Avanafil
(Synonyms: 阿伐那非; TA1790) 目录号 : GC16856
A potent and selective PDE5 inhibitor
Cas No.:330784-47-9
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
Avanafil is a potent and selective inhibitor of phosphodiesterase type 5 (PDE5) with IC50 value of 5.2nM [1].
PDE5 is abundantly expressed in penile corpus cavernosum and regulates penile blood flow by regulating the cGMP concentration. PDE5 inhibitors are similar in structure to cGMP and competitively bind to PDE5, resulting in the inhibition of cGMP hydrolysis. Avanafil is a high selective inhibitor of PDE5 with Ki value of 4.3nM and is developed for the treatment of erectile dysfunction. It shows high selectivity against other PDE enzymes of the PDE family. In the intravenous study, the administration of avanafil at 300μg/kg can potentiate penile tumescence. The calculated ED200% of avanafil on tumescence is 37.5μg/kg and the plasma concentration is 59.6ng/ml. Additionally, avanafil potentiates penile tumescence at a dose range of 100 to 1,000μg/kg intraduodenally. And the ED200% is 151.7μg/kg [1, 2].
References:
[1] Kotera J, Mochida H, Inoue H, Noto T, Fujishige K, Sasaki T, Kobayashi T, Kojima K, Yee S, Yamada Y, Kikkawa K, Omori K. Avanafil, a potent and highly selective phosphodiesterase-5 inhibitor for erectile dysfunction. J Urol. 2012 Aug;188(2):668-74.
[2] Cui YS, Li N, Zong HT, Yan HL, Zhang Y. Avanafil for male erectile dysfunction: a systematic review and meta-analysis. Asian J Androl. 2014 May-Jun;16(3):472-7.
| Cas No. | 330784-47-9 | SDF | |
| 别名 | 阿伐那非; TA1790 | ||
| 化学名 | (S)-4-((3-chloro-4-methoxybenzyl)amino)-2-(2-(hydroxymethyl)pyrrolidin-1-yl)-N-(pyrimidin-2-ylmethyl)pyrimidine-5-carboxamide | ||
| Canonical SMILES | O=C(C1=CN=C(N2[C@H](CO)CCC2)N=C1NCC3=CC=C(OC)C(Cl)=C3)NCC4=NC=CC=N4 | ||
| 分子式 | C23H26ClN7O3 | 分子量 | 483.95 |
| 溶解度 | ≥ 17.6 mg/mL in DMSO | 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 | 2.0663 mL | 10.3316 mL | 20.6633 mL |
| 5 mM | 0.4133 mL | 2.0663 mL | 4.1327 mL |
| 10 mM | 0.2066 mL | 1.0332 mL | 2.0663 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。