DPP-4 inhibitor 1
目录号 : GC31512
DPP-4inhibitor1(compound5)是有效的、长效的二肽基肽酶-4(DPP-4)的抑制剂，有治疗2型糖尿病的潜力，其KD值为0.177nM。
Cas No.:1915007-89-4
Sample solution is provided at 25 µL, 10mM.
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DPP-4 inhibitor 1 (compound 5) is a potent and long acting Dipeptidyl peptidase-4 (DPP-4) inhibitor for t treatment of T2DM, with a KD of 0.177 nM[1].
A single-dose oral administration of DPP-4 inhibitor 1 (compound 5) (3 mg/kg) inhibits >80% of DPP-4 activity for more than 7 days in diabetic mice[1].Administration of DPP-4 inhibitor 1 (compound 5) (3 and 10 mg/kg, p.o., qw for 8 weeks) causes significant reductions in fasting blood glucose (FBG) levels, and the average reduction during the entire treatment period is 24.7 and 33.1%, respectively. Chronic administration of DPP-4 inhibitor 1 (compound 5) (10 mg/kg/week) also significantly improves the glucose tolerance of the diabetic mice[1].|| Animal Model:|ICR mice[1].|Dosage:|0.3, 3, 10 mg/kg.|Administration:|Oral, once.|Result:|Resulted in a time- and dose-dependent inhibition of plasma DPP-4 activity.The active GLP-1 and insulin level were significantly increased compared with the vehicle control.|| Animal Model:|Genetic-type 2 diabetes animal models in db/db Mice[1].|Dosage:|3 and 10 mg/kg.|Administration:|Oral administration once a week, for 8 weeks.|Result:|Caused significant reductions in fasting blood glucose (FBG) levels.Improved the glucose tolerance of the diabetic mice significantly.
[1]. Li S, et al. Discovery of a Natural-Product-Derived Preclinical Candidate for Once-Weekly Treatment of Type 2 Diabetes. J Med Chem. 2019 Feb 1.
| Cas No. | 1915007-89-4 | SDF | |
| Canonical SMILES | FC1=CC(F)=C([C@H]2OC3=CC=C(C=C(C#N)C(OC)=C4)C4=C3C[C@@H]2N)C=C1F | ||
| 分子式 | C21H15F3N2O2 | 分子量 | 384.35 |
| 溶解度 | Soluble in DMSO | 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 | 2.6018 mL | 13.009 mL | 26.018 mL |
| 5 mM | 0.5204 mL | 2.6018 mL | 5.2036 mL |
| 10 mM | 0.2602 mL | 1.3009 mL | 2.6018 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。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet