Oleanolic Acid Acrylate
(Synonyms: OAA) 目录号 : GC45535
A 5-HT1A receptor agonist
Cas No.:1975976-24-9
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >95.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Oleanolic acid acrylate (OAA) is an agonist of the serotonin (5-HT) receptor subtype 5-HT1A and a derivative of oleanolic acid .1 It acts as an agonist at the 5-HT1A receptor in mouse hippocampal homogenates in a [35S]GTPγS binding assay (EC50 = 0.79 μM). It is also a selective inhibitor of MAO-A over MAO-B (IC50s = 48.8 μM and >100 μM, respectively). In mice, OAA (10 mg/kg) reduces immobility in the forced swim test and increases the number of crossings and time spent at the center in the open field test, indicating anti-depressant-like and anxiolytic activities.
References
1. Fajemiroye, J.O., Polepally, P.R., Chaurasiya, N.D., et al. Oleanolic acid acrylate elicits antidepressant-like effect mediated by 5-HT1A receptor. Sci. Rep. 5, 11582 (2015).
| Cas No. | 1975976-24-9 | SDF | |
| 别名 | OAA | ||
| Canonical SMILES | CC1(C)CC[C@]2(C(O)=O)CC[C@@]3(C)[C@]4(C)CC[C@@]5([H])C(C)(C)[C@@H](OC(C=C)=O)CC[C@]5(C)[C@@]4([H])CC=C3[C@]2([H])C1 | ||
| 分子式 | C33H50O4 | 分子量 | 510.7 |
| 溶解度 | DMF: 30mg/mL,DMSO: 20mg/mL,Ethanol: 30mg/mL,Ethanol:PBS (pH 7.2) (1:40): 0.02mg/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 | 1.9581 mL | 9.7905 mL | 19.581 mL |
| 5 mM | 0.3916 mL | 1.9581 mL | 3.9162 mL |
| 10 mM | 0.1958 mL | 0.979 mL | 1.9581 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。
Oleanolic Acid Acrylate elicits antidepressant-like effect mediated by 5-HT1A receptor
Sci Rep 2015 Jul 22;5:11582.PMID:26199018DOI:10.1038/srep11582.
The development of new drugs for the treatment of depression is strategic to achieving clinical needs of patients. This study evaluates antidepressant-like effect and neural mechanisms of four oleanolic acid derivatives i.e. acrylate (D1), methacrylate (D2), methyl fumarate (D3) and ethyl fumarate (D4). All derivatives were obtained by simple one-step esterification of oleanolic acid prior to pharmacological screening in the forced swimming (FS) and open field (OF) tests. Pharmacological tools like α-methyl-p-tyrosine (AMPT, catecholamine depletor), p-chlorophenylalanine (serotonin depletor), prazosin (PRAZ, selective α1-receptor antagonist), WAY-100635 (selective serotonin 5-HT1A receptor antagonist) as well as monoamine oxidase (MAO) and functional binding assays were conducted to investigate possible neural mechanisms. In the FS test, D1 showed the most promising antidepressant-like effect without eliciting locomotor incoordination. Unlike group of mice pretreated with AMPT 100 mg/kg, PCPA 100 mg/kg or PRAZ 1 mg/kg, the effect of D1 was attenuated by WAY-100635 0.3 mg/kg pretreatment. D1 demonstrated moderate inhibition of MAO-A (IC50 = 48.848 ± 1.935 μM), potency (pEC50 = 6.1 ± 0.1) and intrinsic activity (E max = 26 ± 2.0%) on 5-HT1A receptor. In conclusion, our findings showed antidepressant-like effect of D1 and possible involvement of 5-HT1A receptor.