Org-26576
目录号 : GC30852
Org26576是AMPA受体的正变构调节剂。
Cas No.:1026791-61-6
Sample solution is provided at 25 µL, 10mM.
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Org 26576 is a AMPA receptor positive allosteric modulator.
Org 26576 represents structurally a distinct chemical series derived from the first generation ampakine CX516 and displays 10-30 fold greater potency when compared to CX516 in potentiating AMPA-mediated electrophysiological responses with an EC50 of 8-16 μM in rat hippocampal primary cultured neurons. Org 26576 demonstrates selectivity for AMPA receptors when tested at 10 μM against >60 molecular targets including G-Protein Coupled Receptors, ion channels and kinases[1].
Org 26576 (1 mg/kg) produces significant increases in the anteroventral and laterodorsal thalamus, cingulate cortex, dentate gyrus and CA3 subfield of the hippocampus in mice[1]. Chronic administration of Org 26576 increases progenitor cell proliferation in dentate gyrus (approximately 40%) and in prelimbic cortex (approximately 35%) at the 10-mg/kg dosage. Cells born in response to chronic Org 26576 in dentate gyrus exhibits increased rates of survival (approximately 30%) with the majority of surviving cells expressing a neuronal phenotype[2]. AMPA receptor potentiation by Org 26576 exerts a positive modulatory influence on brain derived neurotrophic factor (BDNF) expression during ongoing neuronal activity. Total BDNF mRNA levels are significantly increased in the hippocampus of animals exposed to the combination of Org 26576 and stress[3].
[1]. Jordan GR, et al. Regionally selective and dose-dependent effects of the ampakines Org 26576 and Org 24448 on local cerebral glucose utilisation in the mouse as assessed by 14C-2-deoxyglucose autoradiography. Neuropharmacology. 2005 Aug;49(2):254-64. [2]. Su XW, et al. Chronic treatment with AMPA receptor potentiator Org 26576 increases neuronal cell proliferation and survival in adult rodent hippocampus. Psychopharmacology (Berl). 2009 Oct;206(2):215-22. [3]. Fumagalli F, et al. The AMPA receptor potentiator Org 26576 modulates stress-induced transcription of BDNF isoforms in rat hippocampus. Pharmacol Res. 2012 Feb;65(2):176-81.
Animal experiment: | Rats: Saline and Org-26576 (10 mg/kg) are administered, by intraperitoneal injection, 25 min before acute swim stress. Briefly, rats are subjected to a swim stress session for 5 min and sacrificed by decapitation 15 min after the end of the swim session. Brain regions are immediately dissected, frozen on dry ice and stored at -80°C[3]. Mice: Org-26576 (0.1, 1, 10 mg/kg) and Org 24448 (3, 10, 30 mg/kg) or vehicle (5% Mulgofenesaline) are administered intraperitoneally (i.p.) 10 min prior to the administration of the 14C-2-deoxyglucose. All drugs/vehicle are administered in the contralateral side of the abdomen to the 14C-2-deoxyglucose (2-DG) i.p. injection. A separate group of animals is also administered the AMPA receptor antagonist NBQX. NBQX (10 mg/kg) is injected either alone or 10 min prior to the administration of Org-26576 (10 mg/kg i.p.), Org 24448 (10 mg/kg i.p.) or vehicle (5% Mulgofenesaline i.p.). For each drug dose administered nZ5e7. The behavioural effects of all drugs administered are monitored throughout the entirety of procedure, and any alterations in behaviour noted[1]. |
References: [1]. Jordan GR, et al. Regionally selective and dose-dependent effects of the ampakines Org 26576 and Org 24448 on local cerebral glucose utilisation in the mouse as assessed by 14C-2-deoxyglucose autoradiography. Neuropharmacology. 2005 Aug;49(2):254-64. | |
| Cas No. | 1026791-61-6 | SDF | |
| Canonical SMILES | O=C1N2[C@](CCC2)([H])COC3=NC=CC=C13 | ||
| 分子式 | C11H12N2O2 | 分子量 | 204.23 |
| 溶解度 | DMSO : 25 mg/mL (122.41 mM) | 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 | 4.8964 mL | 24.4822 mL | 48.9644 mL |
| 5 mM | 0.9793 mL | 4.8964 mL | 9.7929 mL |
| 10 mM | 0.4896 mL | 2.4482 mL | 4.8964 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。
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet