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Health & Wellness
Topical Nitric oxide-releasing PDE5 inhibitor for wound healing indications.
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<blockquote data-quote="madman" data-source="post: 189978" data-attributes="member: 13851"><p><strong>Table 1. <span style="color: rgb(184, 49, 47)">Inhibition of human recombinant PDE5A1 by TOP-N53, TOP-52, and reference PDE5 inhibitors. </span>IC50 <span style="color: rgb(184, 49, 47)">(half-maximum inhibition)</span> values were calculated from concentration-dependent inhibition curves recorded at 0.5 µM cGMP and shown as means from at least 3 independent experiments. </strong></p><p>[ATTACH=full]11369[/ATTACH]</p><p></p><p></p><p></p><p><em><span style="color: rgb(184, 49, 47)">TOP-52, the active metabolite which is formed together with nitric oxide from TOP-N53 after intracellular bioactivation is a very potent PDE5 inhibitor (Table 1).</span> </em>The increased activity over TOP-N53 can be explained by the additional binding interaction with the polar residuesSer 661 and Gln 663 (Fig. 6). <span style="color: rgb(184, 49, 47)"><strong><u>The intracellular release of locally active nitric oxide together with the very potent PDE5 inhibitor TOP-52 makes Topadur’s newly invented enzyme regulation system unique and led to unprecedented efficacy to elevate intracellular cGMP levels</u>.</strong></span></p><p></p><p></p><p></p><p><span style="color: rgb(0, 0, 0)">TOP-N53 was a potent inhibitor of PDE5 reflected by an IC50 of 1.18 nM.</span><span style="color: rgb(184, 49, 47)"> <strong><u>TOP-52, its main metabolite after the release of NO was revealed to be an even more potent inhibitor of PDE5 with an IC50 of 0.1 nM. In fact, compared with a range of marketed PDE5 inhibitors, TOP-52 was the most potent molecule</u></strong> (Table 1). </span></p><p><span style="color: rgb(184, 49, 47)"></span></p><p><span style="color: rgb(184, 49, 47)"></span></p><p><span style="color: rgb(184, 49, 47)"></span></p><p><span style="color: rgb(184, 49, 47)"><strong><em>*</em></strong></span><span style="color: rgb(0, 0, 0)"><strong><em>In cellular assays, TOP-N53 was by far more effective than its corresponding PDE5 inhibitor TOP-52 or reference PDE5 inhibitors to increase cGMP as exemplified in washed human platelets (Fig. 7), likely reflecting the synergism inherent in TOP-N53 (Fig. 2). </em></strong></span></p></blockquote><p></p>
[QUOTE="madman, post: 189978, member: 13851"] [B]Table 1. [COLOR=rgb(184, 49, 47)]Inhibition of human recombinant PDE5A1 by TOP-N53, TOP-52, and reference PDE5 inhibitors. [/COLOR]IC50 [COLOR=rgb(184, 49, 47)](half-maximum inhibition)[/COLOR] values were calculated from concentration-dependent inhibition curves recorded at 0.5 µM cGMP and shown as means from at least 3 independent experiments. [/B] [ATTACH type="full" alt="Screenshot (2352).png"]11369[/ATTACH] [I][COLOR=rgb(184, 49, 47)]TOP-52, the active metabolite which is formed together with nitric oxide from TOP-N53 after intracellular bioactivation is a very potent PDE5 inhibitor (Table 1).[/COLOR] [/I]The increased activity over TOP-N53 can be explained by the additional binding interaction with the polar residuesSer 661 and Gln 663 (Fig. 6). [COLOR=rgb(184, 49, 47)][B][U]The intracellular release of locally active nitric oxide together with the very potent PDE5 inhibitor TOP-52 makes Topadur’s newly invented enzyme regulation system unique and led to unprecedented efficacy to elevate intracellular cGMP levels[/U].[/B][/COLOR] [COLOR=rgb(0, 0, 0)]TOP-N53 was a potent inhibitor of PDE5 reflected by an IC50 of 1.18 nM.[/COLOR][COLOR=rgb(184, 49, 47)] [B][U]TOP-52, its main metabolite after the release of NO was revealed to be an even more potent inhibitor of PDE5 with an IC50 of 0.1 nM. In fact, compared with a range of marketed PDE5 inhibitors, TOP-52 was the most potent molecule[/U][/B] (Table 1). [B][I]*[/I][/B][/COLOR][COLOR=rgb(0, 0, 0)][B][I]In cellular assays, TOP-N53 was by far more effective than its corresponding PDE5 inhibitor TOP-52 or reference PDE5 inhibitors to increase cGMP as exemplified in washed human platelets (Fig. 7), likely reflecting the synergism inherent in TOP-N53 (Fig. 2). [/I][/B][/COLOR] [/QUOTE]
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Topical Nitric oxide-releasing PDE5 inhibitor for wound healing indications.
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