CYM 2503
(Synonyms: (9H-芴-9-基)甲基((S)-1(((S)-6-(叔丁氧基羰基)氨基-1-((4-甲基-2-氧代-1,2-二氢喹啉-7-基)氨基)-1-氧代己-2-基)氨基)-3-环己基-1-氧代丙-2-基)氨基甲酸叔丁酯) 目录号 : GC49767
A GAL2 receptor positive allosteric modulator
Cas No.:1308833-36-4
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
CYM 2503 is a positive allosteric modulator (PAM) of the galanin-2 (GAL2) receptor.1 It enhances the production of inositol monophosphate (IP1) induced by galanin in HEK293 cells expressing the GAL2 receptor (EC50 = 0.69 µM). CYM 2503 (60 mg/kg) increases the latency to first electrographic and behavioral seizures and reduces mortality in a lithium-pilocarpine (Li-pilocarpine) rat model of status epilepticus.
1.Lu, X., Roberts, E., Xia, F., et al.GalR2-positive allosteric modulator exhibits anticonvulsant effects in animal modelsProc. Natl. Acad. Sci. USA107(34)15229-15234(2010)
| Cas No. | 1308833-36-4 | SDF | Download SDF |
| 别名 | (9H-芴-9-基)甲基((S)-1(((S)-6-(叔丁氧基羰基)氨基-1-((4-甲基-2-氧代-1,2-二氢喹啉-7-基)氨基)-1-氧代己-2-基)氨基)-3-环己基-1-氧代丙-2-基)氨基甲酸叔丁酯 | ||
| Canonical SMILES | CC(C1=CC=C(C=C1N2)NC([C@H](CCCCNC(OC(C)(C)C)=O)NC([C@H](CC3CCCCC3)NC(OCC4C5=CC=CC=C5C6=CC=CC=C64)=O)=O)=O)=CC2=O | ||
| 分子式 | C45H55N5O7 | 分子量 | 778 |
| 溶解度 | DMSO : 100 mg/mL (128.54 mM; Need ultrasonic) | 储存条件 | -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 | 1.2853 mL | 6.4267 mL | 12.8535 mL |
| 5 mM | 0.2571 mL | 1.2853 mL | 2.5707 mL |
| 10 mM | 0.1285 mL | 0.6427 mL | 1.2853 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。
Structure activity relationships of novel antiepileptic drugs
Curr Med Chem 2014;21(6):722-54.PMID:24251563DOI:10.2174/0929867320666131119153215.
Despite notable success over years in the discovery and development of new antiepileptic drugs (AEDs), about 30-40% of the patients are resistant to drug treatment. There is a still significant need to develop novel AEDs that demonstrate superior efficacy, broad spectrum of activities and good safety profile. The synaptic vesicle glycoprotein 2A (SV2A), α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor (AMPA-R) and voltage-gated potassium channels (KCNQ2/Q3) are clinically validated as new molecular targets for epilepsy. The discovery of SV2A as a target for levetiracetam, 2,3-benzodiazepine GYKI 52466 as a non-competitive AMPA-R antagonist and retigabine as a KCNQ2/Q3 channels activator provided a rational basis to develop novel AEDs. The optimization of SV2A binding affinity of levetiracetam led to the discovery of novel high affinity SV2A ligands that displayed superior efficacy and protective index in animal models of epilepsy. The high-throughput screening (HTS) and medicinal chemistry efforts yielded many non-competitive AMPA-R antagonists of which perampanel was recently approved as a first-in-a new class. The efficacy and lack of sub-type selectivity of retigabine prompted many research efforts to discover several potent and selective KCNQ2/Q3 channel activators of distinct chemical scaffolds that are at various stages of clinical development. Despite the known role of galanin and galanin receptor (Gal-R) in epilepsy over a decade, development of potent and brainpenetrant Gal-R agonists is very challenging. The discovery of selective Gal-R2 positive allosteric modulator, CYM 2503, offers a valuable and an alternative approach. The review focuses on the available structure-activity relationships and preclinical efficacy of novel antiepileptic compounds that are distinct from most of the approved AEDs, specifically SV2A ligands, non-competitive AMPA-R antagonists, KCNQ2/Q3 channels activators and Gal-R modulators.