| 详情描述 |
P2Y1受体的竞争性拮抗剂,MRS 2179是一种有效的,选择性的,竞争性的P2Y1受体拮抗剂,Kb为100 nM;在P2Y2,P2Y4或P2Y6受体(>30 uM)上没有显示出明显的活性;抑制ADP诱导的血小板形状变化,聚集和Ca2+升高但没有对ADP诱导的腺苷酸环化酶抑制的影响;降低小鼠的血小板计数。
<strong>化学名</strong>: 2'-Deoxy-N6-methyladenosine 3',5'-bisphosphate tetrasodium salt
<strong>生物活性</strong>: MRS 2179 tetrasodium salt is a competitive antagonist at P2Y1 receptors (KB = 100 nM). Selective over P2X1 (IC50 = 1.15 μM), P2X3 (IC50 = 12.9 μM), P2X2, P2X4, P2Y2, P2Y4 and P2Y6 receptors. Inhibits the upregulation of NTPDase1 by ATPγS.
<strong>技术参数:</strong>
分子量513.16
公式C11H13N5O9P2Na4
储存Store at -20°C
纯度≥98% (HPLC)
CAS Number1454889-37-2
Physical Appearance: White solid
Solubility: water to 50 mM
<table id="ds_solubility_tbl" class="table table-bordered" style="border-spacing: 0px; border-collapse: collapse; width: 782px; max-width: 100%; margin-bottom: 0px; border: 1px solid #dddddd; color: #333333; font-family: arial, sans-serif; font-size: 14px; text-indent: 0px; height: 45px;">
<tbody style="box-sizing: border-box;">
<tr style="box-sizing: border-box;"><th style="box-sizing: border-box; padding: 8px; text-align: left; line-height: 1.42857; vertical-align: top; border: 1px solid #dddddd;">溶剂</th><th style="box-sizing: border-box; padding: 8px; text-align: left; line-height: 1.42857; vertical-align: top; border: 1px solid #dddddd;">最高浓度 mg/mL</th><th style="box-sizing: border-box; padding: 8px; text-align: left; line-height: 1.42857; vertical-align: top; border: 1px solid #dddddd;">最高浓度 mM</th></tr>
<tr style="box-sizing: border-box;"><th class="solubility_text" style="box-sizing: border-box; padding: 8px; text-align: left; vertical-align: top; line-height: 1.42857; border: 1px solid #dddddd;" rowspan="2">溶解性</th></tr>
<tr style="box-sizing: border-box;">
<td style="box-sizing: border-box; padding: 8px; line-height: 1.42857; vertical-align: top; border: 1px solid #dddddd;">water</td>
<td style="box-sizing: border-box; padding: 8px; line-height: 1.42857; vertical-align: top; border: 1px solid #dddddd;">25.66</td>
<td style="box-sizing: border-box; padding: 8px; line-height: 1.42857; vertical-align: top; border: 1px solid #dddddd;">50</td>
</tr>
</tbody>
</table>
<h2 style="box-sizing: border-box; font-family: arial, sans-serif; line-height: 1; color: #005f9e; margin-top: 0px; margin-bottom: 10px; font-size: 22px;"><span style="font-size: medium;"> </span></h2>
<h2 style="box-sizing: border-box; font-family: arial, sans-serif; line-height: 1; color: #005f9e; margin-top: 0px; margin-bottom: 10px; font-size: 22px;"><span style="color: #000000; font-size: medium;">制备储备液 for MRS 2179 tetrasodium salt</span></h2>
<p style="box-sizing: border-box; margin: 0px 0px 10px; font-size: 14px; color: #333333; font-family: arial, sans-serif;">以下数据基于<span id="ss_type" style="box-sizing: border-box;">产品</span>分子量 <span id="ss_mwt" style="box-sizing: border-box;">513.16</span>。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
<form class="form-inline" style="box-sizing: border-box; color: #333333; font-family: arial, sans-serif; font-size: 14px;">
<div class="form-group" style="box-sizing: border-box; margin-bottom: 0px; display: inline-block; position: relative; height: auto; overflow: visible; vertical-align: middle;">选择批次从而根据批次分子量重新计算:
<div class="select_wrapper" style="box-sizing: border-box; display: inline-block !important; position: relative; max-width: 100%; width: auto; min-width: 50px; height: 30px !important; background: #eeeeee; border-color: #a9a9a9; vertical-align: middle !important; margin: 0px 10px;"><select id="ss_select" class="form-control input-sm" style="margin: 0px; font-style: inherit; font-variant: inherit; font-weight: inherit; font-stretch: inherit; font-size: 14px; line-height: 16px; font-family: inherit; color: #555555; max-width: 100%; width: 110px; background-image: initial; background-position: initial; background-size: initial; background-repeat: initial; background-attachment: initial; background-origin: initial; background-clip: initial; border-color: #a9a9a9; border-radius: 4px; box-shadow: rgba(0, 0, 0, 0.075) 0px 1px 1px inset; transition: border-color 0.15s ease-in-out 0s, box-shadow 0.15s ease-in-out 0s; min-width: 50px; appearance: none; text-indent: 1px; position: initial; z-index: 2; height: 30px !important; padding: 5px 25px 5px 5px !important; vertical-align: middle !important;" name="batch">
<option style="box-sizing: border-box; background: #eeeeee;" value="513.16" data-filtered="filtered"></option>
<option style="box-sizing: border-box; background: #eeeeee;" value="493.35" data-filtered="filtered">3</option>
<option style="box-sizing: border-box; background: #eeeeee;" value="493.35" data-filtered="filtered">4</option>
<option style="box-sizing: border-box; background: #eeeeee;" value="585.22" data-filtered="filtered">5</option>
<option style="box-sizing: border-box; background: #eeeeee;" value="639.27" data-filtered="filtered">6</option>
<option style="box-sizing: border-box; background: #eeeeee;" value="513.16" data-filtered="filtered">7</option>
<option style="box-sizing: border-box; background: #eeeeee;" value="576.21" data-filtered="filtered">8</option>
<option style="box-sizing: border-box; background: #eeeeee;" value="576.21" data-filtered="filtered">9</option>
</select></div>
<button id="recalc_stock_soln_data" class="btn btn-quinary" style="margin: 0px; font-style: inherit; font-variant: inherit; font-stretch: inherit; font-size: 13px; line-height: 15px; font-family: inherit; color: #0084a9; overflow: visible; appearance: button; cursor: pointer; vertical-align: middle; touch-action: manipulation; user-select: none; background-image: none; border-width: 1px; border-style: solid; border-color: #0084a9; background-color: #ffffff; transition: all 0.3s ease-out 0s; font-weight: 700 !important; padding: 6px 7px !important; border-radius: 4px !important; height: 30px !important;">重新计算</button></div>
</form>
<table class="table table-bordered" style="border-spacing: 0px; border-collapse: collapse; width: 847px; max-width: 100%; margin-bottom: 20px; border: 1px solid #dddddd; margin-top: 15px; color: #333333; font-family: arial, sans-serif; font-size: 14px; text-indent: 0px;">
<tbody style="box-sizing: border-box;">
<tr style="box-sizing: border-box;"><th style="box-sizing: border-box; padding: 8px; text-align: left; line-height: 1.42857; vertical-align: top; border: 1px solid #dddddd;">浓度/溶剂体积/质量</th><th style="box-sizing: border-box; padding: 8px; text-align: left; line-height: 1.42857; vertical-align: top; border: 1px solid #dddddd;">1 mg</th><th style="box-sizing: border-box; padding: 8px; text-align: left; line-height: 1.42857; vertical-align: top; border: 1px solid #dddddd;">5 mg</th><th style="box-sizing: border-box; padding: 8px; text-align: left; line-height: 1.42857; vertical-align: top; border: 1px solid #dddddd;">10 mg</th></tr>
<tr style="box-sizing: border-box;">
<td style="box-sizing: border-box; padding: 8px; line-height: 1.42857; vertical-align: top; border: 1px solid #dddddd;">0.5 mM</td>
<td id="ss_0_5_1" style="box-sizing: border-box; padding: 8px; line-height: 1.42857; vertical-align: top; border: 1px solid #dddddd;">3.9 mL</td>
<td id="ss_0_5_5" style="box-sizing: border-box; padding: 8px; line-height: 1.42857; vertical-align: top; border: 1px solid #dddddd;">19.49 mL</td>
<td id="ss_0_5_10" style="box-sizing: border-box; padding: 8px; line-height: 1.42857; vertical-align: top; border: 1px solid #dddddd;">38.97 mL</td>
</tr>
<tr style="box-sizing: border-box;">
<td style="box-sizing: border-box; padding: 8px; line-height: 1.42857; vertical-align: top; border: 1px solid #dddddd;">2.5 mM</td>
<td id="ss_2_5_1" style="box-sizing: border-box; padding: 8px; line-height: 1.42857; vertical-align: top; border: 1px solid #dddddd;">0.78 mL</td>
<td id="ss_2_5_5" style="box-sizing: border-box; padding: 8px; line-height: 1.42857; vertical-align: top; border: 1px solid #dddddd;">3.9 mL</td>
<td id="ss_2_5_10" style="box-sizing: border-box; padding: 8px; line-height: 1.42857; vertical-align: top; border: 1px solid #dddddd;">7.79 mL</td>
</tr>
<tr style="box-sizing: border-box;">
<td style="box-sizing: border-box; padding: 8px; line-height: 1.42857; vertical-align: top; border: 1px solid #dddddd;">5 mM</td>
<td id="ss_5_1" style="box-sizing: border-box; padding: 8px; line-height: 1.42857; vertical-align: top; border: 1px solid #dddddd;">0.39 mL</td>
<td id="ss_5_5" style="box-sizing: border-box; padding: 8px; line-height: 1.42857; vertical-align: top; border: 1px solid #dddddd;">1.95 mL</td>
<td id="ss_5_10" style="box-sizing: border-box; padding: 8px; line-height: 1.42857; vertical-align: top; border: 1px solid #dddddd;">3.9 mL</td>
</tr>
<tr style="box-sizing: border-box;">
<td style="box-sizing: border-box; padding: 8px; line-height: 1.42857; vertical-align: top; border: 1px solid #dddddd;">25 mM</td>
<td id="ss_25_1" style="box-sizing: border-box; padding: 8px; line-height: 1.42857; vertical-align: top; border: 1px solid #dddddd;">0.08 mL</td>
<td id="ss_25_5" style="box-sizing: border-box; padding: 8px; line-height: 1.42857; vertical-align: top; border: 1px solid #dddddd;">0.39 mL</td>
<td id="ss_25_10" style="box-sizing: border-box; padding: 8px; line-height: 1.42857; vertical-align: top; border: 1px solid #dddddd;">0.78 mL<br /><br /></td>
</tr>
</tbody>
</table>
<span style="font-size: medium;"><strong>参考文献</strong></span>
<p style="box-sizing: border-box; margin: 0px 0px 10px; font-size: 14px; color: #333333; font-family: arial, sans-serif;"><em style="box-sizing: border-box;">参考文献是支持产品生物活性的出版物。</em>
<p style="box-sizing: border-box; margin: 0px 0px 10px; font-size: 14px; color: #333333; font-family: arial, sans-serif;"><span class="highlight" style="box-sizing: border-box; font-weight: bold;">Boyer</span> <em style="box-sizing: border-box;">et al</em> (1998) <a style="box-sizing: border-box; background-color: transparent; text-decoration-line: none; color: #7092b1 !important;" title="View abstract" href="https://www.ncbi.nlm.nih.gov/pubmed/9630335" rel="nofollow" target="_blank">Competitive and selective antagonism of P2Y<span style="box-sizing: border-box; position: relative; font-size: 12px; line-height: 0; vertical-align: baseline; bottom: -0.25em;">1</span> receptors by <em style="box-sizing: border-box;">N</em><span style="box-sizing: border-box; position: relative; font-size: 12px; line-height: 0; vertical-align: baseline; top: -0.5em;">6</span>-methyl 2'-deoxyadenosine 3',5'-bisphosphate. </a>Br.J.Pharmacol. <span style="box-sizing: border-box; font-weight: bold;"><em style="box-sizing: border-box;">124</em></span> 1 PMID: 9630335
<p style="box-sizing: border-box; margin: 0px 0px 10px; font-size: 14px; color: #333333; font-family: arial, sans-serif;"><span class="highlight" style="box-sizing: border-box; font-weight: bold;">Lu</span> <em style="box-sizing: border-box;">et al</em> (2007) <a style="box-sizing: border-box; background-color: transparent; text-decoration-line: none; color: #7092b1 !important;" title="View abstract" href="https://www.ncbi.nlm.nih.gov/pubmed/17626796" rel="nofollow" target="_blank">Stimulation of the P2Y<span style="box-sizing: border-box; position: relative; font-size: 12px; line-height: 0; vertical-align: baseline; bottom: -0.25em;">1</span> receptor up-regulates nucleoside-triphosphate diphosphohydrolase-1 in human retinal pigment epithelial cells. </a>J.Pharmacol.Exp.Ther. <span style="box-sizing: border-box; font-weight: bold;"><em style="box-sizing: border-box;">323</em></span> 157 PMID: 17626796
<p style="box-sizing: border-box; margin: 0px 0px 10px; font-size: 14px; color: #333333; font-family: arial, sans-serif;"><span class="highlight" style="box-sizing: border-box; font-weight: bold;">Nandanan</span> <em style="box-sizing: border-box;">et al</em> (2000) <a style="box-sizing: border-box; background-color: transparent; text-decoration-line: none; color: #7092b1 !important;" title="View abstract" href="https://www.ncbi.nlm.nih.gov/pubmed/10715151" rel="nofollow" target="_blank">Synthesis, biological activity, and molecular modeling of ribose-modified deoxyadenosine bisphosphate analogues as P2Y<span style="box-sizing: border-box; position: relative; font-size: 12px; line-height: 0; vertical-align: baseline; bottom: -0.25em;">1</span> receptor ligands. </a>J.Med.Chem. <span style="box-sizing: border-box; font-weight: bold;"><em style="box-sizing: border-box;">43</em></span> 829 PMID: 10715151
<p style="box-sizing: border-box; margin: 0px 0px 10px; font-size: 14px; color: #333333; font-family: arial, sans-serif;"><span class="highlight" style="box-sizing: border-box; font-weight: bold;">Brown</span> <em style="box-sizing: border-box;">et al</em> (2000) <a style="box-sizing: border-box; background-color: transparent; text-decoration-line: none; color: #7092b1 !important;" title="View abstract" href="https://www.ncbi.nlm.nih.gov/pubmed/22791931" rel="nofollow" target="_blank">Activity of novel adenine nucleotide derivatives as agonists and antagonists at recombinant rat P2X receptors. </a>Drug Dev.Res. <span style="box-sizing: border-box; font-weight: bold;"><em style="box-sizing: border-box;">49</em></span> 253 PMID: 22791931
<p style="box-sizing: border-box; margin: 0px 0px 10px; font-size: 14px; color: #333333; font-family: arial, sans-serif;"><span class="highlight" style="box-sizing: border-box; font-weight: bold;">Nandanan</span> <em style="box-sizing: border-box;">et al</em> (1999) <a style="box-sizing: border-box; background-color: transparent; text-decoration-line: none; color: #7092b1 !important;" title="View abstract" href="https://www.ncbi.nlm.nih.gov/pubmed/10229631" rel="nofollow" target="_blank">Structure-activity relationships of bisphosphate nucleotide derivatives as P2Y<span style="box-sizing: border-box; position: relative; font-size: 12px; line-height: 0; vertical-align: baseline; bottom: -0.25em;">1</span> receptor antagonists and partial agonists. </a>J.Med.Chem. <span style="box-sizing: border-box; font-weight: bold;"><em style="box-sizing: border-box;">42</em></span> 1625 PMID: 10229631
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