Vonoprazan Fumarate 富马酸沃诺拉赞; TAK-438,99.88%

产品编号:Bellancom-15295| CAS NO:881681-01-2| 分子式:C21H20FN3O6S| 分子量:461.46

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用,

货号 包装 价格 库存与货期 购买量 操作
Bellancom-15295
490.00 杭州 北京(现货)
Bellancom-15295
630.00 杭州 北京(现货)
Bellancom-15295
1250.00 杭州 北京(现货)
Bellancom-15295
1950.00 杭州 北京(现货)

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Vonoprazan Fumarate 富马酸沃诺拉赞; TAK-438

产品介绍 Vonoprazan Fumarate (TAK-438) 是一种质子泵抑制剂 (PPI),是高效的,具有口服活性的钾竞争性酸阻断剂 (potassium-competitive acid blocker (P-CAB)),具有抗分泌活性。在 pH 为 6.5 时,Vonoprazan Fumarate 抑制猪胃微粒体中的 H+,K+-ATPase 酶活性,IC50 值为 19 nM。Vonoprazan Fumarate 被开发用于研究酸相关疾病,如胃食管反流病和消化性溃疡。
生物活性

Vonoprazan Fumarate (TAK-438), a proton pump inhibitor (PPI), is a potent and orally active potassium-competitive acid blocker (P-CAB), with antisecretory activity. Vonoprazan Fumarate inhibits H+,K+-ATPase activity in porcine gastric microsomes with an IC50 of 19 nM at pH 6.5. Vonoprazan Fumarate is developed for the research of acid-related diseases, such as gastroesophageal reflux disease and peptic ulcer disease.

体外研究

Vonoprazan (0.1 nM-10 μM; 30 minutes) exhibits porcine gastric H+ ,K+-ATPase activity in a concentration-dependent manner.
Vonoprazan does not inhibit Na+,K+-ATPase activity, even at concentrations 500 times higher than their IC50 values against gastric H+,K+-ATPase activity.

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

体内研究

Vonoprazan (1-4 mg/kg; p.o.) completely inhibits basal and 2-deoxy-D-glucose (2DG, 200 mg/kg s.c.)-stimulated gastric acid secretion at the 4 mg/kg dose in rats.

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

Animal Model: Male 7- or 8-week-old Sprague-Dawley rat
Dosage: 0.5, 1, 2, and 4 mg/kg
Administration: Oral administration
Result: Inhibited basal gastric acid secretion in a dose-dependent manner.
体内研究

Vonoprazan (1-4 mg/kg; p.o.) completely inhibits basal and 2-deoxy-D-glucose (2DG, 200 mg/kg s.c.)-stimulated gastric acid secretion at the 4 mg/kg dose in rats.

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

Animal Model: Male 7- or 8-week-old Sprague-Dawley rat
Dosage: 0.5, 1, 2, and 4 mg/kg
Administration: Oral administration
Result: Inhibited basal gastric acid secretion in a dose-dependent manner.
性状Solid
溶解性数据
In Vitro: 

DMSO : 50 mg/mL (108.35 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.1670 mL 10.8352 mL 21.6704 mL
5 mM 0.4334 mL 2.1670 mL 4.3341 mL
10 mM 0.2167 mL 1.0835 mL 2.1670 mL
*

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 and light)。-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。

In Vivo:

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

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.42 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.42 mM,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 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液
  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (5.42 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.42 mM,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。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.42 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.42 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    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。

*以上所有助溶剂都可在 西域 网站选购。
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture and light

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

参考文献

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