1. Metabolic Enzyme/Protease
  2. Dipeptidyl Peptidase
  3. Prodipine hydrochloride

Prodipine hydrochloride  (Synonyms: 普罗地平盐酸盐;卜罗哌苯盐酸盐)

目录号: HY-101605 纯度: 99.84%
COA 产品使用指南 技术支持

Prodipine 是一种二苯基膦酸酯衍生物。抑制兔纯化的和血浆中的二肽基肽酶 IV (DPP IV),IC50 分别为 4.5 μM 和 30 μM。

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Prodipine hydrochloride Chemical Structure

Prodipine hydrochloride Chemical Structure

CAS No. : 31314-39-3

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查看 Dipeptidyl Peptidase 亚型特异性产品:

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Prodipine, a diphenyl-phosphonate derivative. The IC50s of Prodipine for purified and plasma Dipeptidyl peptidase IV (DPP IV) from the rabbit are 4.5 μM and 30 μM, respectively.

IC50 & Target

IC50: 4.5 μM (purified DPP IV), 30 μM (plasma DPP IV)[1]

体外研究
(In Vitro)

Prodipine, a diphenyl-phosphonate derivative selected from a group of slow-binding irreversible inhibitors of this enzyme. The IC50 values of Prodipine for purified and plasma DPP IV from the rabbit are 4.5 μM and 30 μM, respectively[1].

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

体内研究
(In Vivo)

Male rabbits weighing 3-4 kg receive a single intravenous injection with 10 mg Prodipine or saline. After 1 hr, plasma DPP IV activity has decreased to less than 20% of the preinjection value and remaines unchanged during a 24 hr observation period. A profound and long-lasting inhibition of plasma DPP IV activity is observed in the treated animals (1, 5 or 10 mg). It takes 5 to 8 days to reach half of the pretreatment DPP IV activity and generally more than 20 days for a complete recovery[1].

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

分子量

315.88

Formula

C20H26ClN

CAS 号
性状

固体

颜色

Off-white to yellow

中文名称

普罗地平盐酸盐;卜罗哌苯盐酸盐

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

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

溶解性数据
细胞实验: 

DMSO 中的溶解度 : 100 mg/mL (316.58 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.1658 mL 15.8288 mL 31.6576 mL
5 mM 0.6332 mL 3.1658 mL 6.3315 mL
查看完整储备液配制表

* 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。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物实验:

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

  • 方案 一

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

    Solubility: ≥ 2.5 mg/mL (7.91 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

    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;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

    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。
  • 方案 二

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

    Solubility: ≥ 2.5 mg/mL (7.91 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

    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。

    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。
动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
请输入您的动物体内配方组成:
%
DMSO +
+
%
Tween-80 +
%
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%。
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。
计算结果
工作液所需浓度 : mg/mL
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)

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。
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
连续给药周期超过半月以上,请谨慎选择该方案。
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

纯度: 99.84%

参考文献
Kinase Assay
[1]

Dipeptidyl peptidase IV activity is determined using the fluorogenic substrate Gly-Pro-4-methoxy-2-naphthylamide. Hydrolysis of L-Ala-4-methoxy-2-naphthylamide in 60 mM phosphate buffer pH 7.4 is chosen for the determination of aminopeptidase M activity. The intramolecularly quenched fluorogenic substrate Lys (2,4 dinitrophenyl)-Pro-Pro-NH-CH2-CH,-NH,-aminobenzoyl-2HCl is used to assay aminopeptidase P activity. Prolyl oligopeptidase (PO) is measured with N-benzyloxycarbonyl-Gly-Pro-7-amino-4-methylcoumarin. One unit of enzymatic activity is defined as the amount of enzyme catalyzing the formation of 1 μmol of assay product per minute under the conditions used[1].

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

Animal Administration
[1]

Rabbits[1]
Male New Zealand white rabbits (3-4 kg) are used.
EXPERIMENT 1 The rabbits (n=1 for each condition) receive a single iv. injection of 10 mg Prodipine or saline. Blood samples are taken 5 min before injection and 30 min, 1 hr, 2 hr, and 24 hr after the treatment.
EXPERIMENT 2 The rabbits (n=1 for each condition) receive a single i.v. bolus injection of saline or are treated with 1, 5, or 10 mg Prodipine (also in a single i.v. bolus) at time 0. The animals are kept under observation for 40 days. At several time points (-5 min, 4 hr, and at days 1, 2, 3, 6, 12, 21, and 40), blood samples are taken and body weight determined. Rabbits are killed with pentobarbital after termination of the observation period.

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

参考文献

完整储备液配制表

* 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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.1658 mL 15.8288 mL 31.6576 mL 79.1440 mL
5 mM 0.6332 mL 3.1658 mL 6.3315 mL 15.8288 mL
10 mM 0.3166 mL 1.5829 mL 3.1658 mL 7.9144 mL
15 mM 0.2111 mL 1.0553 mL 2.1105 mL 5.2763 mL
20 mM 0.1583 mL 0.7914 mL 1.5829 mL 3.9572 mL
25 mM 0.1266 mL 0.6332 mL 1.2663 mL 3.1658 mL
30 mM 0.1055 mL 0.5276 mL 1.0553 mL 2.6381 mL
40 mM 0.0791 mL 0.3957 mL 0.7914 mL 1.9786 mL
50 mM 0.0633 mL 0.3166 mL 0.6332 mL 1.5829 mL
60 mM 0.0528 mL 0.2638 mL 0.5276 mL 1.3191 mL
80 mM 0.0396 mL 0.1979 mL 0.3957 mL 0.9893 mL
100 mM 0.0317 mL 0.1583 mL 0.3166 mL 0.7914 mL
Help & FAQs
  • 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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产品名称:
Prodipine hydrochloride
目录号:
HY-101605
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