製品番号: HY-14806A

Teneligliptin hydrobromide

(別名: MP-513 hydrobromide)

6 Cited Publications

カスタマーレビュー

Based on 6 publication(s) in Google Scholar

Teneligliptin (MP-513) hydrobromide is an orally active and selective dipeptidyl peptidase 4 (DPP-4) inhibitor (IC₅₀s: 0.37 and 0.29 nM for the human and rat DPP-4, respectively). Teneligliptin hydrobromide improves blood glucose levels and can be used in researches related to type 2 diabetes mellitus.

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研究用途以外に使用した場合、当社は一切の責任を負いかねます。

純度: 99.99%
CAS 番号: 906093-29-6
分子式: C₂₂H₃₀N₆OS.5/2BrH
分子量:628.86

保管条件:

4°C, sealed storage, away from moisture

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

Teneligliptin hydrobromide 構造式

CAS 番号: 906093-29-6

容量

価格（税別）

在庫状況

数量

Amount: USD 0.00

* アイテムを追加する前、数量をご選択ください

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生物活性
- 製品説明
- IC₅₀ & Target
- 体外実験
- 体内実験
化学情報
Publications (6)
溶剤 & 溶解度
- 体外
- 体内
純度とドキュメンテーション
参考文献
Help & FAQs
関連分類
Bioz

生物活性

製品説明

IC₅₀ & Target^[1]^[2]^[3]^[4]^[5]^[6]^[7]^[8]

DPP-4

p38 MAPK

Dipeptidyl Peptidase アイソフォーム固有の製品をすべて表示 :

NOD-like Receptor (NLR) アイソフォーム固有の製品をすべて表示 :

Interleukin Related アイソフォーム固有の製品をすべて表示 :

AMPK アイソフォーム固有の製品をすべて表示 :

p38 MAPK アイソフォーム固有の製品をすべて表示 :

NF-κB アイソフォーム固有の製品をすべて表示 :

JNK アイソフォーム固有の製品をすべて表示 :

体外実験

Teneligliptin (2.5-5 μM, 24 h) hydrobromide prevents activation of the NLRP3 inflammasome and injury by increasing the phosphorylation of AMPK in primary mouse cardiomyocytes treated with high glucose^[3].
Teneligliptin (1-3 μM, 12 h) hydrobromide protects against hypoxia/reoxygenation-induced endothelial cell injury in rat cardiac microvascular endothelial cells, with suppressing reactive oxygen species (ROS) production^[5].
Teneligliptin (1.5-3 μM, 24 h) hydrobromide prevents Doxorubicin (HY-15142A)-induced inflammation (cytokines, including MCP-1 and IL-1β) and Apoptosis (improvement of the Bax/Bcl-2 ratio) in H9c2 cells^[6].
Teneligliptin (2.5-5 μM, 2-48 h) hydrobromide inhibits Lipopolysaccharide-induced cytotoxicity and inflammation through inhibiting TLR4 and JNK/AP1/NF-κB signaling in dental pulp cells, with reducing oxidative stress^[7].
Teneligliptin (3 μM, 3 h) hydrobromide prevents high glucose and H₂O₂ induced USP22-SIRT1 downregulation by p38MAPK inhibition and inhibits high glucose induced mitochondrial dysfunction, beta cell apoptosis as well as insulin secretion decreases in INS-1 cells^[8].
Teneligliptin (3 μM, 3 h) hydrobromide inhibits high glucose induced mitochondrial dysfunction by SIRT1 activation in human 1.1b4 beta cells^[8].

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

Western Blot Analysis^[3]

Cell Line:

Primary mouse cardiomyocytes treated with high glucose (30 mmol/L)
Concentration:

2.5, 5 μM
Incubation Time:

24 h
Result:

Inhibited NLRP3 and caspase-1 at 2.5 and 5 µM.
Increased the p-AMPK.

Western Blot Analysis^[5]

Cell Line:

Cardiac microvascular endothelial cells isolated from 1- to 4-day-old SD rats
Concentration:

1, 3 μM
Incubation Time:

12 h
Result:

Suppressed reactive oxygen species (ROS) and the vascular adhesion molecule ICAM-1.
Suppressed transcriptional factor Egr-1 expression.

Western Blot Analysis^[7]

Cell Line:

Human dental pulp cell
Concentration:

2.5, 5 μM
Incubation Time:

24 h
Result:

Suppressed c-Jun and c-Fos expression
Suppressed nuclear p65 protein accumulation

体内実験

Teneligliptin (0.1-1 mg/kg, p.o.) hydrobromide has excellent pharmacokinetic profile in rats and monkeys^[1].
Teneligliptin (10 mg/kg, p.o., 24 weeks) hydrobromide ameliorates diabetic polyneuropathy and inhibits glucose-stimulated blood glucose elevation by increasing pancreatic β-cell volume density (Vβ), insulin secretion in spontaneously type 2 diabetic rats^[2].
Teneligliptin (30 mg/kg, p.o., 4 weeks) hydrobromide attenuates myocardial hypertrophy, injury and associated inflammatory response in STZ (HY-13753)-induced diabetic cardiomyopathy mice by inhibiting NLRP3 inflammasome activation^[3].
Teneligliptin (30-60 mg/kg, drinking water, 10 weeks) hydrobromide prevents obesity and obesity-related manifestations with increased energy expenditure in a mouse model of high-fat diet-induced obesity (inhibition of adipocyte hypertrophy, hepatic steatosis)^[4].
Pharmacokinetics properties of teneligliptin hydrobromide by oral administration

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

Animal Model:

Diabetic cardiomyopathy (55 mg/kg STZ (HY-13753) was administered to C57BL/6 male mice by intraperitoneal injection for 5 consecutive days, fasting blood glucose level was higher than 16.7 mmol/L)^[3]
Dosage:

30 mg/kg
Administration:

Oral gavage (p.o.), 4 weeks
Result:

Ameliorated myocardial hypertrophy.
Improved heart function, with increasing the fractional shortening to 49.6%.
Reduced the expression of myocardial injury indicators (CK-MB, AST, LDH).
Reduced the critical pathological factor NOX4.
Reduced activation of the NLRP3 inflammasome and IL-1β in the heart.

化学情報

CAS 番号 906093-29-6
性状 Solid
分子量 628.86
分子式 C₂₂H₃₀N₆OS.5/2BrH
Color White to light brown
SMILES

O=C(N1CSCC1)[C@H]2NC[C@@H](N3CCN(C4=CC(C)=NN4C5=CC=CC=C5)CC3)C2.[2.5 HBr]
別名

MP-513 hydrobromide
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

4°C, sealed storage, away from moisture

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

Publications (6)

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Journal Impact Factor

Nephrol Dial Transplant

Dipeptidyl peptidase-4 inhibitor teneligliptin accelerates recovery from cisplatin-induced acute kidney injury by attenuating inflammation and promoting tubular regeneration. [Abstract]

2019 Oct 1;34(10):1669-1680. PMID: 30624740
Antioxidants (Basel)

Teneligliptin Co-Infusion Alleviates Morphine Tolerance by Inhibition of Spinal Microglial Cell Activation in Streptozotocin-Induced Diabetic Rats. [Abstract]

2023 Jul 24;12(7):1478. PMID: 37508016
Antioxidants (Basel)

Teneligliptin Exerts Antinociceptive Effects in Rat Model of Partial Sciatic Nerve Transection Induced Neuropathic Pain. [Abstract]

2021 Sep 9;10(9):1438. PMID: 34573072
Eur J Med Chem

Discovery of bardoxolone derivatives as novel orally active necroptosis inhibitors. [Abstract]

2021 Feb 15;212:113030. PMID: 33248849
Cosmetics

2024 Mar 1, 11(2), 35.
Chem Res Toxicol

Teneligliptin Promotes Bile Acid Synthesis and Attenuates Lipid Accumulation in Obese Mice by Targeting the KLF15-Fgf15 Pathway. [Abstract]

2020 Aug 17;33(8):2164-2171. PMID: 32639145

溶剤 & 溶解度

体外:

H₂O : ≥ 200 mg/mL (318.04 mM)

DMSO : ≥ 100 mg/mL (159.02 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.5902 mL

7.9509 mL

15.9018 mL

5 mM

0.3180 mL

1.5902 mL

3.1804 mL

10 mM

0.1590 mL

0.7951 mL

1.5902 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

モル濃度計算機

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

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

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体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (3.98 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (3.98 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (3.98 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: PBS

Solubility: 100 mg/mL (159.02 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Working solution concentration: 0.22 mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact

MedChemExpress (MCE) .

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

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COA (2659 KB)
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参考文献

[1]. Yoshida T, et al. Discovery and preclinical profile of teneligliptin (3-[(2S,4S)-4-[4-(3-methyl-1-phenyl-1H-pyrazol-5-yl)piperazin-1-yl]pyrrolidin-2-ylcarbonyl]thiazolidine): a highly potent, selective, long-lasting and orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes. Bioorg Med Chem. 2012 Oct 1;20(19):5705-19. [Content Brief]

[2]. Guo D, et al. Beneficial effects of combination therapy of canagliflozin and teneligliptin on diabetic polyneuropathy and β-cell volume density in spontaneously type 2 diabetic Goto-Kakizaki rats. Metabolism. 2020 Jun;107:154232. [Content Brief]

[3]. Zhang GL, et al. Teneligliptin mitigates diabetic cardiomyopathy by inhibiting activation of the NLRP3 inflammasome. World J Diabetes. 2024 Apr 15;15(4):724-734. [Content Brief]

[4]. Fukuda-Tsuru S, et al. The novel dipeptidyl peptidase-4 inhibitor teneligliptin prevents high-fat diet-induced obesity accompanied with increased energy expenditure in mice. Eur J Pharmacol. 2014 Jan 15;723:207-15. [Content Brief]

[5]. Zhang Z, et al. Teneligliptin protects against hypoxia/reoxygenation-induced endothelial cell injury. Biomed Pharmacother. 2019 Jan;109:468-474. [Content Brief]

[6]. Peng W, et al. Teneligliptin prevents doxorubicin-induced inflammation and apoptosis in H9c2 cells. Arch Biochem Biophys. 2020 Apr 15;683:108238. [Content Brief]

[7]. Liu X, et al. Teneligliptin inhibits lipopolysaccharide-induced cytotoxicity and inflammation in dental pulp cells. Int Immunopharmacol. 2019 Aug;73:57-63. [Content Brief]

[8]. Elumalai S, et al. High glucose-induced PRDX3 acetylation contributes to glucotoxicity in pancreatic β-cells: Prevention by Teneligliptin. Free Radic Biol Med. 2020 Nov 20;160:618-629. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Animal	Dose (mg/kg)	t_max (h)	C_max (ng/mL)	t_1/2 (h)	AUC_0-last (h × ng/mL)	BA (%)
Rat	0.1	0.88	5.48	15.84	91.81	85.9
Rat	0.3	0.75	20.65	8.97	202.12	63
Rat	1	0.75	152.41	8.43	672.94	62.9
Monkey	0.1	0.5	28.27	18.86	295.44	83.2
Monkey	0.3	1.38	85.13	15.24	613.16	57.6
Monkey	1	0.88	273.54	16.11	1571.64	44.1

Optional Solvent	Concentration Solvent Mass	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

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Teneligliptin hydrobromide

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MedChemExpress（MCE）の使用を引用している文献 Teneligliptin hydrobromide

Dipeptidyl Peptidase アイソフォーム固有の製品をすべて表示

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Interleukin Related アイソフォーム固有の製品をすべて表示