RG3039 (PF-06687859)
(Synonyms: 5-[[1-(2,6-二氯苄基)哌啶-4-基]甲氧基]喹唑啉-2,4-二胺,PF-06687859) 目录号 : GC30784
A DcpS inhibitor
Cas No.:1005504-62-0
Sample solution is provided at 25 µL, 10mM.
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RG3039 is an inhibitor of mRNA decapping scavenger enzyme (DcpS; IC50 = 0.069 nM).1 It prevents denervation of the neuromuscular junction (NMJ) and decreases in NMJ synaptic transmission and myofiber size of the longissimus muscle in a mouse model of spinal muscular atrophy (SMA) induced by knockout of the gene encoding survival motor neuron 1 (Smn1) when administered at a dose of 10 mg/kg.2 RG3039 improves survival and motor function in the same model.
1.Gopalsamy, A., Narayanan, A., Liu, S., et al.Design of potent mRNA decapping scavenger enzyme (DcpS) inhibitors with improved physicochemical properties to investigate the mechanism of therapeutic benefit in spinal muscular atrophy (SMA)J. Med. Chem.60(7)3094-3108(2017) 2.Van Meerbeke, J.P., Gibbs, R.M., Plasterer, H.L., et al.The DcpS inhibitor RG3039 improves motor function in SMA miceHum. Mol. Genet.22(20)4074-4083(2013)
Animal experiment: | Mice: Mice receive intraperitoneal (i.p.) injections of RG3039 starting on post natal day 1 (P1) defined as the day of birth. All treated litters are culled at P4 to a total of six pups. Daily weights and righting-time are determined starting on P1. Ambulation index is performed between P13 and P23. A compilation score is determined during two 60 s trials[3]. |
References: [1]. Gopalsamy A, et al. Design of Potent mRNA Decapping Scavenger Enzyme (DcpS) Inhibitors with Improved Physicochemical Properties To Investigate the Mechanism of Therapeutic Benefit in Spinal Muscular Atrophy (SMA). J Med Chem. 2017 Apr 13;60(7):3094-3108. | |
| Cas No. | 1005504-62-0 | SDF | |
| 别名 | 5-[[1-(2,6-二氯苄基)哌啶-4-基]甲氧基]喹唑啉-2,4-二胺,PF-06687859 | ||
| Canonical SMILES | NC1=NC(N)=C2C(OCC3CCN(CC4=C(Cl)C=CC=C4Cl)CC3)=CC=CC2=N1 | ||
| 分子式 | C21H23Cl2N5O | 分子量 | 432.35 |
| 溶解度 | DMSO : 6 mg/mL (13.88 mM);Water : < 0.1 mg/mL (insoluble) | 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 | 2.3129 mL | 11.5647 mL | 23.1294 mL |
| 5 mM | 0.4626 mL | 2.3129 mL | 4.6259 mL |
| 10 mM | 0.2313 mL | 1.1565 mL | 2.3129 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