Alminoprofen
(Synonyms: 阿明洛芬,EB-382) 目录号 : GC61689
Alminoprofen是苯丙酸类非甾体抗炎药(NSAID)。Alminoprofen同时具有抑制分泌磷脂酶A2(sPLA2)活性和抗环氧化酶(COX-2)的活性。
Cas No.:39718-89-3
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
Alminoprofen (EB-382) is a nonsteroidal anti-inflammatory drug (NSAID) of the phenylpropionic acid class. Alminoprofen possesses a dual anti-inflammatory action, by inhibiting both secretory phospholipase A2 (sPLA2) and COX-2[1].
Alminoprofen possesses a dual anti-inflammatory action, by inhibiting both sPLA2 but also COX-2. Alminoprofen (from 0 to 50 μM) induces a dose-related inhibitory response on thelevels of PGE2 formed by the CRL-1517 cell line[1].
Alminoprofen (100-300 mg/kg; p.o.) exerts an anti-inflammatory activity[1]. Animal Model: Groups of Wistar Rats (Oedema of the paw)[1]
[1]. Raguenes-Nicol C, et al. Anti-inflammatory mechanism of alminoprofen: action on the phospholipid metabolism pathway. Biochem Pharmacol. 1999;57(4):433-443.
| Cas No. | 39718-89-3 | SDF | |
| 别名 | 阿明洛芬,EB-382 | ||
| Canonical SMILES | O=C(O)C(C)C1=CC=C(NCC(C)=C)C=C1 | ||
| 分子式 | C13H17NO2 | 分子量 | 219.28 |
| 溶解度 | 储存条件 | 4°C, protect from light | |
| 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 | 4.5604 mL | 22.8019 mL | 45.6038 mL |
| 5 mM | 0.9121 mL | 4.5604 mL | 9.1208 mL |
| 10 mM | 0.456 mL | 2.2802 mL | 4.5604 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。
Enantioseparation and determination of Alminoprofen in rat plasma and its application to a stereoselective pharmacokinetic study
J Pharm Biomed Anal 2020 Nov 30;191:113552.PMID:32877823DOI:10.1016/j.jpba.2020.113552.
An enantioselective study of Alminoprofen (AMF) in rat plasma was performed by a rapid, specific and sensitive chiral liquid chromatography-tandem mass spectrometry (LCMS/MS) method. A homemade β-cyclodextrin (β-CD) derivatized based chiral column and a commercial polysaccharide type chiral column were selected and evaluated. The former one per-4-chlorophenylcarbamate-β-CD bonded chiral stationary phase (CSP) which was synthesized in our lab produced the enhanced enantioselective separation. The dextro-ketoprofen (d-KTF) was selected as the internal standard (IS). The approach was linear in the concentration ranges of 1.00-20000.0 ng mL-1 (r2≥0.99) for each enantiomer. The mean recoveries of R-(-)- and S-(+)-AMF at three spiked levels of 2.00, 1000.0 and 16000.0 ng mL-1 ranged from 92.0 %-96.1 %, and the intra-day and inter-day relative standard deviations (RSDs) were within 8.9 %. The lower limit of quantification (LLOQ) values of R-(-)- and S-(+)-AMF in rat plasma matrices were both 1.00 ng mL-1. The established method was successfully applied to a stereoselective pharmacokinetic study of AMF enantiomers in rat plasma following oral administration. The pharmacokinetic results revealed that S-(+)-AMF displayed prominently higher Cmax and AUC values than R-(-)-enantiomer.
[The anti-pyretic mechanism of Alminoprofen]
Nihon Yakurigaku Zasshi 1991 Dec;98(6):457-66.PMID:1783327DOI:10.1254/fpj.98.6_457.
The anti-pyretic activity of Alminoprofen (AP), a non-steroidal anti-inflammatory agent, and its mode of action were investigated in conscious febrile rabbits. A fever was evoked by i.v. injection of lipopolysaccharide (LPS), intracisternal (i.c.) injection of leukocytic pyrogen (LP) or i.c. injection of arachidonic acid (AA). The amount of PGE2 or AP in the cerebrospinal fluid (CSF) after i.v. LPS was estimated using an RIA or HPLC method. AP (3-30 mg/kg, p.o.) dose-dependently inhibited the LPS (0.5 micrograms/kg, i.v.)-induced fever; AP, ibuprofen, indomethacin and pranoprofen had ED50 values of 9.64, 26.45, 4.41 and 11.91 mg/kg, p.o., respectively. PGE2 in the CSF was markedly increased during the elevation of body temperature after i.v. LPS (0.5 microgram/kg). AP (30 mg/kg, p.o.) markedly inhibited the increase in PGE2 that was observed in the CSF during fever developed in response to i.v. LPS (0.5 micrograms/kg). The AP concentration in the CSF 2 hr after AP (30 mg/kg, p.o.) was 2.86 x 10(-6) (1.15-4.57 x 10(-6) M, a concentration too low to inhibit PG synthesis. A dose-dependent fever was observed after i.c. LP (1-8 unit) or AA (10-100 micrograms). AP (30 mg/kg, p.o.) shifted the dose-response curves for the i.c. LP-induced fever to the right, but did not have any effect on the i.c. AA-induced fever. These results suggest that AP has a relatively potent anti-pyretic activity, and its mechanism of action involves competition with LP at a site in the CNS, but does not involve an inhibition of cyclooxygenase at a central site, which has been considered as an anti-pyretic mechanism of nonsteroidal anti-inflammatory drugs.
Anti-inflammatory mechanism of Alminoprofen: action on the phospholipid metabolism pathway
Biochem Pharmacol 1999 Feb 15;57(4):433-43.PMID:9933032DOI:10.1016/s0006-2952(98)00312-8.
Alminoprofen is a nonsteroidal anti-inflammatory drug (NSAID) of the phenylpropionic acid class. It has anti-inflammatory properties different from the classical NSAID. Using both in vitro systems of cells in culture and in vivo models of inflammation, we report here that Alminoprofen possesses both antiphospholipase A2 (PLA2) activity and anti-cycloxygenase (COX) activity. The PLA2 targeted by Alminoprofen is likely the secretory phospholipase A2 (sPLA2) while the COX targeted is the COX-2.
[Effects of Alminoprofen on the allergic reactions]
Nihon Yakurigaku Zasshi 1990 Dec;96(6):315-21.PMID:2076851DOI:10.1254/fpj.96.6_315.
The effects of Alminoprofen, a nonsteroidal anti-inflammatory agent, on the experimental animal models of allergic reactions were examined and compared with those of ibuprofen. Alminoprofen at 30 mg/kg given intraduodenally significantly suppressed passive anaphylactic bronchoconstrictions, while ibuprofen did not at the same doses. In vitro studies revealed that Alminoprofen, in contrast to ibuprofen, exerted an inhibitory effect on arachidonate 5-lipoxygenase activity which initiates the bio-synthesis of leukotrienes. Alminoprofen inhibited arachidonic acid-induced ear edema in mice and homologous passive cutaneous anaphylaxis in rats at high doses, while ibuprofen did not at the high doses. From its characteristic feature of inhibitory effects on 5-lipoxygenase activity and the experimental model of type I allergic reaction, it is suggested that Alminoprofen is a new type of nonsteroidal anti-inflammatory agent.
Pharmacological profile of Alminoprofen among four writhing models of mice caused by kaolin, zymosan, acetylcholine and phenylquinone
J Pharmacobiodyn 1990 Jan;13(1):44-8.PMID:2341969DOI:10.1248/bpb1978.13.44.
The effects of Alminoprofen and other non-steroidal antiinflammatory drugs (NSAIDs) on the writhing reaction caused by kaolin, acetylcholine, phenylquinone and zymosan were studied. Aspirin, indomethacin, ibuprofen and diclofenac-Na, as cyclooxygenase inhibitors, showed similar potency ratios on four writhing tests, although, Alminoprofen exhibited a somewhat rather higher potency ratio on kaolin- and zymosan-induced writhing models than on acetylcholine- and phenylquinone-induced writhing models. All NSAIDs, cyclooxygenase inhibitors except Alminoprofen showed similar shapes in illustrations of potency ratio when the potency of aspirin was expressed as 1.0. The potency of Alminoprofen produced a figure unlike those of other cyclooxygenase inhibitors. These results suggest that Alminoprofen has a different pharmacological profile from other general NSAIDs in terms of analgesic action. This combination method with potency ratios for writhing reactions caused by the above four inducers could be a simple method for classification of pharmacological profiles of the analgesic actions of NSAIDs.