GlpBio

RG3039 (PF-06687859)

目录号: GC30784纯度: >99.50%同义词: 5-[[1-(2,6-二氯苄基)哌啶-4-基]甲氧基]喹唑啉-2,4-二胺,PF-06687859
A DcpS inhibitor
RG3039 (PF-06687859)
Cas No.: 1005504-62-0
规格价格库存数量操作
5mg¥589.00现货
1
10mg¥884.00现货
1
25mg¥1,741.00现货
1
50mg¥2,945.00现货
1
100mg¥4,455.00现货
1
10mM (in 1mL DMSO)¥578.00现货
1
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文献被引

本产品暂无引用记录;以下为 GlpBio 产品在 Nature / Cell / Science 等顶刊的客户引用样例
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    Cell
    187(9):2288-2304 (2024)
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    183(7):1867-1883 (2020)
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产品描述 Description

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)

实验参考方法 Experimental Reference Method

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.
[2]. Gogliotti RG, et al. The DcpS inhibitor RG3039 improves survival, function and motor unit pathologies in two SMA mouse models. Hum Mol Genet. 2013 Oct 15;22(20):4084-101.
[3]. Van Meerbeke J, et al. The DcpS inhibitor RG3039 improves motor function in SMA mice. Hum Mol Genet. 2013 Oct 15;22(20):4074-83.

产品文档 Product Documents

Purity:>99.50%

化学性质Chemical Properties

CAS 号
1005504-62-0
同义词
5-[[1-(2,6-二氯苄基)哌啶-4-基]甲氧基]喹唑啉-2,4-二胺,PF-06687859
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 g/mol
溶解性
DMSO : 6 mg/mL (13.88 mM);Water : < 0.1 mg/mL (insoluble)
保存条件
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°C，然后在超声波浴中震荡一段时间。
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。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

g/mol