Nocloprost
(Synonyms: 诺氯前列素) 目录号 : GC44433
A gastoprotective PGE2 analog
Cas No.:79360-43-3
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
Nocloprost is a stable prostaglandin E2 analog with gastroprotective and ulcer-healing properties. As a weak acid (pKa = 5), it accumulates in the gastric mucosa at low pH and can prevent the formation of gastric lesions in rats when administered intragastrically 30 minutes before 100% ethanol, acidified aspirin, acidified taurocholate, water immersion, or restraint stress (ID50s = 0.25, 0.58, 0.06 and 0.12 μg/kg, respectively). Additionally, nocloprost has been used to inhibit evoked acetylcholine release from isolated human bronchi (IC50 = 4 nM) to study factors that regulate human airway smooth muscle tone and secretion.
| Cas No. | 79360-43-3 | SDF | |
| 别名 | 诺氯前列素 | ||
| Canonical SMILES | Cl[C@H]1[C@H](C/C=C\CCCC(O)=O)[C@@H](/C=C/[C@@H](O)C(C)(C)CCCC)[C@H](O)C1 | ||
| 分子式 | C22H37ClO4 | 分子量 | 401 |
| 溶解度 | DMF: 11 mg/ml,DMSO: 10 mg/ml,Ethanol: 16 mg/ml,Ethanol:PBS (pH 7.2)(1:2): 0.3 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 | 2.4938 mL | 12.4688 mL | 24.9377 mL |
| 5 mM | 0.4988 mL | 2.4938 mL | 4.9875 mL |
| 10 mM | 0.2494 mL | 1.2469 mL | 2.4938 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。
Nocloprost, a unique prostaglandin E2 analog with local gastroprotective and ulcer-healing activity
Eur J Pharmacol 1991 Apr 3;195(3):347-57.PMID:1868881DOI:10.1016/0014-2999(91)90475-6.
Nocloprost (9 beta-chloro-16,16-dimethyl prostaglandin E2 (PGE2)) was examined for gastroprotective and ulcer-healing activity and compared to 16,16-dimethyl PGE2 (dmPGE) in rats. Nocloprost given intragastrically (i.g.) at various doses (0.01-10 micrograms/kg) 30 min before 100% ethanol, acidified aspirin (ASA), acidified taurocholate, water immersion, or restraint stress dose dependently prevented the formation of gastric lesions, the ID50 values being 0.25, 0.58, 0.06 and 0.12 micrograms/kg, respectively. The gastroprotection provided by Nocloprost given i.g. was somewhat enhanced by the presence of acid in the stomach and was reduced by inhibition of gastric acid secretion. Nocloprost given s.c. also showed protective activity against ethanol damage but was ineffective when applied intraduodenally. The protective effect of Nocloprost lasted about 8 h whereas that induced by dmPGE lasted 6 h. Nocloprost (0.01-100 micrograms/kg) given i.g. failed to affect gastric acid secretion or intestinal secretion (enteropooling) but prevented the increased gastroduodenal alkaline secretion. Nocloprost alone caused only a transient increase in the mucosal blood flow but prevented the fall in blood flow caused by 100% ethanol. [3H]Nocloprost was absorbed from the small intestine but was then taken up and metabolized by the liver and excreted into the bile so that very little reached the systemic circulation in an unchanged form. Nocloprost, unlike dmPGE, accelerated the healing of chronic gastric ulcerations and enhanced mucosal growth. We conclude that Nocloprost is a locally active PGE2 analog with high cytoprotective and ulcer-healing efficacy.
Gastric protection by Nocloprost against aspirin damage in humans. Possible role of epidermal growth factor
Scand J Gastroenterol 1991 Mar;26(3):231-6.PMID:1853145DOI:10.3109/00365529109025036.
Ten healthy young male subjects took part in a double-blind, placebo-controlled crossover study to assess the effects of Nocloprost on gastric microbleeding and endoscopic mucosal injury induced by the administration of aspirin (2.5 g). In addition, basal and pentagastrin-induced gastric acid and pepsin secretion and salivary and plasma contents of epidermal growth factor (EGF) were measured after placebo plus aspirin or Nocloprost plus aspirin treatment in these subjects. Nocloprost (100 micrograms/dose) significantly reduced spontaneous gastric microbleeding and almost completely prevented gastric mucosal injury induced by aspirin. Nocloprost failed to affect basal and pentagastrin-stimulated gastric acid and pepsin secretion but increased significantly the salivary outputs and plasma concentrations of EGF. In conclusion, Nocloprost is effective in preventing gastric injury by aspirin even at a non-antisecretory dose, and this protection may involve an excessive release of EGF.
Synthesis of a deuterated analogue and development of antibody/GC/MS for the determination of Nocloprost in plasma
Prostaglandins 1990 Sep;40(3):283-96.PMID:2247618DOI:10.1016/0090-6980(90)90016-o.
An analytical method for the determination of the PGE derivative Nocloprost in plasma was developed combining the features of both radioimmunoassay and GC/MS. The antibody usually employed in Nocloprost radioimmunoassay was coupled to Sepharose 4B and used as a stationary phase for the extraction of the drug. After appropriate derivatisation, Nocloprost was determined by GC/MS in the negative ion-chemical ionisation mode. As an internal standard deuterated Nocloprost was synthesized and added to the plasma samples before extraction. The extraction recovery was 94% and the limit of detection was 5 pg/ml. Intra- and interassay precision at 100 pg/ml was calculated as 3.3 and 4.0%, respectively.
Pharmacokinetics of Nocloprost in human volunteers and its relation to dose
Eur J Clin Pharmacol 1993;44(5):497-500.PMID:8359191DOI:10.1007/BF00315552.
The pharmacokinetics and absolute bioavailability of Nocloprost, a synthetic PGE2-analogue with cytoprotective properties, was investigated in human volunteers as a function of the dose. Ten young male volunteers received Nocloprost 5 micrograms i.v. and 100, 200 and 400 micrograms p.o. in random order at weekly intervals. Serum Nocloprost levels were monitored for up to 12 h after each dose, using a specific, validated assay. After Nocloprost 5 micrograms i.v. the highest serum level of 373 pg.ml-1 was found in the first sample 5 min after injection, and the subsequent decline showed one or two phases, with half-lives of 4 and 49 min. The AUC was 89 pg.h.ml-1, the total plasma clearance was 13.2 ml.min-1.kg-1, and the volume of distribution at steady state was 0.16 l.kg-1. After oral administration the maximum serum level and AUC increased in proportion to the dose. tmax showed a wide scatter, with an average value of about 30 min independent of the dose. Although not detectable in every subject, post maximum serum levels declined biphasically, with half-lives of ca 10 and 35-40 min. The absolute bioavailability after oral administration averaged about 2% and was independent of the dose.
Effects of ranitidine or Nocloprost on the selected gastric juice components in the patients with the gastric ulcer
Rocz Akad Med Bialymst 1997;42(1):257-66.PMID:9581490doi
The 24 patients with gastric ulcer were treated ranitidine (2 x 150 mg daily) or Nocloprost (2 x 200 micrograms daily). The effects of these drugs on the gastric juice components were measured. We evaluated hydrochloric acid, total protein, pepsin and some carbohydrates components secretion. We showed, that ranitidine decreased significantly total protein, fucose, N-acetylneuraminic acid and hexoses contents in the gastric juice in the basal secretion; the same tendency was observed in the pentagastrin-stimulated secretion. The similar direction of the changes, but weakly expressed was confirmed in the patients treated with Nocloprost. It has been shown, that ranitidine modified the gastric mucin components content, what can suggest diminished degradation of mucus directly adhering to the gastric mucosa.