Canagliflozin D4
(Synonyms: 卡格列净D4,JNJ 28431754-d4) 目录号 : GC39178
An internal standard for the quantification of canagliflozin
Cas No.:1997338-61-0
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
Canagliflozin-d4 is intended for use as an internal standard for the quantification of canagliflozin by GC- or LC-MS. Canagliflozin is an inhibitor of sodium-glucose cotransporter 2 (SGLT2; IC50 = 2.2 nM) that less potently blocks SGLT1 (IC50 = 910 nM).1 Canagliflozin is orally bioavailable and lowers plasma glucose by lowering the renal threshold for glucose and increasing urinary glucose excretion in animals.1,2 Formulations containing SGLT2 inhibitors, including canagliflozin, have been used to treat type 2 diabetes mellitus.3
1.Nomura, S., Sakamaki, S., Hongu, M., et al.Discovery of canagliflozin, a novel C-glucoside with thiophene ring, as sodium-dependent glucose cotransporter 2 inhibitor for the treatment of type 2 diabetes mellitusJ. Med. Chem.53(17)6355-6360(2010) 2.Sha, S., Devineni, D., Ghosh, A., et al.Canagliflozin, a novel inhibitor of sodium glucose co-transporter 2, dose dependently reduces calculated renal threshold for glucose excretion and increases urinary glucose excretion in healthy subjectsDiabetes Obes. Metab.13(7)669-672(2011) 3.Reed, J.W.Impact of sodium-glucose cotransporter 2 inhibitors on blood pressureVasc. Health Risk Manag.12393-405(2016)
| Cas No. | 1997338-61-0 | SDF | |
| 别名 | 卡格列净D4,JNJ 28431754-d4 | ||
| Canonical SMILES | FC1=C([2H])C([2H])=C(C2=CC=C(CC3=C(C=CC([C@@H]4O[C@@H]([C@H]([C@@H]([C@H]4O)O)O)CO)=C3)C)S2)C([2H])=C1[2H] | ||
| 分子式 | C24H21D4FO5S | 分子量 | 448.54 |
| 溶解度 | DMF: 30 mg/ml,DMSO: 30 mg/ml,Ethanol: 30 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.2295 mL | 11.1473 mL | 22.2946 mL |
| 5 mM | 0.4459 mL | 2.2295 mL | 4.4589 mL |
| 10 mM | 0.2229 mL | 1.1147 mL | 2.2295 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。
Development of LC-MS/MS method for simultaneous determination of Canagliflozin and Metformin in human plasma and its pharmacokinetic application in Indian population under fast and fed conditions
J Chromatogr B Analyt Technol Biomed Life Sci 2020 Oct 1;1154:122281.PMID:32763846DOI:10.1016/j.jchromb.2020.122281
A novel, selective and sensitive method is developed for simultaneous estimation of canagliflozin and metformin and successfully applied to fast and fed pharmacokinetic studies in healthy Indian volunteers. The current study reports the development, optimization, and validation of liquid chromatography-mass spectrometry (LC-MS/MS) method for simultaneous quantification of canagliflozin and metformin in human plasma using deuterated Canagliflozin D4 and metformin D6 as an internal standard (IS). The solid-phase extraction technique was employed where strata X polymeric reverse phase (30 mg-1 cc) SPE cartridges were used for the extraction of analytes and IS from plasma. The ACE 5 C18 column (50 × 4.6 mm, 5µ) was used to chromatograph the prepared samples. The mobile phase consisted of methanol and 5 mM ammonium trifluoroacetate in water, pH 5 (50:50, v/v) at a flow rate of 0.8 mL/min. Detection was performed by positive ion Turbo ion spray in Multiple reaction monitoring (MRM) mode, monitoring the transitions m/z 461.9 → m/z 191.1 and m/z 461.9 → m/z 267.2, for quantification of canagliflozin. The response of canagliflozin fragments m/z 461.9 → m/z 191.1 and m/z 461.9 → m/z 267.2 was combined. Also, for metformin transitions were monitored at m/z 130.0 → m/z 71.1. Full validation of the method was performed according to the United States Food and Drugs Administration (USFDA) guidelines. Linearity was in the range of 24.95-2806.55 ng/mL for canagliflozin and 24.99-3400.72 ng/mL for metformin. The mean extraction recovery of canagliflozin, Canagliflozin D4, metformin, and metformin D6 was 77.240, 84.663, 66.747, and 67.449, respectively across four QC levels. This rapid method with the run time of 2.80 min allows the analysis of more than 400 plasma samples per day.