2. Metabolic Enzyme/Protease
  3. Dipeptidyl Peptidase
  4. Teneligliptin hydrobromide

Teneligliptin hydrobromide  (Synonyms: MP-513 hydrobromide)

目录号: HY-14806A 纯度: 99.99% ee.: 100.00%
COA 产品使用指南

摩尔计算器

Teneligliptin hydrobromide (MP-513 hydrobromide) 是一种抗高血压剂，为 β2 肾上腺素能受体 (β2AR) 阻滞剂，具有抗氧化、清除自由基的活性。

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Teneligliptin hydrobromide Chemical Structure

Teneligliptin hydrobromide Chemical Structure

CAS No. : 906093-29-6

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规格 价格 是否有货 数量
Free Sample (0.1 - 0.2 mg)   Apply now  
10 mM * 1 mL in DMSO ￥550
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5 mg ￥343
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10 mg ￥500
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50 mg ￥1500
In-stock
100 mg ￥2200
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500 mg   询价  

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Customer Review

Other Forms of Teneligliptin hydrobromide:

Teneligliptin hydrobromide 相关抗体

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DPP-1 DPP-2 DPP-4 DPP-8 DPP-9

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Teneligliptin (MP-513) hydrobromide is a potent chemotype prolylthiazolidine-based DPP-4 inhibitor, which competitively inhibits human plasma, rat plasma, and human recombinant DPP-4 in vitro, with IC50s of approximately 1 nM.

IC50 & Target

IC50: 1 nM (DPP4)[1]
体外研究
(In Vitro)

Teneligliptin (MP-513) inhibits all these DPP-4 enzymes in a concentration-dependent manner. The IC50s of Teneligliptin for rhDPP-4, human plasma, and rat plasma are 0.889, 1.75, and 1.35 nM, respectively. A study of enzyme inhibition kinetics is conducted for Teneligliptin (MP-513) using Gly-Pro-MCA as the substrate and rhDPP-4 as the enzyme source. Plots based on the Michaelis-Menten equation reveals that Teneligliptin (MP-513) inhibits DPP-4 in a substrate-competitivemanner; the residual sum of squares for competitive and non-competitive models is 0.162 and 0.192, respectively. Ki, Km, and Vmax values are 0.406 nM, 24 μM, and 6.06 nmol/min, respectively. Teneligliptin (MP-513) inhibits the degradation of GLP-1(7-36)amide with an IC50 of 2.92 nM[1].

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

Teneligliptin hydrobromide 相关抗体:
体内研究
(In Vivo)

Oral administration of Teneligliptin (MP-513) in Wistar rats results in the inhibition of plasma DPP-4 with an ED50 of 0.41 mg/kg. Plasma DPP-4 inhibition is sustained even at 24 h after administration of Teneligliptin (MP-513). An oral carbohydrate-loading test in Zucker fatty rats shows that Teneligliptin (MP-513) at ≥0.1 mg/kg increases the maximum increase in plasmaglucagon-like peptide-1 and insulin levels, and reduces glucose excursions. This effect is observed over 12 h after a dose of 1 mg/kg. An oral fat-loading test in Zucker fatty rats also shows that Teneligliptin (MP-513) at 1 mg/kg reduces triglyceride and free fatty acid excursions. In Zucker fatty rats, repeated administration of Teneligliptin (MP-513) for two weeks reduces glucose excursions in the oral carbohydrate-loading test and decreased the plasma levels of triglycerides and free fatty acids under non-fasting conditions. Oral administration of Teneligliptin (MP-513) inhibits plasma DPP-4 in rats in a dose-dependent manner. The ED50 value for Teneligliptin (MP-513) is calculated to be 0.41 mg/kg, while those for Sitagliptin and Vildagliptin, 27.3 and 12.8 mg/kg, respectively[1]. Teneligliptin (MP-513) improves the histopathological appearance of the liver and decreases intrahepatic triglyceride levels in an NAFLD model mouse, which is associated with downregulation of hepatic lipogenesis-related genes due to AMPK activation[2].

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

628.86

Formula

C22H30N6OS.5/2BrH
CAS 号
性状

固体

颜色

Off-white to light brown

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
In Vitro: 

H2O 中的溶解度 : ≥ 200 mg/mL (318.04 mM)

DMSO 中的溶解度 : ≥ 100 mg/mL (159.02 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.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.5902 mL 7.9509 mL 15.9018 mL
5 mM 0.3180 mL 1.5902 mL 3.1804 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。

* 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

  • 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

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

  • 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 (3.98 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。

    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；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 (3.98 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。

    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。

    20% SBE-β-CD in Saline 的配制（4°C，储存一周）：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。

以下溶解方案，请直接配置工作液。建议现用现配，在短期内尽快用完。 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： PBS

    Solubility: 100 mg/mL (159.02 mM); 澄清溶液; 超声助溶

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

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
该产品水溶性佳，请具体参考实测 水 / PBS / Saline 中的溶解度数据。
您所需的储备液浓度超过该产品的实测溶解度，如有需要，请与 MCE 中国技术支持联系。
纯度 & 产品资料

纯度: 99.99% ee.: 100.00%

COA (271 KB) HNMR (196 KB) RP-HPLC (339 KB) NP-HPLC (330 KB) LCMS (290 KB)

产品使用指南 (1538 KB)
参考文献
Animal Administration
[1][2]

Rats[1]
Nine-week-old Wistar rats are randomly divided into 13 groups of eight animals each based on body weight (306.2-374.2 g) and plasma DPP-4 activity. Teneligliptin (MP-513) is orally administered to four groups (0.01, 0.1, 1 and 10 mg/2 mL/kg). Sitagliptin and vildagliptin is orally administered to each four groups (0.1, 1, 10 and 100 mg/kg). Vehicle (0.5% hydroxypropyl methylcellulose) is orally administered to one group. Blood samples are collected from the tail vein with heparinized capillary tubes at 0 h (pre dose) and 0.5, 1, 2, 3, 6, 9, 12, and 24 h (post dose) and centrifuged at 1800 g for 15 min at 4°C. Separated plasma is used for the measurement of DPP-4 activity. For dose-response curve using the maximum effect in each dose, the dose of the inhibitors which produce half of the maximum effect; ED50 are calculated.
Mice[2]
Monosodium glutamate (MSG) is administered into the neonatal ICR mice at birth as a single-dose subcutaneous injection (4 mg/g body weight). Among these mice, males are divided into two groups at 4 weeks of age: the MSG/HFD group (n=6, Group 1) and the MSG/HFD/Teneligliptin (MP-513)-treated group (n=6, Group 2). The mice in Group 2 are administered Teneligliptin (MP-513) (30 mg/kg per day) in the drinking water from 4 weeks of age. The treatment dose of Teneligliptin (MP-513) is determined according to the data from the animal experiments in the drug development process. Although the dose is relatively higher than that for humans in clinical practice, no notable adverse effect is observed in the treatment with the dose for the experimental animal in the process. Both groups are fed HFD from 4-14 weeks of age. At the termination of the experiment (14 weeks of age), all animals are sacrificed by CO2 asphyxiation to analyze hepatic histopathology.

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

Teneligliptin hydrobromide 相关分类

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 / H2O 1 mM 1.5902 mL 7.9509 mL 15.9018 mL 39.7545 mL
5 mM 0.3180 mL 1.5902 mL 3.1804 mL 7.9509 mL
10 mM 0.1590 mL 0.7951 mL 1.5902 mL 3.9754 mL
15 mM 0.1060 mL 0.5301 mL 1.0601 mL 2.6503 mL
20 mM 0.0795 mL 0.3975 mL 0.7951 mL 1.9877 mL
25 mM 0.0636 mL 0.3180 mL 0.6361 mL 1.5902 mL
30 mM 0.0530 mL 0.2650 mL 0.5301 mL 1.3251 mL
40 mM 0.0398 mL 0.1988 mL 0.3975 mL 0.9939 mL
50 mM 0.0318 mL 0.1590 mL 0.3180 mL 0.7951 mL
60 mM 0.0265 mL 0.1325 mL 0.2650 mL 0.6626 mL
80 mM 0.0199 mL 0.0994 mL 0.1988 mL 0.4969 mL
100 mM 0.0159 mL 0.0795 mL 0.1590 mL 0.3975 mL

* 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

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.

Keywords:

Teneligliptin906093-29-6MP-513MP513MP 513Dipeptidyl PeptidaseDPPInhibitorinhibitorinhibit

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