Zastaprazan
(Synonyms: JP-1366) 目录号 : GC63472
Zastaprazan 是一种 proton pump 抑制剂 (WO2018008929)。Zastaprazan 可用于胃肠道炎症或胃酸相关疾病的研究。
Cas No.:2133852-18-1
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Zastaprazan is a proton pump inhibitor (WO2018008929). Zastaprazan can be used for the research of gastrointestinal inflammatory diseases or gastric acid-related diseases[1].
Zastaprazan is a proton pump inhibitor[1]
[1]. WO2018008929
| Cas No. | 2133852-18-1 | SDF | |
| 别名 | JP-1366 | ||
| 分子式 | C22H26N4O | 分子量 | 362.47 |
| 溶解度 | DMSO : 33.33 mg/mL (91.95 mM; Need ultrasonic) | 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 | 2.7588 mL | 13.7942 mL | 27.5885 mL |
| 5 mM | 0.5518 mL | 2.7588 mL | 5.5177 mL |
| 10 mM | 0.2759 mL | 1.3794 mL | 2.7588 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。
Randomised clinical trial: Safety, tolerability, pharmacodynamics and pharmacokinetics of Zastaprazan (JP-1366), a novel potassium-competitive acid blocker, in healthy subjects
Aliment Pharmacol Ther 2023 Apr;57(7):763-772.PMID:36732884DOI:10.1111/apt.17406
Background: Zastaprazan (JP-1366) is a novel potassium-competitive acid blocker with favourable preclinical safety and efficacy profile being developed for the treatment of acid-related diseases. Aims: To investigate the safety, tolerability, pharmacodynamics and pharmacokinetics of Zastaprazan. Methods: A randomised, open-label, placebo- and active-controlled, single and multiple ascending dose clinical trial was conducted in healthy Korean male subjects. Intragatric pH and serum gastrin were measured to assess the pharmacodynamics, while serial blood and urine samples were collected to assess the pharmacokinetics. Pharmacogenomic evaluation was conducted to explore genetic variants, which can affect the pharmacodynamics and pharmacokinetics. Safety and tolerability including hepatotoxicity were evaluated. Results: Suppression of gastric acid secretion increased as the dose of Zastaprazan increased. The percentage of time that gastric pH was over 4 (%Time pH >4) with Zastaprazan 20 mg (85.19%) and 40 mg (91.84%) were similar to or greater than that with esomeprazole 40 mg (72.06%). Zastaprazan was rapidly absorbed within 2 h and eliminated with a half-life of 6-10 h. Pharmacogenomic analysis found no genetic variant of drug metabolising enzymes including CYP2C19 or drug transporters associated with the exposure of Zastaprazan. Zastaprazan was well tolerated with no clinically significant changes in safety and tolerability assessments. Conclusions: Zastaprazan was safe and well tolerated after a single oral dose up to 60 mg and multiple oral doses up to 40 mg. It also showed rapid, potent suppression of gastric acid secretion. Pharmacodynamic and pharmacokinetic profile of Zastaprazan was suitable for treatment of patients with acid-related diseases.