Tadalafil-d3
(Synonyms: 他达拉非-D3,IC-351-d3) 目录号 : GC48121
An internal standard for the quantification of tadalafil
Cas No.:960226-55-5
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
Tadalafil-d3 is intended for use as an internal standard for the quantification of tadalafil by GC- or LC-MS. Tadalafil is a potent inhibitor of phosphodiesterase 5 (PDE5; IC50 = 1.2 nM).1 It is selective for PDE5 over PDE1-4 and 7-10 (IC50s = 9.2-280 μM), however, it does also inhibit PDE11 (IC50 = 11 nM). In vivo, tadalafil (10 mg/kg) decreases production of the proinflammatory cytokines TNF-α, IL-1β, and IL-6 and improves renal function in a rat model of ischemia/reperfusion injury.2 It also reduces development of tobacco smoke-induced emphysema and pulmonary hypertension in mice.3 Formulations containing tadalafil have been used to treat erectile dysfunction, pulmonary arterial hypertension, and lower urinary tract dysfunction.
1.Card, G.L., England, B.P., Suzuki, Y., et al.Structural basis for the activity of drugs that inhibit phosphodiesterasesStructure12(12)2233-2247(2004) 2.Medeiros, V.F., Azevedo, Í.M., Carvalho, M.D., et al.The renoprotective effect of oral tadalafil pretreatment on ischemia/reperfusion injury in ratsActa. Cir. Bras.32(2)90-97(2017) 3.Seimetz, M., Parajuli, N., Pichl, A., et al.Cigarette smoke-induced emphysema and pulmonary hypertension can be prevented by phosphodiesterase 4 and 5 inhibition in micePLoS One10(6)e0129327(2015)
| Cas No. | 960226-55-5 | SDF | |
| 别名 | 他达拉非-D3,IC-351-d3 | ||
| Canonical SMILES | O=C1N(C([2H])([2H])[2H])CC(N2[C@H](C3=CC=C(OCO4)C4=C3)C5=C(C6=CC=CC=C6N5)C[C@@]21[H])=O | ||
| 分子式 | C22H16D3N3O4 | 分子量 | 392.4 |
| 溶解度 | DMSO: Soluble,Methanol: Soluble | 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 | 2.5484 mL | 12.7421 mL | 25.4842 mL |
| 5 mM | 0.5097 mL | 2.5484 mL | 5.0968 mL |
| 10 mM | 0.2548 mL | 1.2742 mL | 2.5484 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。
Quantitation of tadalafil in human plasma using a sensitive and rapid LC-MS/MS method for a bioequivalence study
J Pharm Anal 2018 Aug;8(4):271-276.PMID:30140492DOI:PMC6104147
A highly sensitive liquid chromatography-tandem mass spectrometry (LC-MS/MS) method was developed for the determination of tadalafil (TAD) in human plasma. TAD and its deuterated internal standard (IS), Tadalafil-d3, were extracted from 200 µL plasma using Phenomenex Strata-X-C 33 µ extraction cartridges. Chromatographic analysis was carried out on Synergi™ Hydro-RP C18 (100 mm × 4.6 mm, 4 µm) column with a mobile phase consisting of methanol and 10 mM ammonium formate, pH 4.0 (90:10, v/v), delivered at a flow rate of 0.9 mL/min. Quantitation of the protonated analyte was done on a triple quadrupole mass spectrometer using multiple reaction monitoring via electrospray ionization. The precursor to product ions transitions monitored for TAD and TAD-d3 were m/z 390.3 → 268.2 and m/z 393.1 → 271.2, respectively. The calibration curve was linear over the concentration range of 0.50-500 ng/mL with correlation coefficient, r2 ≥ 0.9994. Acceptable intra-batch and inter-batch precision (≤ 3.7%) and accuracy (97.8% to 104.1%) were obtained at five concentration levels. The recovery of TAD from spiked plasma was highly precise and quantitative (98.95% to 100.61%). Further, the effect of endogenous matrix components was minimal. TAD was found to be stable under different storage conditions in human plasma and also in whole blood samples. The validated method was successfully used to determine TAD plasma concentration in a bioequivalence study with 20 mg TAD tablets in 24 healthy volunteers. Method performance was evaluated by reanalyzing 115 study samples.