Misoprostol
(Synonyms: 米索前列醇,SC-29333) 目录号 : GC16074
Misoprostol是一种具口服活性的前列腺素E1（PGE1）类似物，用于预防胃溃疡、治疗过期流产、引产和诱导流产。
Cas No.:59122-46-2
Sample solution is provided at 25 µL, 10mM.
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Misoprostol is an orally active prostaglandin E1 (PGE1) analog used to prevent gastric ulcers, treat missed abortion, induce labor and induce miscarriage[1, 2]. Misoprostol is used to prevent gastric ulcers induced by nonsteroidal anti-inflammatory drugs. It can bind to prostaglandin receptors and directly act on parietal cells to inhibit gastric acid secretion[3].
In vitro, Misoprostol (10μM) pretreatment of human peripheral blood mononuclear cells (PBMC) and RAW264.7 cells for 90min significantly increased the phosphorylation of cAMP response element binding protein (CREB) in cells[4]. Misoprostol (10μM) treatment of HCT-116 cells for 2h significantly activated intracellular protein kinase A (PKA)[5]. Misoprostol (8ng/mL) treatment of 3D cultured annular cells significantly increased the epidermal growth factor (EGF) level of cells[6].
In vivo, oral administration of Misoprostol (0.2mg/kg/day) to rats with doxorubicin-induced cardiac injury for 6 days alleviated cardiac injury in rats, significantly reduced serum cardiac troponin-I (cTn-I) and brain natriuretic peptide (BNP) levels, and reduced lactate dehydrogenase (LDH), aspartate aminotransferase (AST), alanine aminotransferase (ALT), and creatine kinase isoenzyme-MB (CK-MB) activities[7].
References:
[1] Ahmed T A, Mohammed A H. Brief Overview About Prostaglandins & Misoprostol For Cervical Ripening[J]. Journal of Pharmaceutical Negative Results, 2023, 14(2).
[2] Chong Y S, Su L L, Arulkumaran S. Misoprostol: a quarter century of use, abuse, and creative misuse[J]. Obstetrical & gynecological survey, 2004, 59(2): 128-140.
[3] Sostres C, Lanas A. Prostaglandins and other mucosal protecting agents[J]. Pocket Guide to Gastrointestinal Drugs, 2014: 44-56.
[4] Gobejishvili L, Ghare S, Khan R, et al. Misoprostol modulates cytokine expression through a cAMP pathway: Potential therapeutic implication for liver disease[J]. Clinical Immunology, 2015, 161(2): 291-299.
[5] Field J T, Martens M D, Mughal W, et al. Misoprostol regulates Bnip3 repression and alternative splicing to control cellular calcium homeostasis during hypoxic stress[J]. Cell Death Discovery, 2018, 4(1): 98.
[6] Gruber H E, Hoelscher G, Loeffler B, et al. Prostaglandin E1 and misoprostol increase epidermal growth factor production in 3D-cultured human annulus cells[J]. The Spine Journal, 2009, 9(9): 760-766.
[7] Bilgic S, Ozgocmen M, Ozer M K, et al. Misoprostol ameliorates doxorubicin induced cardiac damage by decreasing oxidative stress and apoptosis in rats[J]. Biotechnic & Histochemistry, 2020, 95(7): 514-521.
Misoprostol是一种具口服活性的前列腺素E1（PGE1）类似物，用于预防胃溃疡、治疗过期流产、引产和诱导流产[1, 2]。Misoprostol用于预防非甾体抗炎药诱发的胃溃疡，能够与前列腺素受体结合直接作用于壁细胞来抑制胃酸分泌[3]。
在体外，Misoprostol（10μM）预处理人外周血单核细胞（PBMC）和RAW264.7细胞90min，显著增加了细胞中cAMP反应元件结合蛋白（CREB）的磷酸化[4]。Misoprostol（10μM）处理HCT-116细胞2h，显著激活了细胞内蛋白激酶A（PKA）[5]。Misoprostol（8ng/mL）处理3D培养的环状细胞，显著增加了细胞的表皮生长因子（EGF）水平[6]。
在体内，Misoprostol（0.2mg/kg/day）通过口服治疗阿霉素诱导的心脏损伤大鼠6天，减轻了大鼠的心脏损伤，显著降低了血清心肌肌钙蛋白-I（cTn-I）和脑钠肽（BNP）水平，降低了乳酸脱氢酶（LDH）、天冬氨酸转氨酶（AST）、丙氨酸转氨酶（ALT）和肌酸激酶同工酶-MB（CK-MB）活性[7]。
| Cell experiment [1]: | |
Cell lines | Human peripheral blood mononuclear cells (PBMCs)、RAW264.7 cells |
Preparation Method | Cells were plated at 0.5 million/mL density, treated with 10μM Misoprostol for 90min and further stimulated with LPS, 100ng/mL. PKA inhibitor, H89 was used at 10μM concentration 30min before Misoprostol treatment. Nuclear extracts were subjected to Western blot analysis. |
Reaction Conditions | 10μM; 90min |
Applications | Misoprostol exposure resulted in increased phosphorylation of cAMP response element-binding protein (CREB) in both PBMCs and RAW cells; pretreatment with PKA inhibitor, H89 prevented Misoprostol effect on CREB phosphorylation. |
| Animal experiment [2]: | |
Animal models | Sprague-Dawley rats |
Preparation Method | Divided the rats randomly into three groups of seven: group 1, control; group 2, Doxorubicin; group 3, Doxorubicin+ MP. The control group was injected intraperitoneally (i.p.) with 0.5mL 0.9% NaCl and given 1mL 0.9% NaCl orally for 6 days. The Doxorubicin group was injected i.p. with a single dose of 20mg/kg Doxorubicin on the third day of the study. The Doxorubicin+Misoprostol group was injected i.p. with a single 20mg/kg dose of Doxorubicin on day 3 of the study and given 0.2mg/kg/day Misoprostol orally for 6 days. The treatment course lasted 6 days for all groups. |
Dosage form | 0.2mg/kg/day for 6 days; p.o. |
Applications | Cardiac damage caused by Doxorubicin was attenuated by Misoprostol treatment. Treatment with Misoprostol decreased significantly serum cardiac troponin-I, brain natriuretic peptide levels, and lactate dehydrogenase, aspartate aminotransferase, alanine transaminase and creatine kinase isoenzyme-MB activities. Misoprostol also decreased NADPH oxidase-4 and caspase-3 levels. |
References: | |
| Cas No. | 59122-46-2 | SDF | |
| 别名 | 米索前列醇,SC-29333 | ||
| 化学名 | methyl 7-((1R,2R,3R)-3-hydroxy-2-((E)-4-hydroxy-4-methyloct-1-en-1-yl)-5-oxocyclopentyl)heptanoate | ||
| Canonical SMILES | CCCCC(C/C([H])=C([H])/[C@]1([H])[C@@](C(C[C@@]1([H])O)=O)([H])CCCCCCC(OC)=O)(O)C | ||
| 分子式 | C22H38O5 | 分子量 | 382.53 |
| 溶解度 | ≥ 11.05mg/mL in DMSO | 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 | 2.6142 mL | 13.0709 mL | 26.1417 mL |
| 5 mM | 0.5228 mL | 2.6142 mL | 5.2283 mL |
| 10 mM | 0.2614 mL | 1.3071 mL | 2.6142 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。
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Quality Control & SDS
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- Purity: >98.00%
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