Teneligliptin hydrobromide hydrate
(Synonyms: 氢溴酸替格列汀水合物,MP-513 hydrobromide hydrate) 目录号 : GC37757
A DPP-4 inhibitor
Cas No.:1572583-29-9
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Teneligliptin is a dipeptidyl peptidase 4 (DPP-4) inhibitor (IC50s = 0.37 and 0.29 nM for the human and rat enzymes, respectively).1 It is selective for DPP-4 over DPP-8 and DPP-9 (IC50s = 260 and 540 nM, respectively, for the human enzymes). Teneligliptin (0.03-1 mg/kg) inhibits increases in plasma glucose levels in an oral glucose tolerance test in Zucker fatty rats. It reduces body weight, inhibits hepatic steatosis, and decreases plasma insulin levels in a mouse model of high-fat diet-induced obesity when administered at doses of 30 and 60 mg/kg.2 Teneligliptin scavenges hydroxyl radicals in a cell-free assay (IC50 = 0.315 mM) and decreases urinary levels of 8-hydroxy-2′-deoxyguanosine , a marker of oxidative stress, in a DPP-4-deficient rat model of diabetes induced by streptozotocin when administered at a dose of 10 mg/kg per day.3
1.Yoshida, T., Akahoshi, F., Sakashita, H., 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 diabetesBioorg. Med. Chem.20(19)5705-5719(2012) 2.Fukuda-Tsuru, S., Kakimoto, T., Utsumi, H., et al.The novel dipeptidyl peptidase-4 inhibitor teneligliptin prevents high-fat diet-induced obesity accompanied with increased energy expenditure in miceEur. J. Pharmacol.723207-215(2014) 3.Kimura, S., Inoguchi, T., Yamasaki, T., et al.A novel DPP-4 inhibitor teneligliptin scavenges hydroxyl radicals: In vitro study evaluated by electron spin resonance spectroscopy and in vivo study using DPP-4 deficient ratsMetabolism65(3)138-145(2016)
| Cas No. | 1572583-29-9 | SDF | |
| 别名 | 氢溴酸替格列汀水合物,MP-513 hydrobromide hydrate | ||
| Canonical SMILES | O=C([C@H]1NC[C@@H](N2CCN(C3=CC(C)=NN3C4=CC=CC=C4)CC2)C1)N5CSCC5.[x H2O].[5/2 HBr] | ||
| 分子式 | C22H30N6OS | 分子量 | 426.58 |
| 溶解度 | DMF: 30 mg/ml,DMSO: 30 mg/ml,Ethanol: 2 mg/ml,PBS (pH 7.2): 10 mg/ml | 储存条件 | Store at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 |
| 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） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 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，
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 saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Analysis of patients with drug-induced pemphigoid using the Japanese Adverse Drug Event Report database
J Dermatol 2019 Mar;46(3):240-244.PMID:30575097DOI:10.1111/1346-8138.14741.
To clarify the incidence of drug-induced pemphigoid in Japan, we conducted a database search and analysis using the Japanese Adverse Drug Event Report database (JADER). Among the cases recorded in JADER between April 2004 and November 2017, we targeted "pemphigoid" and analyzed the patients' backgrounds, drug involvement, time of pemphigoid onset, outcomes and year reported. For cases where three or more drugs were reportedly involved, the signal index was calculated using the reporting odds ratio (ROR) method. The total number of reported pemphigoid cases was 769. Males accounted for 58% (446 cases) and patients over the age of 60 years accounted for 82% (630 cases). The most frequently reported causative drug was vildagliptin (288 cases), followed in order by sitagliptin phosphate hydrate (102 cases), Teneligliptin hydrobromide hydrate (86 cases), linagliptin (64 cases) and furosemide (46 cases). For the 27 causative drugs, the safety signal was detected by the ROR method. The median time to onset tended to be long for these drugs. For vildagliptin with the largest reported number, the value was 508 days (range, 2-1871). Analysis of outcomes demonstrated recovery or improvement in 66.3% of cases. Analysis of the years in which reports had been published revealed that the number of pemphigoid cases has increased rapidly in recent years. Our survey was able to reveal useful data on the incidence of drug-induced pemphigoid. We expect that these results will aid the early detection and treatment of this condition.