體外研究In Vitro )
Teneligliptin (2.5-5 μM, 24 h) hydrobromide hydrate 通過(guò)增加 AMPK NLRP3 炎癥小體激活和損傷[3] [5] Doxorubicin (HY-15142A ) 誘導(dǎo)的 H9c2 細(xì)胞炎癥 (細(xì)胞因子，包括 MCP-1 和 IL-1β) 和凋亡 (Apoptosis ) (Bax/Bcl-2 比率的改善)[6] TLR4 和 JNK/AP1/NF-κB 信號(hào)傳導(dǎo)，抑制 Lipopolysaccharide 誘導(dǎo)的細(xì)胞毒性和炎癥反應(yīng)，同時(shí)降低氧化應(yīng)激反應(yīng)[7] 2 O2 誘導(dǎo)的 USP22-SIRT1 下調(diào)，并抑制高糖誘導(dǎo)的 INS-1 細(xì)胞線粒體功能障礙、β 細(xì)胞凋亡以及胰島素分泌減少[8] SIRT1 抑制人 1.1b4 β 細(xì)胞中高血糖誘導(dǎo)的線粒體功能障礙[8]
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Teneligliptin hydrobromide hydrate 相關(guān)抗體:
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.
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.
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
體內(nèi)研究In Vivo )
Teneligliptin (10 mg/kg，口服，24 周) hydrobromide hydrate 改善自發(fā)性 2 型糖尿病大鼠糖尿病性多發(fā)性神經(jīng)病變，增加胰腺 β 細(xì)胞體積密度 (Vβ)、胰島素分泌, 從而抑制葡萄糖刺激后的血糖升高[2] NLRP3 炎性小體激活減輕 STZ (HY-13753 ) 誘導(dǎo)的糖尿病心肌病小鼠心肌肥大、損傷和相關(guān)的炎癥反應(yīng)[3] [4] [1] 口服 Teneligliptin hydrobromide hydrate 的藥代動(dòng)力學(xué)特性
Animal
Dose (mg/kg)
t max (h)C max (ng/mL)t 1/2 (h) AUC0-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
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.
Clinical Trial
分子量
Formula
CAS 號(hào)
性狀
顏色
中文名稱
運(yùn)輸條件
Room temperature in continental US; may vary elsewhere.
儲(chǔ)存方式
4°C, sealed storage, away from moisture
溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn)：
H2 O 中的溶解度 : ≥ 100 mg/mL (234.42 mM )
* "≥" means soluble, but saturation unknown.
配制儲(chǔ)備液
濃度
溶劑體積
質(zhì)量
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
查看完整儲(chǔ)備液配制表
*
請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效 。 儲(chǔ)備液的保存方式和期限： -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用。
*
備注：如您選擇水作為儲(chǔ)備液，請(qǐng)稀釋至工作液后，再用 0.22 μm 的濾膜過(guò)濾除菌后使用。
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1 V1 = C2 V2
動(dòng)物溶解方案計(jì)算器
請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息：
純度 & 產(chǎn)品資料
純度: 99.87%
選擇批次：
HY-14806B-15****
HY-14806B-28****
參考文獻(xiàn)
[1]. Fukuda-Tsuru S, et al. 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.
[Content Brief]
[2]. 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]
[3]. 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]
[4]. 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]
[5]. 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]
[6]. Zhang Z, et al. Teneligliptin protects against hypoxia/reoxygenation-induced endothelial cell injury. Biomed Pharmacother. 2019 Jan;109:468-474.
[Content Brief]
[7]. Peng W, et al. Teneligliptin prevents doxorubicin-induced inflammation and apoptosis in H9c2 cells. Arch Biochem Biophys. 2020 Apr 15;683:108238.
[Content Brief]
[8]. Liu X, et al. Teneligliptin inhibits lipopolysaccharide-induced cytotoxicity and inflammation in dental pulp cells. Int Immunopharmacol. 2019 Aug;73:57-63.
[Content Brief]
[9]. 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]
[1]. Fukuda-Tsuru S, et al. 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]. 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.
[3]. 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.
[4]. 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.
[5]. 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.
[6]. Zhang Z, et al. Teneligliptin protects against hypoxia/reoxygenation-induced endothelial cell injury. Biomed Pharmacother. 2019 Jan;109:468-474.
[7]. Peng W, et al. Teneligliptin prevents doxorubicin-induced inflammation and apoptosis in H9c2 cells. Arch Biochem Biophys. 2020 Apr 15;683:108238.
[8]. Liu X, et al. Teneligliptin inhibits lipopolysaccharide-induced cytotoxicity and inflammation in dental pulp cells. Int Immunopharmacol. 2019 Aug;73:57-63.
[9]. 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.
Teneligliptin hydrobromide hydrate 相關(guān)分類
完整儲(chǔ)備液配制表
*
請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效 。 儲(chǔ)備液的保存方式和期限： -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用。
可選溶劑
濃度
溶劑體積
質(zhì)量
1 mg 5 mg 10 mg 25 mg
H2 O
1 mM
2.3442 mL
11.7211 mL
23.4423 mL
58.6057 mL
5 mM
0.4688 mL
2.3442 mL
4.6885 mL
11.7211 mL
10 mM
0.2344 mL
1.1721 mL
2.3442 mL
5.8606 mL
15 mM
0.1563 mL
0.7814 mL
1.5628 mL
3.9070 mL
20 mM
0.1172 mL
0.5861 mL
1.1721 mL
2.9303 mL
25 mM
0.0938 mL
0.4688 mL
0.9377 mL
2.3442 mL
30 mM
0.0781 mL
0.3907 mL
0.7814 mL
1.9535 mL
40 mM
0.0586 mL
0.2930 mL
0.5861 mL
1.4651 mL
50 mM
0.0469 mL
0.2344 mL
0.4688 mL
1.1721 mL
60 mM
0.0391 mL
0.1954 mL
0.3907 mL
0.9768 mL
80 mM
0.0293 mL
0.1465 mL
0.2930 mL
0.7326 mL
100 mM
0.0234 mL
0.1172 mL
0.2344 mL
0.5861 mL
*
備注：如您選擇水作為儲(chǔ)備液，請(qǐng)稀釋至工作液后，再用 0.22 μm 的濾膜過(guò)濾除菌后使用。
Your information is safe with us. * Required Fields.
Inquiry Information
產(chǎn)品名稱：
Teneligliptin hydrobromide hydrate
目錄號(hào)：
HY-14806B
需求量：
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