{"product_id":"gkt136901-hydrochloride-bhb21900069","title":"GKT136901 hydrochloride","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\"\u003eInhibitors\u003c\/span\u003e\u003ch2\u003eCompound Overview\u003c\/h2\u003e\n\u003cp\u003eGKT136901 hydrochloride is a potent, selective and orally active inhibitor of NADPH oxidase NOX1\/4, with K\u003csub\u003ei\u003c\/sub\u003e values of 160 nM and 165 nM, respectively. It also acts as a selective, direct scavenger of peroxynitrite and has anti-inflammatory activity, and can be used to study diabetic nephropathy, stroke, and neurodegeneration\u003csup\u003e[1][2][3]\u003c\/sup\u003e. It is supplied as a light yellow to light brown solid (C19H16Cl2N4O2, MW 403.26) at 99.59% 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\u003e1254507-01-1\u003c\/td\u003e\n\u003c\/tr\u003e\n\u003ctr\u003e\n\u003cth\u003eMolecular Formula\u003c\/th\u003e\n\u003ctd\u003eC19H16Cl2N4O2\u003c\/td\u003e\n\u003c\/tr\u003e\n\u003ctr\u003e\n\u003cth\u003eMolecular Weight\u003c\/th\u003e\n\u003ctd\u003e403.26 g\/mol\u003c\/td\u003e\n\u003c\/tr\u003e\n\u003ctr\u003e\n\u003cth\u003ePurity\u003c\/th\u003e\n\u003ctd\u003e99.59%\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\u003eLight yellow to light brown\u003c\/td\u003e\n\u003c\/tr\u003e\n\u003ctr\u003e\n\u003cth\u003eSMILES\u003c\/th\u003e\n\u003ctd\u003eO=C1N(C2=CC=CC=C2Cl)NC(C1=C(C)N3CC4=NC=CC=C4)=CC3=O.[H]Cl\u003c\/td\u003e\n\u003c\/tr\u003e\n\u003ctr\u003e\n\u003cth\u003eSignaling Pathway\u003c\/th\u003e\n\u003ctd\u003eMetabolic Enzyme\/Protease\u003c\/td\u003e\n\u003c\/tr\u003e\n\u003ctr\u003e\n\u003cth\u003eSolubility\u003c\/th\u003e\n\u003ctd\u003eIn Vitro: DMSO: 62.5 mg\/mL (154.99 mM; Requires sonication; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)\u003cbr\u003eH2O: 4 mg\/mL (9.92 mM; Requires sonication and warming and heat to 60°C)\u003c\/td\u003e\n\u003c\/tr\u003e\n\u003ctr\u003e\n\u003cth\u003eStorage\u003c\/th\u003e\n\u003ctd\u003e4°C, sealed storage, away from moisture. In solvent: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture).\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\"\u003eActivity \u0026amp; Target\u003c\/h3\u003e\n\u003cp\u003eKi: 160 (NOX1), 165 (NOX4)\u003csup\u003e[1]\u003c\/sup\u003e\u003c\/p\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=\"https:\/\/pubmed.ncbi.nlm.nih.gov\/20942471\/\"\u003eLaleu B, et al. First in class, potent, and orally bioavailable NADPH oxidase isoform 4 (Nox4) inhibitors for the treatment of idiopathic pulmonary fibrosis. J Med Chem. 2010 Nov 11;53(21):7715-30.\u003c\/a\u003e\u003c\/p\u003e\n\u003cp\u003e [2]. \u003ca target=\"_blank\" rel=\"noopener\" href=\"https:\/\/pubmed.ncbi.nlm.nih.gov\/27273790\/\"\u003eTeixeira G, et al. Therapeutic potential of NADPH oxidase 1\/4 inhibitors. Br J Pharmacol. 2017 Jun;174(12):1647-1669.\u003c\/a\u003e\u003c\/p\u003e\n\u003cp\u003e [3]. \u003ca target=\"_blank\" rel=\"noopener\" href=\"https:\/\/pubmed.ncbi.nlm.nih.gov\/23848532\/\"\u003eSchildknecht S, et al. The NOX1\/4 inhibitor GKT136901 as selective and direct scavenger of peroxynitrite. Curr Med Chem. 2014;21(3):365-76.\u003c\/a\u003e\u003c\/p\u003e\n\u003cp\u003e [4]. \u003ca target=\"_blank\" rel=\"noopener\" href=\"https:\/\/pubmed.ncbi.nlm.nih.gov\/20630933\/\"\u003eSedeek M, et al. Critical role of Nox4-based NADPH oxidase in glucose-induced oxidative stress in the kidney: implications in type 2 diabetic nephropathy. Am J Physiol Renal Physiol. 2010 Dec;299(6):F1348-58.\u003c\/a\u003e\u003c\/p\u003e\n\u003cp\u003e [5]. \u003ca target=\"_blank\" rel=\"noopener\" href=\"https:\/\/pubmed.ncbi.nlm.nih.gov\/32525001\/\"\u003eHwang JS, et al. GKT136901 protects primary human brain microvascular endothelial cells against methamphetamine-induced blood-brain barrier dysfunction. Life Sci. 2020 Sep 1;256:117917.\u003c\/a\u003e\u003c\/p\u003e\n\u003cp\u003e [6]. \u003ca target=\"_blank\" rel=\"noopener\" href=\"https:\/\/pubmed.ncbi.nlm.nih.gov\/22920224\/\"\u003eSedeek M, et al. Renoprotective effects of a novel Nox1\/4 inhibitor in a mouse model of Type 2 diabetes. Clin Sci (Lond). 2013 Feb;124(3):191-202.\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":"5 mg","offer_id":67604849000813,"sku":"HY-101499A-5MG","price":60.0,"currency_code":"USD","in_stock":true},{"title":"10 mg","offer_id":67605018771821,"sku":"HY-101499A-10MG","price":90.0,"currency_code":"USD","in_stock":true},{"title":"25 mg","offer_id":67605018804589,"sku":"HY-101499A-25MG","price":168.0,"currency_code":"USD","in_stock":true},{"title":"50 mg","offer_id":67605018837357,"sku":"HY-101499A-50MG","price":240.0,"currency_code":"USD","in_stock":true},{"title":"100 mg","offer_id":67605018870125,"sku":"HY-101499A-100MG","price":336.0,"currency_code":"USD","in_stock":true},{"title":"200 mg","offer_id":67605018902893,"sku":"HY-101499A-200MG","price":0.0,"currency_code":"USD","in_stock":true},{"title":"500 mg","offer_id":67605018935661,"sku":"HY-101499A-500MG","price":0.0,"currency_code":"USD","in_stock":true},{"title":"1 mL x 10 mM (in DMSO)","offer_id":67605018968429,"sku":"HY-101499A-1MLX10MM","price":66.0,"currency_code":"USD","in_stock":true}],"thumbnail_url":"\/\/cdn.shopify.com\/s\/files\/1\/0949\/7424\/7277\/files\/hy-101499a.gif?v=1790972873","url":"https:\/\/www.ebiohippo.com\/products\/gkt136901-hydrochloride-bhb21900069","provider":"BioHippo","version":"1.0","type":"link"}