15(R)-15-methyl Prostaglandin E2
(Synonyms: 阿伯前列素) 目录号 : GC41165
A prodrug for 15(S)-15-methyl PGE2
Cas No.:55028-70-1
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
15(R)-15-methyl Prostaglandin E2 (15(R)-15-methyl PGE2) is a prodrug for the potent PGE2 analog 15(S)-15-methyl PGE2 . Acid-catalyzed epimerization in the stomach produces the 15(S)-hydroxy compound which is biologically active. Oral administration of 15(R)-15-methyl PGE2 to dogs or rats at 10-300 µg/kg results in a dose-dependent inhibition of gastric acid secretion and an increase in the rate of duodenal bicarbonate secretion.
| Cas No. | 55028-70-1 | SDF | |
| 别名 | 阿伯前列素 | ||
| Canonical SMILES | O=C1[C@H](C/C=C\CCCC(O)=O)[C@@H](/C=C/[C@](C)(O)CCCCC)[C@H](O)C1 | ||
| 分子式 | C21H34O5 | 分子量 | 366.5 |
| 溶解度 | DMF: >100 mg/ml (from PGE2),DMSO: >100 mg/ml (from PGE2),Ethanol: >100 mg/ml (from PGE2),PBS pH 7.2: >5 mg/ml (from PGE2) | 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 | 2.7285 mL | 13.6426 mL | 27.2851 mL |
| 5 mM | 0.5457 mL | 2.7285 mL | 5.457 mL |
| 10 mM | 0.2729 mL | 1.3643 mL | 2.7285 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。
Effect of 15(R)-15-methyl-prostaglandin E2 on iron absorption in the rat
Experientia 1982 Jan 15;38(1):116-7.PMID:7056351DOI:10.1007/BF01944561.
The administration of 15(R)-15-methyl Prostaglandin E2 (15(R)-15-M-PGE2) in vivo significantly diminished the uptake of (59)Fe into blood, spleen, liver, femur and dried intestine of rats, whereas acetylsalicylic acid (ASA) increased the counts significantly. This effect of ASA was counteracted by 15(R)-15-M-PGE2. It is suggested that prostaglandins (PGs)might play an important role in inhibiting iron absorption at the intestinal level.
The effect of 15(R)-15-methyl Prostaglandin E2 on meal-stimulated gastric acid secretion, serum gastrin, and pancreatic polypeptide in duodenal ulcer patients
Dig Dis Sci 1979 May;24(5):381-4.PMID:456224DOI:10.1007/BF01297125.
The effects of 100-microgram of 15(R)-15-methyl Prostaglandin E2 on meal-stimulated acid secretion, serum gastrin, and pancreatic polypeptide concentrations were measured in patients with duodenal ulcer. The drug given in encapsulated or unencapsulated form significantly reduced gastric acid secretion by 59% or 70%, respectively. Rises in serum gastrin and pancreatic polypeptide concentrations after the meal were significantly blunted by 15(R)-15-methyl Prostaglandin E2. This dose of prostaglandin led to no side effects and merits clinical evaluation in the treatment of peptic ulcer disease.
Arbaprostil [15(R)-15-methyl Prostaglandin E2] in a single nighttime dose of either 50 or 100 micrograms in acute duodenal ulcer
Gastroenterology 1989 Jul;97(1):98-103.PMID:2656368DOI:10.1016/0016-5085(89)91421-2.
To determine the efficacy of single nighttime doses of arbaprostil [15(R)-15-methyl Prostaglandin E2], 50 or 100 micrograms for 4 wk, a double-blind randomized placebo-controlled multiclinic trial was undertaken. Success was defined as complete healing of the ulcer documented by endoscopy. Fifty-one of 64 patients enrolled were considered evaluable. Ulcer healing was documented in 64.3%, 85.7%, and 31.2% of the 100-micrograms arbaprostil, 50-micrograms arbaprostil, and placebo treatment groups (p value vs. placebo = 0.003 and 0.002, respectively). No difference in side effects or changes in laboratory parameters were found between the treatment groups except that diarrhea, usually mild, was found more often in the 100-micrograms arbaprostil group (60.0%) than in the 50-micrograms arbaprostil (31.8%) or placebo groups (23.5%) (p value 100 micrograms arbaprostil vs. placebo = 0.02). A single nighttime administration of arbaprostil seems to be a safe and efficacious agent for the treatment of acute duodenal ulcer.
Effect of 15(R)-15-methyl Prostaglandin E2 (arbaprostil) on the healing of duodenal ulcer: a double-blind multicenter study
Gastroenterology 1982 Aug;83(2):357-63.PMID:7044880doi
A multicenter study was conducted on 173 patients with active, endoscopically proven duodenal ulcers (158 men, 15 women). They were randomly assigned, in a double-blind manner, to two groups: those receiving placebo capsules (91 patients) and those receiving capsules containing 100 microgram of 15(R)-15-methyl Prostaglandin E2 (arbaprostil) (82 patients). Each drug was ingested four times a day (1 h before meals and at bedtime) for 28 days. Endoscopy was performed on days 0, 14, and 28 after the trial began. At each examination, the ulcer size was measured and whether the ulcer had healed was recorded. Arbaprostil increased the incidence of ulcer healing to approximately the same degree as reported in most extensive studies with cimetidine. At 14 days, three times as many patients were totally healed in the arbaprostil-treated as in the placebo-treated group (37% vs. 12%, p less than 0.001). At 28 days, 67% of patients receiving arbaprostil were healed compared with 39% in the group receiving placebo (p less than 0.001). Similarly, the ulcer size, measured endoscopically, was much smaller after arbaprostil administration than in the group receiving placebo after both 14 and 28 days (p less than 0.001). Side effects attributable to treatment consisted primarily of loose stools and diarrhea (34%). Smoking retarded healing in the placebo-treated group (p less than 0.05), but did not significantly retard healing in patients treated with arbaprostil. We conclude that arbaprostil markedly accelerates the healing rate of active duodenal ulcers. This effect may be due to inhibition of acid secretion as well as gastric cytoprotection.
Effects of 15(R)-15-methyl Prostaglandin E2 (arbaprostil) on gastric secretion and various gastric lesions induced in rats
Jpn J Pharmacol 1986 Feb;40(2):329-37.PMID:3702150DOI:10.1254/jjp.40.329.
We studied the effects of 15(R)-15-methyl Prostaglandin E2 (arbaprostil) on gastric secretion and various acute and chronic gastric lesions produced in rats. Arbaprostil significantly inhibited gastric secretion in 4 hr-pylorus-ligated preparations when given intraduodenally in a dose of 30 or 100 micrograms/kg. The agent, however, significantly stimulated gastric secretion of rats with either a ligated or intact pylorus when given orally in doses of 3-100 micrograms/kg. Orally administered arbaprostil dose-dependently prevented the development of HCI-ethanol-, histamine-, water-immersion stress-, or indomethacin-induced gastric erosions. Intraduodenally administered arbaprostil also dose-dependently prevented the development of aspirin-induced gastric erosions in pylorus-ligated rats. Arbaprostil, given orally in doses of 1-100 micrograms/kg twice daily for 2 weeks, had little or no effect on the healing of acetic acid-induced gastric ulcers. However, oral administration of the agent in a dose of 3 or 10 micrograms/kg twice daily for 4 weeks significantly accelerated the healing of acetic acid-induced gastric ulcers. The increase in doses up to 100 micrograms/kg twice daily for 4 weeks had no effect on ulcer healing. These results indicate that arbaprostil, at either antisecretory or even acid stimulating doses, is effective in preventing the development of acute gastric erosions and in accelerating the healing of chronic gastric ulcers.