(±)-5'-Chloro-5'-deoxy-ENBA
目录号 : GC17413
adenosine A1 receptor agonist, selective and high-affinity
Cas No.:103626-26-2
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
(±)-5'-Chloro-5'-deoxy-ENBA is a selective and high-affinity adenosine A1 receptor agonist with Ki values of 0.51 [1].
Adenosine A1 receptor mediated neuroand cardioprotection (an antiarrhythmic effect), reduction of lipolysis in adipose tissue and reduction of neuropathic pain [1].
In mice injected with formalin at doses between 1 and 2mg/kg, (±)-5'-Chloro-5'-deoxy-ENBA inhibited the first and the second phases of the nocifensive response induced by formalin [1]. In a mouse model of neuropathic pain (the Spared Nerve Injury (SNI) of the sciatic nerve), (±)-5'-Chloro-5'-deoxy-ENBA (0.5 mg/kg) reduced thermal hyperalgesia and mechanical allodynia 7 and 3 days post-SNI without significantly changed the motor coordination and arterial blood pressure. Also, (±)-5'-Chloro-5'-deoxy-ENBA chronic treatment reduced activated and hypertrophic microglia [2]. In a Parkinson's disease (PD) mouse model, (±)-5'-Chloro-5'-deoxy-ENBA prevented the increase in sIPSC frequency and eIPSC amplitude produced by SKF. In mice with unilateral DA denervation, (±)-5'-Chloro-5'-deoxy-ENBA reduced the development of abnormal involuntary movements induced by L-DOPA [3].
References:
[1]. Franchetti P, Cappellacci L, Vita P, Petrelli R, et al. N6-Cycloalkyl- and N6-bicycloalkyl-C5'(C2')-modified adenosine derivatives as high-affinity and selective agonists at the human A1 adenosine receptor with antinociceptive effects in mice. J Med Chem, 2009, 52(8): 2393-2406.
[2]. Luongo L, Petrelli R, Gatta L, et al. 5'-Chloro-5'-deoxy-(±)-ENBA, a potent and selective adenosine A(1) receptor agonist, alleviates neuropathic pain in mice through functional glial and microglial changes without affecting motor or cardiovascular functions. Molecules, 2012, 17(12): 13712-13726.
[3]. Mango D, Bonito-Oliva A, Ledonne A, et al. Adenosine A1 receptor stimulation reduces D1 receptor-mediated GABAergic transmission from striato-nigral terminals and attenuates l-DOPA-induced dyskinesia in dopamine-denervated mice. Exp Neurol, 2014, 261: 733-743.
| Cas No. | 103626-26-2 | SDF | |
| 化学名 | (2R,3R,4S,5S)-2-(6-((1R,2R,4R)-bicyclo[2.2.1]heptan-2-ylamino)-9H-purin-9-yl)-5-(chloromethyl)tetrahydrofuran-3,4-diol | ||
| Canonical SMILES | ClC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)N2C(N=CN=C3N[C@H]4[C@H](CC5)C[C@@H]5C4)=C3N=C2 | ||
| 分子式 | C17H22ClN5O3 | 分子量 | 379.84 |
| 溶解度 | <37.98mg/ml in DMSO; <37.98mg/ml in ethanol | 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 | 2.6327 mL | 13.1634 mL | 26.3269 mL |
| 5 mM | 0.5265 mL | 2.6327 mL | 5.2654 mL |
| 10 mM | 0.2633 mL | 1.3163 mL | 2.6327 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。