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RG3039 (Synonyms: PF-06687859)

目录号: HY-102020 纯度: 99.75%
产品使用指南

RG3039 (PF-06687859) 是具有口服活性,可渗透大脑的 DcpS 抑制剂, IC50 值为 0.069 nM。

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RG3039 Chemical Structure

RG3039 Chemical Structure

CAS No. : 1005504-62-0

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10 mM * 1 mL in DMSO ¥726
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5 mg ¥660
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100 mg ¥5600
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  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

RG3039 (PF-06687859) is an orally bioavailable and brain-penetrant DcpS inhibitor with an IC50 of 0.069 nM.

IC50 & Target

IC50: 0.069 nM (DcpS)[1]

体外研究
(In Vitro)

RG3039 is a dibasic lipophilic molecule that is predicted to accumulate in lysosomes[1]. In motor neurons, RG3039 significantly increases both the average number of cells with gems and average number of gems per cell, which is used as an indirect measure of SMN levels[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

RG3039 can extend survival and improve function in two SMA mouse models of varying disease severity (Taiwanese 5058 Hemi and 2B/− SMA mice), and positively impacts neuromuscular pathologies. In 2B/− SMA mice, RG3039 provides a >600% survival benefit (median 18 days to >112 days) when dosing began at P4, highlighting the importance of early intervention[2]. RG3039 distributes to central nervous system tissues where it robustly inhibits DcpS enzyme activity, but minimally activates SMN expression or the assembly of small nuclear ribonucleoproteins. RG3039 treated SMA mice shows a dose-dependent increase in survival, weight and motor function and it is associated with improved motor neuron somal and neuromuscular junction synaptic innervation and function and increased muscle size. RG3039 also enhances survival of conditional SMA mice in which SMN has been genetically restored to motor neurons[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

432.35

Formula

C21H23Cl2N5O

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 5 mg/mL (11.56 mM; ultrasonic and warming and heat to 60°C)

H2O : < 0.1 mg/mL (insoluble)

配制储备液
浓度 溶剂体积 质量 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
*

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, 6 months; -20°C, 1 month。-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。

参考文献
Animal Administration
[3]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献

纯度: 99.75%

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The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2

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产品名称:
RG3039
目录号:
HY-102020
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