Vildagliptin-d7
(Synonyms: 维格列汀D7,LAF237-d7; NVP-LAF 237-d7) 目录号 : GC48250
An internal standard for the quantification of vildagliptin
Cas No.:1133208-42-0
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Vildagliptin-d7 has 7 deuteriums. Vildagliptin-d7 is intended for use as an internal standard for the quantification of vildagliptin by GC- or LC-MS. Vildagliptin is an inhibitor of DPP-4 (IC50 = 3.5-34 nM).1,2 It also inhibits DPP-8 and DPP-9 (Ki = 810 and 95 nM, respectively) but not DPP-2 or the related fibroblast activation protein α.3 Through its effects on DPP-4, it blocks the degradation of several circulating peptides, including incretins (stimulators of insulin secretion) like glucose-dependent insulinotropic polypeptide and glucagon-like peptide-1.4,5 Vildagliptin reduces fasting and postprandial glucose levels and decreases inflammatory and oxidative stress in diverse animal models of disease.6,7
1.Weber, A.E.Dipeptidyl peptidase IV inhibitors for the treatment of diabetesJournal of Medicinal Chemistry47(17)4135-4141(2004) 2.Parmee, E.R., He, J., Mastracchio, A., et al.4-amino cyclohexylglycine analogues as potent dipeptidyl peptidase IV inhibitorsBioorganic & Medicinal Chemistry Letters14(1)43-46(2004) 3.Ikuma, Y., Hochigai, H., Kimura, H., et al.Discovery of 3H-imidazol[4,5-c]quinolin-4(5H)-ones as potent and selective dipeptidyl peptidase IV (DPP-4) inhibitorsBioorganic & Medicinal Chemistry20(19)5864-5883(2012) 4.Mari, A., Sallas, W.M., He, Y.L., et al.Vildagliptin, a dipeptidyl peptidase-IV inhibitor, improves model-assessed β-cell function in patients with type 2 diabetesJournal of Clinical Endocrinology and Metabolism90(8)4888-4894(2005) 5.Burkey, B.F., Li, X., Bolognese, L., et al.Acute and chronic effects of the incretin enhancer vildagliptin in insulin-resistant ratsJournal of Pharmacology and Experimental Therapeutics315(2)688-695(2005) 6.Scheen, A.J.Cardiovascular effects of gliptinsNat.Rev.Cardiol.10(2)73-84(2013) 7.Strain, W.D., Lukashevich, V., Kothny, W., et al.Individualised treatment targets for elderly patients with type 2 diabetes using vildagliptin add-on or lone therapy (INTERVAL): A 24 week, randomised, double-blind, placebo-controlled studyLangmuir382(9890)409-416(2013)
| Cas No. | 1133208-42-0 | SDF | |
| 别名 | 维格列汀D7,LAF237-d7; NVP-LAF 237-d7 | ||
| Canonical SMILES | O=C(CN[C@@]1(CC(C2)C3)CC3C[C@]2(O)C1)N4[C@]([2H])(C#N)C([2H])([2H])C([2H])([2H])C4([2H])[2H] | ||
| 分子式 | C17H18D7N3O2 | 分子量 | 310.4 |
| 溶解度 | DMF: 20 mg/ml,DMSO: 15 mg/ml,Ethanol: 15 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 | 3.2216 mL | 16.1082 mL | 32.2165 mL |
| 5 mM | 0.6443 mL | 3.2216 mL | 6.4433 mL |
| 10 mM | 0.3222 mL | 1.6108 mL | 3.2216 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。