ALK4290
(Synonyms: AKST4290) 目录号 : GC62833
ALK4290 (AKST4290) 是一种有效的，具有口服活性的 CCR3 抑制剂，对 hCCR3 的 Ki 值为 3.2 nM，详细信息请参考专利文献 US20130261153A1 中的化合物 Example 2。ALK4290 可用于研究新生血管性年龄相关性黄斑变性和帕金森症。
Cas No.:1251528-23-0
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
ALK4290 (AKST4290) is a potent and orally actively CCR3 inhibitor extracted from patent US20130261153A1, compound Example 2, with a Ki of 3.2 nM for hCCR3[1]. ALK4290 can be used for the research of neovascular age-related macular degeneration and Parkinsonism[2][3].
[1]. NIVENS MC, et, al. Use of ccr3-inhibitors. US20130261153A1.
[2]. Samanta A, te, al. Emerging Therapies in Neovascular Age-Related Macular Degeneration in 2020. Asia Pac J Ophthalmol (Phila). May-Jun 2020; 9(3):250-259.
[3]. Clinical Development of AKST4290 as a Novel Parkinson’s Therapeutic
| Cas No. | 1251528-23-0 | SDF | |
| 别名 | AKST4290 | ||
| 分子式 | C27H34ClN5O3 | 分子量 | 512.04 |
| 溶解度 | DMSO : 50 mg/mL (97.65 mM; ultrasonic and warming and heat to 60°C) | 储存条件 | |
| 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 | 1.953 mL | 9.7649 mL | 19.5297 mL |
| 5 mM | 0.3906 mL | 1.953 mL | 3.9059 mL |
| 10 mM | 0.1953 mL | 0.9765 mL | 1.953 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。
SAFETY AND THERAPEUTIC EFFECTS OF ORALLY ADMINISTERED AKST4290 IN NEWLY DIAGNOSED NEOVASCULAR AGE-RELATED MACULAR DEGENERATION
Retina 2022 Jun 1;42(6):1038-1046.PMID:35537111DOI:10.1097/IAE.0000000000003446
Purpose: To evaluate the safety and therapeutic effects of orally administered AKST4290 (formerly BI 144807 and ALK4290) in treatment-naive patients with neovascular age-related macular degeneration. Methods: In this prospective, multicenter, open-label Phase 2a pilot clinical study, 30 patients with newly diagnosed neovascular age-related macular degeneration self-administered AKST4290 (400 mg) orally twice daily for 6 weeks. Patients were examined weekly for safety, to measure best-corrected visual acuity (BCVA), and to perform exploratory morphologic assessments. The primary endpoint was the mean change in BCVA from baseline to end of treatment, and the secondary endpoint was safety. Exploratory endpoints investigated potential changes in macular morphology. Results: Mean BCVA improved by +7.0 letters (95% CI, 2.2-11.7); 24 patients (82.8%) had stable or improved BCVA, with 6 (20.7%) gaining ≥15 letters. No patients experienced severe or serious adverse events. Conclusion: In this 6-week study, AKST4290 treatment was associated with improved BCVA scores in patients with treatment-naive neovascular age-related macular degeneration. All adverse events were mild or moderate in severity and no safety issues were identified. Treatment of neovascular age-related macular degeneration with AKST4290 warrants further investigation in randomized, placebo-controlled trials.