\n\u003ctable\u003e\u003ctbody\u003e\u003ctr\u003e\n\u003ctd\u003e\n\u003cp\u003e\u003cspan\u003eET\u003csub\u003eA\u003c\/sub\u003e\u003c\/span\u003e\u003c\/p\u003e\n\u003cp\u003e\u003cspan\u003e3.4 nM (IC\u003csub\u003e50\u003c\/sub\u003e)\u003c\/span\u003e\u003c\/p\u003e\n\u003c\/td\u003e\n\u003ctd\u003e\n\u003cp\u003e\u003cspan\u003eET\u003csub\u003eA\u003c\/sub\u003e\u003c\/span\u003e\u003c\/p\u003e\n\u003cp\u003e\u003cspan\u003e6.7 (pA2)\u003c\/span\u003e\u003c\/p\u003e\n\u003c\/td\u003e\n\u003ctd\u003e\n\u003cp\u003e\u003cspan\u003eET\u003csub\u003eB\u003c\/sub\u003e\u003c\/span\u003e\u003c\/p\u003e\n\u003cp\u003e\u003cspan\u003e987 nM (IC\u003csub\u003e50\u003c\/sub\u003e)\u003c\/span\u003e\u003c\/p\u003e\n\u003c\/td\u003e\n\u003ctd\u003e\n\u003cp\u003e\u003cspan\u003eET\u003csub\u003eB\u003c\/sub\u003e\u003c\/span\u003e\u003c\/p\u003e\n\u003cp\u003e\u003cspan\u003e5.5 (pA2)\u003c\/span\u003e\u003c\/p\u003e\n\u003c\/td\u003e\n\u003c\/tr\u003e\u003c\/tbody\u003e\u003c\/table\u003e\n\u003ch2\u003eLiterature Cited\u003c\/h2\u003e\n\u003cp style=\"font-size:14px;color:#555;margin:0 0 10px\"\u003e\u003cem\u003eSources cited in this description and in the In Vitro \u0026amp; In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.\u003c\/em\u003e\u003c\/p\u003e\n\u003cp\u003e [1]. \u003ca target=\"_blank\" rel=\"noopener\" href=\"http:\/\/www.ncbi.nlm.nih.gov\/pubmed\/18780830\"\u003eIglarz M, et al. Pharmacology of macitentan, an orally active tissue-targeting dual endothelin receptor antagonist. J Pharmacol Exp Ther. 2008 Dec;327(3):736-45.\u003c\/a\u003e\u003c\/p\u003e\n\u003cp\u003e [2]. \u003ca target=\"_blank\" rel=\"noopener\" href=\"https:\/\/www.ncbi.nlm.nih.gov\/pubmed\/26770447\"\u003eZhang J, et al. Pharmacokinetic study of ACT-132577 in rat plasma by ultra performance liquid chromatography-tandem mass spectrometry. Int J Clin Exp Med. 2015 Oct 15;8(10):18420-6\u003c\/a\u003e\u003c\/p\u003e\n\u003ch2\u003eSafety\u003c\/h2\u003e\n\u003cdiv class=\"bhp-warning-box\"\u003e\u003cp\u003e\u003cstrong\u003eFor Research Use Only.\u003c\/strong\u003e Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.\u003c\/p\u003e\u003c\/div\u003e\n\u003c\/div\u003e","brand":"MedChemExpress (MCE)","offers":[{"title":"1 mg","offer_id":67604945863021,"sku":"HY-15895-1MG","price":96.0,"currency_code":"USD","in_stock":true},{"title":"5 mg","offer_id":67605375156589,"sku":"HY-15895-5MG","price":237.0,"currency_code":"USD","in_stock":true},{"title":"10 mg","offer_id":67605375189357,"sku":"HY-15895-10MG","price":342.0,"currency_code":"USD","in_stock":true},{"title":"25 mg","offer_id":67605375222125,"sku":"HY-15895-25MG","price":597.0,"currency_code":"USD","in_stock":true},{"title":"50 mg","offer_id":67605375254893,"sku":"HY-15895-50MG","price":836.0,"currency_code":"USD","in_stock":true},{"title":"100 mg","offer_id":67605375287661,"sku":"HY-15895-100MG","price":1128.0,"currency_code":"USD","in_stock":true},{"title":"200 mg","offer_id":67605375320429,"sku":"HY-15895-200MG","price":0.0,"currency_code":"USD","in_stock":true},{"title":"500 mg","offer_id":67605375353197,"sku":"HY-15895-500MG","price":0.0,"currency_code":"USD","in_stock":true},{"title":"1 mL x 10 mM (in DMSO)","offer_id":67605375385965,"sku":"HY-15895-1MLX10MM","price":285.0,"currency_code":"USD","in_stock":true}],"thumbnail_url":"\/\/cdn.shopify.com\/s\/files\/1\/0949\/7424\/7277\/files\/hy-15895.gif?v=1790973070","url":"https:\/\/www.ebiohippo.com\/products\/aprocitentan-bhb21902323","provider":"BioHippo","version":"1.0","type":"link"}