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重组蛋白

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Delcasertib (Synonyms: KAI-9803; BMS-875944)

目录号: HY-106262: Data Sheet SDS COA 产品使用指南
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Delcasertib (KAI-9803) 是有效，选择性的 δ 蛋白激酶C (δPKC) 抑制剂。Delcasertib (KAI-9803) 可改善急性心肌梗死动物模型的缺血再灌注损伤。

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该游离形式化合物不稳定，推荐具有相同生物学活性的稳定盐形式 Delcasertib hydrochloride。

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MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

Custom Peptide Synthesis

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Delcasertib Chemical Structure

CAS No. : 949100-39-4

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1. 客户无需承担相应的运输费用。

2. 同一机构（单位）同一产品试用装仅限申领一次，同一机构（单位）一年内

可免费申领三个不同产品的试用装。

3. 试用装只面向终端客户。

规格		是否有货
25 mg		询价
50 mg		询价

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Customer Review

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Other Forms of Delcasertib:

Delcasertib hydrochloride In-stock

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Delcasertib 相关抗体

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MCE 顾客使用本产品发表的 3 篇科研文献

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Delcasertib 相关产品

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•同靶点产品:

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•同靶点蛋白产品:

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查看 PKC 亚型特异性产品:

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生物活性
纯度 & 产品资料
参考文献

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生物活性

Delcasertib (KAI-9803) is a potent and selective δ-protein kinase C (δPKC) inhibitor. Delcasertib (KAI-9803) could ameliorate injury associated with ischemia and reperfusion in animal models of acute myocardial infarction (MI)^[1]^[2].

IC₅₀ & Target^[1]

δPKC

体外研究
(In Vitro)

Delcasertib (KAI-9803) 由一种选择性 δ-蛋白激酶 C (δPKC) 抑制肽组成，该抑制肽源自 δPKC 的 δV1-1 部分 (称为“货物肽”)，并通过二硫键可逆地与细胞穿透肽 11-氨基酸结合，细胞穿透肽富含精氨酸的 HIV 1 型反式激活蛋白序列 (TAT47–57；称为“载体肽”)^[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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Delcasertib 相关抗体:

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体内研究
(In Vivo)

Delcasertib (KAI-9803，单次腹腔注射) 在小鼠中导致选择性抑制肝、肾、肺、心脏和脑中的 PKC 易位^[1]。
Delcasertib (KAI-9803) 在急性心肌梗死大鼠模型中被发现在缺血末期给药可减少缺血再灌注引起的心脏损伤^[1]。
Delcasertib (KAI-9803) 已被研究用于预防急性心肌梗死后接受血管成形术的患者的再灌注损伤^[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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Animal Model:	Six-week-old male Crl:CD(SD) rats^[1].
Dosage:	1 mg/kg (Pharmacokinetic Analysis).
Administration:	Via the femoral vein.
Result:	The distribution to tissues such as the liver, kidney, and heart is facilitated by the reversible conjugation to TAT47-57.

Clinical Trial

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分子量

2880.28

Formula

C₁₂₀H₁₉₉N₄₅O₃₄S₂

CAS 号

949100-39-4

性状

固体

颜色

White to off-white

Sequence Shortening

Sequence 1:CYGRKKRRQRRR;Sequence 1':CSFNSYELGSL (Disulfide bridge:Cys1-Cys1’)

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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Sealed storage, away from moisture

Powder	-80°C	2 years
	-20°C	1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据

class="ss-title solution-tit" id="solution-tit" style="font-style: normal">细胞实验： class="ss-vitro solution-vitro">

DMSO 中的溶解度 : ≥ 100 mg/mL (34.72 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

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浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	0.3472 mL	1.7359 mL	3.4719 mL
5 mM	0.0694 mL	0.3472 mL	0.6944 mL
10 mM	0.0347 mL	0.1736 mL	0.3472 mL

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* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

class="molarity-calculator"> class="cpd-cal-tit molarity-tit" id="compoundCalTit">

摩尔计算器
稀释计算器

class="cpd-cal-con molarity-con" id="compoundCalCon"> class="cpd-cal-div"> class="calculator-brief" style="padding-left: 0">

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

style="height: 20px;"> id="errorInfoM" style="color:red;font-size: 12px;"> class="cpd-cal-div dis-hide"> class="calculator-brief p-dulition" style="padding-left: 0;">

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

class="calculator-new-box">

浓度 _(start) class="after-line">

体积 _(start) class="after-line">

浓度 _(final) class="after-line">

体积 _(final) class="after-line">

style="height: 20px;"> id="errorInfo" class="errortip-new" style="color:red; font-size: 12px;"> class="ss-title solution-tit" style="font-style: normal">动物实验： class="ss-vivo" style="padding: 6px 0 7px 0;"> style="padding:2px 14px 0;">

请根据您的实验动物和给药方式选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

class="invivo-step invivo-step-new">
class="ss-vivo-order step-tit">方案一
class="ss-vivo-text ss-vivo-text-new">
请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 7.69 mg/mL (2.67 mM); 澄清溶液

class="invivo-brief invivo-brief-new">
此方案可获得 ≥ 7.69 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 76.9 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
class='f12'>生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
class="invivo-step invivo-step-new">
class="ss-vivo-order step-tit">方案二
class="ss-vivo-text ss-vivo-text-new">
请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (0.87 mM); 澄清溶液

class="invivo-brief invivo-brief-new">
此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
class='f12'>2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
class="invivo-step invivo-step-new">
class="ss-vivo-order step-tit">方案三
class="ss-vivo-text ss-vivo-text-new">
请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (0.87 mM); 澄清溶液

class="invivo-brief invivo-brief-new">
此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

class="ss-vivo" style="padding: 6px 0 7px 0;"> id="c-qrcode-box" style="position: relative; display: none;"> class="qrcode-box"> id="qrcode" data-qrcode="HY-106262">

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动物溶解方案

id="solCalcWrapper"> class="a-solution-item">动物溶解方案计算器 class="a-scheme"> class="a-scheme-tit">请输入动物实验的基本信息： class="calculator-form c-flex-form"> style="display: flex"> class="c-form-item">

给药剂量

mg/kg class="c-form-item">

动物的平均体重

g class="c-form-item">

每只动物的给药体积

μL class="c-form-item">

动物数量

只 class="c-tip">由于实验过程有损耗，建议您多配一只动物的量 class="a-scheme a-matching"> class="a-matching-tit">请输入您的动物体内配方组成： class="calculator-form c-flex-form" style="align-items: center; padding-bottom: 7px;justify-content: flex-start; flex-flow: row nowrap;"> style="position:relative;"> % DMSO + style="position: relative;"> % class="c-form-item" style="display: flex; align-items: center;" data-bind="if: opCount() > 2"> + style="position: relative; margin-right: 5px;"> % Tween-80 + style="position: relative;"> % Saline 如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。 style="margin: 10px 0;"> 方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。 class="a-scheme a-matching" style="padding-top: 0;"> > data-bind="text: lastError" class="error"> class="btn-list"> class="calculator-form" data-bind="if: isWorkConcVisible" style="padding: 5px 12px 0; margin-bottom: 0; box-sizing: border-box; overflow: visible;"> class="result-tit">计算结果 class="line"> class="result" style="margin-top: 15px;display: flex; flex-wrap: wrap;"> 工作液所需浓度 : mg/mL class="calculator-form" data-bind="if: isStepVisible" style="padding: 0 12px; margin-bottom: 0; margin-top: 0; box-sizing: border-box; overflow: visible;"> class="result" style="display: flex; flex-wrap: wrap; margin-top: 10px;"> 储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

class="result-tip" style="position: relative;" data-bind="if: storeConc() > 100.0"> 您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。 class="tooltip-panel normal-saline-div-6" style="left: 535.453px; top: 23px; position: absolute; display: none; line-height: 24px; margin-left: -40px; padding-top: 5px; margin-top: -5px;"> class="tooltip-arrowup"> class="tooltip-container"> 免费服务热线：400-820-3792
E-mail：sales@hg.y866.cn/biomolecule
技术支持电话：021-58950656
技术支持邮箱：tech@hg.y866.cn/biomolecule class="result" style="margin-top: 10px; position:relative; display: flex; flex-wrap: wrap;"> 动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。 class="tooltip-panel normal-saline-div-5" style="left: 315.453px; top: 49.6562px; position: absolute; display: none; line-height: 24px;"> class="tooltip-arrowup"> class="tooltip-container"> 将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液 data-bind="if: isWorkCornOil">连续给药周期超过半月以上，请谨慎选择该方案。 class="result-tip lh24"> 请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

> class="details_batch">

纯度: 98.21%

选择批次： class="details_info_doc"> Data Sheet (654 KB) SDS (252 KB)

COA (302 KB) RP-HPLC (176 KB) 元素分析报告 (225 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Miyaji Y, et al. Distribution of KAI-9803, a novel δ-protein kinase C inhibitor, after intravenous administration to rats. Drug Metab Dispos. 2011 Oct;39(10):1946-53. [Content Brief]

[2]. Bates E, et al. Intracoronary KAI-9803 as an adjunct to primary percutaneous coronary intervention for acute ST-segment elevation myocardial infarction. Circulation. 2008 Feb 19;117(7):886-96. [Content Brief]

class="details_info hide" id="pro_info_4"> class="details_info hide" id="pro_info_5">

[1]. Miyaji Y, et al. Distribution of KAI-9803, a novel δ-protein kinase C inhibitor, after intravenous administration to rats. Drug Metab Dispos. 2011 Oct;39(10):1946-53.

[2]. Bates E, et al. Intracoronary KAI-9803 as an adjunct to primary percutaneous coronary intervention for acute ST-segment elevation myocardial infarction. Circulation. 2008 Feb 19;117(7):886-96.

class="detail_pro_fea levelMaps"> class="details_h2">

Delcasertib 相关分类

class="recommendations_pro"> class="recommendations_pro_map recommendations_protein_con" > class="classify-container">

Inflammation/Immunology Cardiovascular Disease

> id="stock-solution-complete" style="margin: 0;"> class="details_h2" style=" font-size: 14px; border-bottom: 0;" class="solution-table">

完整储备液配制表

class="ss-table"> id="stock-solution-tips" class="ss-table-tip">

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	0.3472 mL	1.7359 mL	3.4719 mL	8.6797 mL
	5 mM	0.0694 mL	0.3472 mL	0.6944 mL	1.7359 mL
	10 mM	0.0347 mL	0.1736 mL	0.3472 mL	0.8680 mL
	15 mM	0.0231 mL	0.1157 mL	0.2315 mL	0.5786 mL
	20 mM	0.0174 mL	0.0868 mL	0.1736 mL	0.4340 mL
	25 mM	0.0139 mL	0.0694 mL	0.1389 mL	0.3472 mL
	30 mM	0.0116 mL	0.0579 mL	0.1157 mL	0.2893 mL

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data-bind="click: $root.toggleFaq"> Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Delcasertib949100-39-4KAI-9803 BMS-875944KAI9803KAI 9803BMS875944BMS 875944BMS-875944PKCProtein kinase CInhibitorinhibitorinhibit

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