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Teneligliptin (MP-513)

别名: 特力利汀;3-[[(2S,4S)-4-[4-(3-甲基-1-苯基-1H-吡唑-5-基)-1-哌嗪基]-2-吡咯烷基]甲酰基]噻唑烷; 特利力汀;替格列汀-D4;特利列汀
目录号: V8225 纯度: ≥98%
COA 产品数据 产品说明书 SDS
Teneligliptin（MP513；日本商品名 Tenelia）是一种新型、有效、口服生物可利用且长效的二肽基肽酶 4 (DPP-4) 抑制剂；它在体外竞争性抑制人血浆、大鼠血浆和人重组 DPP-4，IC50 值约为 1 nM。
Teneligliptin (MP-513) CAS号: 760937-92-6
产品类别: Dipeptidyl Peptidase
产品仅用于科学研究，不针对患者销售
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Other Forms of Teneligliptin (MP-513):

  • 氢溴酸替格列汀
  • 特力利汀氢溴酸盐水合物
  • 特力利汀-D8
  • Teneligliptin-d4
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InvivoChem产品被CNS等顶刊论文引用
产品描述

描述：替格列汀（MP513；在日本以商品名Tenelia销售）是一种新型、高效、口服生物利用度高且作用持久的二肽基肽酶-4 (DPP-4) 抑制剂；体外实验表明，它能竞争性抑制人血浆、大鼠血浆和人重组DPP-4，IC50值约为1 nM。长期使用0.1至3.0 µmol/L剂量的替格列汀治疗不会降低人脐静脉内皮细胞 (HUVEC) 的细胞活力，但能降低高糖应激标志物，并增加高糖培养条件下HUVEC细胞中血红素加氧酶-1 (HMOX1) 基因的表达。替格列汀在日本已获批准用于治疗2型糖尿病。


生物活性&实验参考方法
靶点
Teneligliptin is a dipeptidyl peptidase-4 (DPP-4) inhibitor. [2]
体外研究 (In Vitro)
所有这些DPP-4酶均能被替格列汀（MP-513）以浓度依赖的方式抑制。替格列汀（MP-513）对重组人DPP-4（rhDPP-4）、人血浆和鼠血浆的IC50值分别为0.889 nM、1.75 nM和1.35 nM。在酶抑制动力学研究中，以替格列汀（MP-513）为酶源，Gly-Pro-MCA为底物。根据基于米氏方程的曲线图，替格列汀（MP-513）以底物竞争的方式抑制DPP-4；竞争模型和非竞争模型的残差平方和分别为0.162和0.192。 Ki、Km 和 Vmax 的值分别为 6.06 nmol/min、24 μM 和 0.406 nM。替格列汀 (MP-513) 的 IC50 为 2.92 nM，可抑制 GLP-1(7-36)酰胺的分解[1]。
替格列汀 以浓度依赖的方式竞争性抑制 DPP-4 活性。IC₅₀ 值：对重组人 DPP-4 为 0.889 nmol/L；对人血浆 DPP-4 为 1.75 nmol/L；对大鼠血浆 DPP-4 为 1.35 nmol/L。 [1]
使用重组人 DPP-4 和底物 Gly-Pro-MCA 进行的动力学分析表明，替格列汀是一种竞争性抑制剂，其 Kᵢ = 0.406 nmol/L，Kₘ = 24.0 μmol/L，Vₘₐₓ = 6.06 mmol/min。[1]
替格列汀抑制大鼠血浆中 GLP-1(7-36)酰胺的降解，IC₅₀ 为 2.92 nmol/L。 [1]
体外对比研究表明，替格列汀（对rhDPP-4的IC₅₀ = 1.01 nmol/L，对人血浆的IC₅₀ = 1.45 nmol/L，对大鼠血浆的IC₅₀ = 1.14 nmol/L）的效力高于西格列汀（IC₅₀分别为6.74、4.88和10.4 nmol/L）和维格列汀（IC₅₀分别为10.5、7.67和6.81 nmol/L）。[1]
体内研究 (In Vivo)
替格列汀 (MP-513) 的 ED50 为 0.41 mg/kg，口服给药后可抑制 Wistar 大鼠血浆中的 DPP-4 活性。即使在给药 24 小时后，血浆 DPP-4 活性仍受到抑制。根据口服碳水化合物负荷试验，替格列汀 (MP-513) 在 ≥0.1 mg/kg 剂量下可最大程度地提高 Zucker 脂肪大鼠血浆中胰高血糖素样肽-1 (GLP-1) 和胰岛素水平，并降低血糖波动。在摄入 1 mg/kg 剂量后 12 小时内即可观察到此效应。此外，在 Zucker 脂肪大鼠进行的口服脂肪负荷试验中，替格列汀 (MP-513) 在 1 mg/kg 剂量下可降低甘油三酯和游离脂肪酸的波动。在Zucker肥胖大鼠中，每周两次、连续两周给予替格列汀（MP-513）。该治疗降低了动物非空腹状态下的血浆甘油三酯和游离脂肪酸水平。此外，口服碳水化合物负荷试验中，该治疗也降低了血糖波动。替格列汀（MP-513）的口服治疗以剂量依赖的方式抑制大鼠血浆DPP-4活性。替格列汀（MP-513）的ED50值为0.41 mg/kg，而西格列汀和维格列汀的ED50值分别为27.3 mg/kg和12.8 mg/kg[1]。替格列汀 (MP-513) 与 AMPK 激活引起的肝脏脂肪生成相关基因的下调有关，从而改善 NAFLD 模型小鼠的肝脏组织学外观并降低肝内甘油三酯水平 [2]。在非酒精性脂肪性肝病 (NAFLD) 小鼠模型（喂食高脂饮食的 MSG 处理的新生 ICR 小鼠）中，替格列汀（30 mg/kg/天，溶于饮用水中，持续 10 周）显著降低了肝脏脂肪变性和炎症，NAFLD 活动评分 (NAS) 证实了这一点。[2] - 与对照组小鼠相比，替格列汀显著降低了肝内甘油三酯水平。[2] - 替格列汀显著提高了肝组织中磷酸化 AMPK (p-AMPK) 与总 AMPK 的比值，表明 AMPK 被激活。 [2]
- 替格列汀显著降低了肝脏中脂肪生成相关基因（Acc、Fas、Srebp1c 和 Elovl6）的 mRNA 表达。[2]
- 替格列汀治疗组小鼠血清丙氨酸氨基转移酶 (ALT) 水平显著降低。[2]
- 各组间血清游离脂肪酸 (FFA)、葡萄糖、胰岛素或甘油三酯水平无显著变化。[2]
- 对照组和治疗组小鼠的体重、肝脏重量和白色脂肪组织重量均无显著差异。[2]
酶活实验
DPP-4抑制试验：将DPP-4抑制剂用试验缓冲液稀释至不同浓度。取20 μL抑制剂溶液、20 μL酶源（重组人DPP-4、稀释20倍的人血浆或稀释10倍的大鼠血浆）和20 μL Gly-Pro-MCA（终浓度25 μmol/L）与140 μL（体外）或160 μL（体内）试验缓冲液混合，启动反应。在37℃下反应20分钟（rhDPP-4）或1小时（血浆）后，在360 nm激发波长和465 nm发射波长下测定Gly-Pro-MCA生成的7-氨基-4-甲基香豆素的荧光强度。[1]
DPP-4抑制动力学：在不同浓度的替格列汀和Gly-Pro-MCA作用下测定rhDPP-4活性。采用非线性回归分析抑制模式，模型为米氏方程扩展至竞争性或非竞争性抑制。计算了Log(Kᵢ)、log(Kₘ)和Vₘₐₓ，并通过对数倒数转换计算了Kᵢ和Kₘ的估计值。[1]
GLP-1降解测定：将替格列汀用含0.003% Brij-35溶液和1%牛血清白蛋白的PBS稀释。将5 μL替格列汀溶液或溶剂与175 μL稀释的大鼠血浆（终浓度30%）孵育。加入20 μL GLP-1溶液（终浓度150 pmol/L）启动反应。在37°C下反应1小时后，使用自动微孔板读数仪测定活性GLP-1的浓度。[1]
动物实验
新生ICR小鼠出生时接受单次皮下注射谷氨酸钠（MSG）（4 mg/g体重）。4周龄时，雄性小鼠被分为两组：MSG/高脂饮食（HFD）对照组和MSG/HFD/替格列汀治疗组（每组n = 6）。[2]
- 从4周龄到14周龄，替格列汀以30 mg/kg/天的剂量通过饮用水给予。[2]
- 两组小鼠均从4周龄到14周龄饲喂高脂饮食（HFD）。[2]
- 14周龄时，所有动物均采用二氧化碳窒息法处死。禁食6小时后，从下腔静脉采集血样。取肝组织进行组织病理学、脂质分析和分子检测。 [2]
新生ICR小鼠出生时接受单次皮下注射谷氨酸钠（MSG）（4 mg/g体重）。4周龄时，雄性小鼠被分为两组：MSG/高脂饮食（HFD）对照组和MSG/HFD/替格列汀治疗组（每组n = 6）。[2]
- 从4周龄到14周龄，替格列汀以30 mg/kg/天的剂量通过饮用水给药。[2]
- 两组小鼠均从4周龄到14周龄饲喂高脂饮食（HFD）。[2]
- 14周龄时，所有动物均采用二氧化碳窒息法处死。禁食6小时后，从下腔静脉采集血样。取肝组织进行组织病理学、脂质分析和分子检测。[2]
参考文献

[1]. A novel, potent, and long-lasting dipeptidyl peptidase-4 inhibitor, teneligliptin, improves postprandial hyperglycemia and dyslipidemia after single and repeated administrations. Eur J Pharmacol. 2012 Dec 5;696(1-3):194-202.

[2]. The Dipeptidyl Peptidase-4 Inhibitor Teneligliptin Attenuates Hepatic Lipogenesis via AMPK Activation in Non-Alcoholic Fatty Liver Disease Model Mice. Int J Mol Sci. 2015 Dec 8;16(12):29207-18.
其他信息
替卡利汀是一种氨基酸酰胺。它已被研究用于治疗2型糖尿病。替卡利汀是一种长效、口服生物利用度高的吡咯烷二肽基肽酶-4 (DPP-4) 抑制剂，具有降血糖活性。替卡利汀还可以通过维持GLP-1水平的升高来降低血浆甘油三酯水平。
替格列汀是一种二肽基肽酶-4 (DPP-4) 抑制剂，临床上用于治疗2型糖尿病。[2]
- 该研究表明，替格列汀通过激活AMPK并随后下调脂肪生成基因（Srebp1c、Fas、Acc、Elovl6），改善NAFLD小鼠模型中的肝脂肪变性和炎症。 [2]
- 本研究采用的非酒精性脂肪性肝病（NAFLD）模型包括新生儿注射谷氨酸钠（MSG）联合高脂饮食，可诱导肥胖、胰岛素抵抗和肝脂肪变性。[2]
- 该研究表明，DPP-4抑制剂（如替格列汀）可能具有治疗NAFLD/NASH的潜力。[2]
*注: 文献方法仅供参考, InvivoChem并未独立验证这些方法的准确性
化学信息 & 存储运输条件
分子式
C22H30N6OS
分子量
426.58
精确质量
426.22
CAS号
760937-92-6
相关CAS号
Teneligliptin hydrobromide;906093-29-6;Teneligliptin hydrobromide hydrate;1572583-29-9;Teneligliptin-d8;1391012-95-5;Teneligliptin-d4
PubChem CID
11949652
外观&性状
White to off-white solid powder
密度
1.4±0.1 g/cm3
沸点
663.4±55.0 °C at 760 mmHg
闪点
355.0±31.5 °C
蒸汽压
0.0±2.0 mmHg at 25°C
折射率
1.721
LogP
1.15
tPSA
81.94
氢键供体(HBD)数目
1
氢键受体(HBA)数目
6
可旋转键数目(RBC)
4
重原子数目
30
分子复杂度/Complexity
594
定义原子立体中心数目
2
SMILES
O=C([C@H]1NC[C@@H](N2CCN(C3=CC(C)=NN3C4=CC=CC=C4)CC2)C1)N5CSCC5
InChi Key
WGRQANOPCQRCME-PMACEKPBSA-N
InChi Code
InChI=1S/C22H30N6OS/c1-17-13-21(28(24-17)18-5-3-2-4-6-18)26-9-7-25(8-10-26)19-14-20(23-15-19)22(29)27-11-12-30-16-27/h2-6,13,19-20,23H,7-12,14-16H2,1H3/t19-,20-/m0/s1
化学名
[(2S,4S)-4-[4-(5-methyl-2-phenylpyrazol-3-yl)piperazin-1-yl]pyrrolidin-2-yl]-(1,3-thiazolidin-3-yl)methanone
HS Tariff Code
2934.99.9001
存储方式

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month
运输条件
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
溶解度数据
溶解度 (体外实验)
DMSO : ~33.33 mg/mL (~78.13 mM)
溶解度 (体内实验)
配方 1 中的溶解度: ≥ 2.5 mg/mL (5.86 mM) (饱和度未知) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将100 μL 25.0 mg/mL澄清DMSO储备液加入到400 μL PEG300中，混匀；然后向上述溶液中加入50 μL Tween-80，混匀；加入450 μL生理盐水定容至1 mL。
*生理盐水的制备：将 0.9 g 氯化钠溶解在 100 mL ddH₂O中，得到澄清溶液。
配方 2 中的溶解度: ≥ 2.5 mg/mL (5.86 mM) (饱和度未知) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将 100 μL 25.0 mg/mL澄清DMSO储备液加入900 μL 20% SBE-β-CD生理盐水溶液中，混匀。
*20% SBE-β-CD 生理盐水溶液的制备（4°C，1 周）：将 2 g SBE-β-CD 溶解于 10 mL 生理盐水中，得到澄清溶液。
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配方 3 中的溶解度: ≥ 2.5 mg/mL (5.86 mM) (饱和度未知) in 10% DMSO + 90% Corn Oil (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将 100 μL 25.0 mg/mL 澄清 DMSO 储备液加入到 900 μL 玉米油中并混合均匀。

请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。
制备储备液 1 mg 5 mg 10 mg
1 mM 2.3442 mL 11.7211 mL 23.4423 mL
5 mM 0.4688 mL 2.3442 mL 4.6885 mL
10 mM 0.2344 mL 1.1721 mL 2.3442 mL

1、根据实验需要选择合适的溶剂配制储备液 (母液)：对于大多数产品，InvivoChem推荐用DMSO配置母液 (比如：5、10、20mM或者10、20、50 mg/mL浓度），个别水溶性高的产品可直接溶于水。产品在DMSO 、水或其他溶剂中的具体溶解度详见上”溶解度 (体外)”部分;

2、如果您找不到您想要的溶解度信息，或者很难将产品溶解在溶液中，请联系我们;

3、建议使用下列计算器进行相关计算（摩尔浓度计算器、稀释计算器、分子量计算器、重组计算器等）;

4、母液配好之后，将其分装到常规用量，并储存在-20°C或-80°C，尽量减少反复冻融循环。

计算器
计算 重置

摩尔浓度计算器可计算特定溶液所需的质量、体积/浓度，具体如下：

  • 计算制备已知体积和浓度的溶液所需的化合物的质量
  • 计算将已知质量的化合物溶解到所需浓度所需的溶液体积
  • 计算特定体积中已知质量的化合物产生的溶液的浓度
使用摩尔浓度计算器计算摩尔浓度的示例如下所示：
假如化合物的分子量为350.26 g/mol，在5mL DMSO中制备10mM储备液所需的化合物的质量是多少？
  • 在分子量（MW）框中输入350.26
  • 在“浓度”框中输入10，然后选择正确的单位（mM）
  • 在“体积”框中输入5，然后选择正确的单位（mL）
  • 单击“计算”按钮
  • 答案17.513 mg出现在“质量”框中。以类似的方式，您可以计算体积和浓度。
计算 重置

稀释计算器可计算如何稀释已知浓度的储备液。例如，可以输入C1、C2和V2来计算V1，具体如下：

制备25毫升25μM溶液需要多少体积的10 mM储备溶液？
使用方程式C1V1=C2V2，其中C1=10mM，C2=25μM，V2=25 ml，V1未知：
  • 在C1框中输入10，然后选择正确的单位（mM）
  • 在C2框中输入25，然后选择正确的单位（μM）
  • 在V2框中输入25，然后选择正确的单位（mL）
  • 单击“计算”按钮
  • 答案62.5μL（0.1 ml）出现在V1框中
g/mol
计算 重置

分子量计算器可计算化合物的分子量 (摩尔质量)和元素组成，具体如下：

注：化学分子式大小写敏感：C12H18N3O4  c12h18n3o4
计算化合物摩尔质量（分子量）的说明：
  • 要计算化合物的分子量 (摩尔质量)，请输入化学/分子式，然后单击“计算”按钮。
分子质量、分子量、摩尔质量和摩尔量的定义：
  • 分子质量（或分子量）是一种物质的一个分子的质量，用统一的原子质量单位（u）表示。（1u等于碳-12中一个原子质量的1/12）
  • 摩尔质量（摩尔重量）是一摩尔物质的质量，以g/mol表示。
/
计算 重置

配液计算器可计算将特定质量的产品配成特定浓度所需的溶剂体积 (配液体积)

  • 输入试剂的质量、所需的配液浓度以及正确的单位
  • 单击“计算”按钮
  • 答案显示在体积框中
动物体内实验配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
第二步：请输入动物体内配方组成（配方适用于不溶/难溶于水的化合物），不同的产品和批次配方组成不同，如对配方有疑问，可先联系我们提供正确的体内实验配方。此外，请注意这只是一个配方计算器，而不是特定产品的确切配方。
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计算 重置

计算结果:

工作液浓度： mg/mL；

DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL)。如该浓度超过该批次药物DMSO溶解度，请首先与我们联系。

体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL ddH2O，混匀澄清。

(1) 请确保溶液澄清之后，再加入下一种溶剂 (助溶剂) 。可利用涡旋、超声或水浴加热等方法助溶；
            (2) 一定要按顺序加入溶剂 (助溶剂) 。

临床试验信息
Title:Confirmatory Study of MT-2412 in Japanese Patients With Type 2 Diabetes (Add-on Study of Canagliflozin)
Status:Completed
updateDate:2026-01-07
Ctid:NCT02354235

Link: https://clinicaltrials.gov/ct2/show/NCT02354235

Conditions:Type 2 Diabetes Mellitus
Interventions:Placebo
Phase:Phase 3
Title:Confirmatory Study of MT-2412 in Japanese Patients With Type 2 Diabetes (Add-on Study of Teneligliptin)
Status:Completed
updateDate:2026-01-07
Ctid:NCT02354222

Link: https://clinicaltrials.gov/ct2/show/NCT02354222

Conditions:Type 2 Diabetes Mellitus
Interventions:Placebo
Phase:Phase 3
Title:Efficacy and Safety of Teneligliptin in Combination With Metformin in Chinese Patients With Type 2 Diabetes Mellitus
Status:Completed
updateDate:2026-01-06
Ctid:NCT02924064

Link: https://clinicaltrials.gov/ct2/show/NCT02924064

Conditions:Type 2 Diabetes Mellitus
Interventions:Metformin ≥ 1000 mg
Phase:Phase 3
View More

Title:Efficacy and Safety of Teneligliptin in Chinese Patients With Type 2 Diabetes Mellitus
Status:Completed
updateDate:2026-01-06
Ctid:NCT02916706

Link: https://clinicaltrials.gov/ct2/show/NCT02916706

Conditions:Type 2 Diabetes Mellitus
Interventions:Placebo
Phase:Phase 3
Title:Long-term Safety Study of MP-513 as Monotherapy or in Combination With Sulfonylurea in Japanese Type 2 Diabetic Patients
Status:Completed
updateDate:2026-01-05
Ctid:NCT02314637

Link: https://clinicaltrials.gov/ct2/show/NCT02314637

Conditions:Type 2 Diabetes Mellitus
Interventions:Teneligliptin + Sulfonylurea
Phase:Phase 3
Title:Efficacy and Safety Study of MP-513 in Patients With Type 2 Diabetes
Status:Completed
updateDate:2026-01-02
Ctid:NCT00628212

Link: https://clinicaltrials.gov/ct2/show/NCT00628212

Conditions:Type 2 Diabetes
Interventions:Placebo
Phase:Phase 2
Title:Long-term Safety Study of MP-513 in Patients With Type 2 Diabetes
Status:Completed
updateDate:2026-01-02
Ctid:NCT01301833

Link: https://clinicaltrials.gov/ct2/show/NCT01301833

Conditions:Type 2 Diabetes Mellitus
Interventions:alpha-glucosidase inhibitor
Phase:Phase 3
Title:Pharmacokinetic/Pharmacodynamic Study of MP-513 With Type 2 Diabetes Mellitus
Status:Completed
updateDate:2026-01-02
Ctid:NCT01072331

Link: https://clinicaltrials.gov/ct2/show/NCT01072331

Conditions:Type 2 Diabetes Mellitus
Interventions:Placebo of MP-513
Phase:Phase 3
Title:Efficacy and Safety Study of Teneligliptin (MP-513) in Combination With Insulin in Patients With Type 2 Diabetes
Status:Completed
updateDate:2026-01-02
Ctid:NCT02081599

Link: https://clinicaltrials.gov/ct2/show/NCT02081599

Conditions:Type 2 Diabetes Mellitus
Interventions:Insulin
Phase:Phase 4
Title:Monotherapy Study of MP-513 in Patients With Type 2 Diabetes
Status:Completed
updateDate:2026-01-02
Ctid:NCT00998881

Link: https://clinicaltrials.gov/ct2/show/NCT00998881

Conditions:Type 2 Diabetes Mellitus
Interventions:Placebo
Phase:Phase 3
Title:Pharmacokinetics and Safety of HD-P023 and Co-administration of Teneligliptin and Empagliflozin High in Healthy Volunteers
Status:Completed
updateDate:2025-07-31
Ctid:NCT06889350

Link: https://clinicaltrials.gov/ct2/show/NCT06889350

Conditions:Healthy Volunteers
Interventions:Empagliflozin High
Phase:Phase 1
Title:Pharmacokinetics of HD-P023 and Co-administration of Teneligliptin and Empagliflozin High in Healthy Volunteers
Status:Completed
updateDate:2025-02-04
Ctid:NCT06339788

Link: https://clinicaltrials.gov/ct2/show/NCT06339788

Conditions:Healthy Volunteers
Interventions:Empagliflozin
Phase:Phase 1
Title:Clinical Efficacy and Safety Evaluation of Teneligliptin in Type 2 Diabetes Who Have Inadequate GlycemIc Control With Empaglyflozin 25 mg and Metformin
Status:Completed
updateDate:2025-01-27
Ctid:NCT05504226

Link: https://clinicaltrials.gov/ct2/show/NCT05504226

Conditions:Type 2 Diabetes
Interventions:Teneligliptin Placebo Oral Tablet
Phase:Phase 3
Title:Observational Study to Evaluate the Efficacy and Safety of Teneligliptin
Status:Completed
updateDate:2025-01-27
Ctid:NCT03793023

Link: https://clinicaltrials.gov/ct2/show/NCT03793023

Conditions:Type 2 Diabetes Mellitus
Interventions:Teneligliptin 20mg
Phase:
Title:Exploratory Study to Compare the Effects of Tenelia® or Januvia® on Glucose Variability in add-on to Metformin (CGMS Study)
Status:Completed
updateDate:2025-01-27
Ctid:NCT02512523

Link: https://clinicaltrials.gov/ct2/show/NCT02512523

Conditions:Type 2 Diabetes Mellitus
Interventions:Sitagliptin
Phase:Phase 4
Title:Clinical Efficacy and Safety Evaluation of Teneligliptin in Type 2 Diabetes Who Have Inadequate GlycemIc Control With Empaglyflozin and Metformin
Status:Completed
updateDate:2025-01-24
Ctid:NCT05504239

Link: https://clinicaltrials.gov/ct2/show/NCT05504239

Conditions:Type 2 Diabetes
Interventions:Teneligliptin Placebo Oral Tablet
Phase:Phase 3
Title:Tenelia Elderly CGMS Study(TEDDY)
Status:Completed
updateDate:2022-06-30
Ctid:NCT03508323

Link: https://clinicaltrials.gov/ct2/show/NCT03508323

Conditions:Type 2 Diabetes Mellitus
Interventions:Placebo
Phase:Phase 4
Title:Pharmacokinetic Drug Interaction Between Teneligliptin and Empagliflozin
Status:Completed
updateDate:2021-11-15
Ctid:NCT04431141

Link: https://clinicaltrials.gov/ct2/show/NCT04431141

Conditions:Type 2 Diabetes Mellitus
Interventions:Teneligliptin and Empagliflozin
Phase:Phase 1
Title:A Randomized, Placebo-controlled Clinical Trial of Teneligliptin as Quadruple Oral Combination Therapy for Type 2 DM After Failure of an Oral Triple Anti-diabetic Regimen
Status:Completed
updateDate:2021-06-09
Ctid:NCT04446026

Link: https://clinicaltrials.gov/ct2/show/NCT04446026

Conditions:Type 2 Diabetes Mellitus
Interventions:Placebo
Phase:Phase 4
Title:Teneligliptin and Atorvastatin DDI Study
Status:Completed
updateDate:2019-05-30
Ctid:NCT03769870

Link: https://clinicaltrials.gov/ct2/show/NCT03769870

Conditions:Diabete Mellitus
Interventions:Teneligliptin 20mg/day + Atorvastatin 40mg/day
Phase:Phase 1
Title:Teneligliptin Versus Linagliptin in Diabetes Mellitus Type Two Patients
Status:Completed
updateDate:2019-02-22
Ctid:NCT03011177

Link: https://clinicaltrials.gov/ct2/show/NCT03011177

Conditions:Type2 Diabetes Mellitus
Interventions:Linagliptin
Phase:Phase 4
Title:A Study to Compare MP-513 20mg & Metformin XR 1000mg FDC With Coadministration of the Two Separate Drugs
Status:Completed
updateDate:2018-12-27
Ctid:NCT03787017

Link: https://clinicaltrials.gov/ct2/show/NCT03787017

Conditions:Healthy Volunteers
Interventions:Metformin XR 1000mg
Phase:Phase 1
Title:Teneligliptin on the Progressive Left Ventricular Diastolic Dysfunction With Type 2 Diabetes Mellitus Study
Status:Unknown status
updateDate:2018-08-22
Ctid:NCT02449330

Link: https://clinicaltrials.gov/ct2/show/NCT02449330

Conditions:Diabetes Mellitus, Type 2
Interventions:Teneligliptin
Phase:Phase 4
Title:Teneligliptin-Glimepiride DDI Study
Status:Completed
updateDate:2018-05-02
Ctid:NCT03009513

Link: https://clinicaltrials.gov/ct2/show/NCT03009513

Conditions:Diabetes Mellitus
Interventions:Teneligliptin+Glimepiride
Phase:Phase 1
Title:Tenelia Triple Combination Study
Status:Completed
updateDate:2018-05-02
Ctid:NCT02567994

Link: https://clinicaltrials.gov/ct2/show/NCT02567994

Conditions:Type 2 Diabetes Mellitus
Interventions:Teneligliptin
Phase:Phase 3
Title:Teneligliptin(MP-513) vs. Placebo in Patient With Metformin Monotherapy
Status:Completed
updateDate:2015-10-06
Ctid:NCT01805830

Link: https://clinicaltrials.gov/ct2/show/NCT01805830

Conditions:Type 2 Diabetes
Interventions:Placebo
Phase:Phase 3
Title:Teneligliptin(MP-513) Versus Placebo in Type 2 Diabetes Mellitus
Status:Completed
updateDate:2014-08-05
Ctid:NCT01798238

Link: https://clinicaltrials.gov/ct2/show/NCT01798238

Conditions:Type 2 Diabetes Mellitus
Interventions:Placebo
Phase:Phase 3
Title:Comparison of the efficacy of sitagliptin 25mg and teneligliptin 20mg in patient with type2 diabetes and chronic kidney disease.
Status:Complete: follow-up complete
Date:2016-07-20
Ctid:UMIN000023243

Link: https://rctportal.mhlw.go.jp/en/detail?trial_id=UMIN000023243

Condition:type2 diabetes meliitus
Phase:
Title:Comparison of efficacy of Teneligliptin and Sitagliptin for glucose fluctuation in Type 2 diabetes
Status:Complete: follow-up complete
Date:2016-06-25
Ctid:UMIN000022885

Link: https://rctportal.mhlw.go.jp/en/detail?trial_id=UMIN000022885

Condition:Type 2 diabetes
Phase:
Title:RUBY
Status:completed
Date:2015-10-23
Ctid:jRCT1080222993

Link: https://rctportal.mhlw.go.jp/en/detail?trial_id=jRCT1080222993

Condition:Type 2 diabetes mellitus
Phase:
Title:Effects of one of antidiabetic agents, teneligliptin, on the vascular endothelium function of ACS patients with diabetes
Status:Complete: follow-up complete
Date:2015-09-08
Ctid:UMIN000018936

Link: https://rctportal.mhlw.go.jp/en/detail?trial_id=UMIN000018936

Condition:Acute Coronary Syndrome (ACS) and diabetes
Phase:
Title:THe effect of canagliflozin on active GLP-1 levels and betatrophin in patients with type 2 diabetes (CANARIA-STUDY)
Status:Complete: follow-up complete
Date:2015-02-15
Ctid:UMIN000016539

Link: https://rctportal.mhlw.go.jp/en/detail?trial_id=UMIN000016539

Condition:Type 2 diabetes
Phase:Not applicable
Title:Comparison of DPP-4 Inhibitors versus Dapagliflozin in combination with insulin using continuous glucose monitoring in patients with type 2 diabetes mellitus -prospective randomized controlled trial-
Status:Complete: follow-up complete
Date:2014-09-03
Ctid:UMIN000015033

Link: https://rctportal.mhlw.go.jp/en/detail?trial_id=UMIN000015033

Condition:type 2 diabetes mellitus
Phase:Phase IV
Title:Efficacy and safety of teneligliptin in patients with type 2 diabetes who responded insufficiently to dipeptidyl peptidase-4 (DPP-4) inhibitors
Status:Complete: follow-up complete
Date:2014-06-18
Ctid:UMIN000014298

Link: https://rctportal.mhlw.go.jp/en/detail?trial_id=UMIN000014298

Condition:Type 2 diabetes
Phase:Not applicable
Title:The study for efficacy of teneligliptin in non-alcoholic fatty liver disease (NAFLD) with type 2 diabetes mellitus
Status:Complete: follow-up complete
Date:2014-02-03
Ctid:UMIN000013048

Link: https://rctportal.mhlw.go.jp/en/detail?trial_id=UMIN000013048

Condition:non-alcoholic fatty liver disease/type 2 diabetes mellitus
Phase:Not applicable
Title:Teneligliptin effects on DPP-4 and glucagon concentrations in the serum during a meal test in patients with type 2 diabetes
Status:Recruiting
Date:2013-12-06
Ctid:UMIN000012508

Link: https://rctportal.mhlw.go.jp/en/detail?trial_id=UMIN000012508

Condition:Type 2 diabetes
Phase:
Title:Evaluation of blood glucose and serum lipids lowring effects of teneligliptin in patients with type 2 diabetes mellitus
Status:Complete: follow-up complete
Date:2013-11-05
Ctid:UMIN000012206

Link: https://rctportal.mhlw.go.jp/en/detail?trial_id=UMIN000012206

Condition:Patients with type 2 diabetes mellitus
Phase:
Title:The effect of regular exercise and regular exercise with teneligliptin on plasma GLP-1 concetration in the elderly patients with type 2 diabetes
Status:Complete: follow-up complete
Date:2013-11-05
Ctid:UMIN000012197

Link: https://rctportal.mhlw.go.jp/en/detail?trial_id=UMIN000012197

Condition:type 2 diabetes
Phase:
Title:The effects of teneligliptin on cardiac function and endothelial function in patients with type 2 diabetes
Status:Recruiting
Date:2013-10-28
Ctid:UMIN000012120

Link: https://rctportal.mhlw.go.jp/en/detail?trial_id=UMIN000012120

Condition:Type 2 diabetes
Phase:Not applicable
Title:DIrect Effect of DPP-4 inhibitor on HbA1c levels and Renal Dysfunction
Status:Complete: follow-up complete
Date:2013-10-18
Ctid:UMIN000012068

Link: https://rctportal.mhlw.go.jp/en/detail?trial_id=UMIN000012068

Condition:Type 2 diabetes
Phase:Not applicable
Title:Effects of Teneligliptin improvement endotherial dysfunction, inflammation, coagulation and oxidative stress in patients with coronary artery disease and diabetes, pilot study(Tiramisu study).
Status:Complete: follow-up complete
Date:2013-10-05
Ctid:UMIN000011960

Link: https://rctportal.mhlw.go.jp/en/detail?trial_id=UMIN000011960

Condition:Coronary artery disease
Phase:Not applicable
Title:Evaluation of the anticoagulant effect in Teneligliption in type 2 diabetic patients
Status:Complete: follow-up complete
Date:2013-10-01
Ctid:UMIN000011847

Link: https://rctportal.mhlw.go.jp/en/detail?trial_id=UMIN000011847

Condition:Type 2 Diabetes Mellitus
Phase:
Title:Effective and safe examination of teneligliptin for the type 2 diabetes with dialysis patient
Status:Complete: follow-up complete
Date:2013-09-30
Ctid:UMIN000011902

Link: https://rctportal.mhlw.go.jp/en/detail?trial_id=UMIN000011902

Condition:type 2 diabetes with dialysis patient
Phase:
Title:Effects of teneligliptin on glycemic control and bone metabolic markers in diabetic patients undergoing hemodialysis
Status:Complete: follow-up complete
Date:2013-05-22
Ctid:UMIN000010780

Link: https://rctportal.mhlw.go.jp/en/detail?trial_id=UMIN000010780

Condition:diabetic patients undergoing hemodialysis
Phase:

生物数据图片

  • Effects of teneligliptin on hepatic histopathology in experimental mice. (A) Hematoxylin and eosin (H&E) staining of liver sections from experimental mice. Representative photomicrographs of the liver sections of MSG/high-fat diet (HFD)-administered mice treated with or without teneligliptin. Bar, 100 μm; (B,C) The NAFLD activity score (NAS) was determined based on histopathological analysis (steatosis, inflammation and ballooning). Ctrl, control. TNL, teneligliptin. The values are expressed as the mean ± SD. * p < 0.05 versus the control group.[2]. Ideta T, et al. The Dipeptidyl Peptidase-4 Inhibitor Teneligliptin Attenuates Hepatic Lipogenesis via AMPK Activation in Non-Alcoholic Fatty Liver Disease Model Mice. Int J Mol Sci. 2015 Dec 8;16(12):29207-18

  • Effects of teneligliptin on hepatic steatosis and the levels of AMPK and p-AMPK in the livers of experimental mice. (A) Hepatic lipids were extracted from liver samples, and intrahepatic triglyceride (TG) levels were measured (n = 6); (B) steatosis in frozen liver sections from experimental mice treated with or without teneligliptin was analyzed with Oil Red O staining. Bar, 100 μm; (C) Total proteins were extracted from the livers of experimental mice, and the expression levels of AMPK and p-AMPK proteins were examined by Western blot analysis using the respective antibodies. GAPDH served as a loading control (left panel). Band intensities were quantified using densitometry. After the average of band intensity ratios of p-AMPK to GAPDH and AMPK to GAPDH were calculated in each sample, the ratios of these calculated values, which was expressed as p-AMPK/AMPK, were determined (right panel). Similar results were obtained in repeat experiments. The values are expressed as the mean ± SD. * p < 0.05 versus the control group.[2]. Ideta T, et al. The Dipeptidyl Peptidase-4 Inhibitor Teneligliptin Attenuates Hepatic Lipogenesis via AMPK Activation in Non-Alcoholic Fatty Liver Disease Model Mice. Int J Mol Sci. 2015 Dec 8;16(12):29207-18

  • Effects of teneligliptin on the expression levels of genes related to lipogenesis in the livers of experimental mice. Total RNA was isolated from the livers of the experimental mice (n = 6), and the expression levels of Acc, Fas, Srebp1c and Elovl6 mRNAs were examined using quantitative real-time RT-PCR with specific primers. The values are expressed as the mean ± SD. * p < 0.05 versus the control group.[2]. Ideta T, et al. The Dipeptidyl Peptidase-4 Inhibitor Teneligliptin Attenuates Hepatic Lipogenesis via AMPK Activation in Non-Alcoholic Fatty Liver Disease Model Mice. Int J Mol Sci. 2015 Dec 8;16(12):29207-18
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