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Rg3039

Name: Rg3039
Brand: TargetMol
SKU: T3336
Price: 297 CNY
Availability: InStock
Rating: 5 (10 reviews)

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很棒

纯度: 99.58%

货号 T3336Cas号 1005504-62-0

别名 PF-06687859

Rg3039 (PF-06687859) 是一种具有口服活性、能够透过血脑屏障的DcpS 抑制剂，其IC50=0.069 nM。

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Rg3039

一键复制产品信息

很棒

纯度: 99.58%

货号 T3336 别名 PF-06687859Cas号 1005504-62-0

Rg3039 (PF-06687859) 是一种具有口服活性、能够透过血脑屏障的DcpS 抑制剂，其IC50=0.069 nM。

规格	价格	库存
2 mg	¥ 297	现货
5 mg	¥ 496	现货
10 mg	¥ 792	现货
25 mg	¥ 1,590	现货
50 mg	¥ 2,430	现货
100 mg	¥ 3,580	现货
500 mg	¥ 7,780	现货

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TargetMol的所有产品仅用作科学研究或药证申报，不能被用于人体，我们不向个人提供产品和服务。请您遵守承诺用途，不得违反法律法规规定用于任何其他用途。

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纯度: 99.58%

颜色: 白色

性状: Solid

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产品介绍

Rg3039 AI Summary

Rg3039 exhibits potent inhibition of human DcpS with an IC50 of 0.069 nM, indicating potential as a therapeutic agent for increasing SMN2 promoter activity. It also shows an IC50 of 4.2 nM for the same enzyme and demonstrates significant brain distribution in the spinal muscular atrophy mouse model, with an AUC of 6762.0 ng.hr.mL-1 and a high brain to plasma ratio of 16.0. The compound's pharmacokinetic profile includes high intrinsic clearance in human liver microsomes (> 250.0 mL.min-1.g-1), good passive cell permeability, and a high efflux ratio in MDR1-expressing cells. It has a log D value of 2.8 at pH 7.4 and high kinetic solubility at pH 6.5. Although it shows good stability in human liver microsomes with a stability of 3.0 minutes at 1 uM, it also exhibits moderate cytotoxicity against human HepG2 cells with an IC50 value of 4000.0 nM. In terms of antiviral activity, Rg3039 inhibits SARS-CoV-2 3CL-Pro protease activity by 13.4% at a concentration of 20μM and shows antiviral effects in VERO-6 cells at 10 uM concentration with an inhibition rate of -0.33% after 48 hours of exposure. The compound's efficacy and activity in the spinal muscular atrophy mouse model vary, demonstrating survival rates ranging from 26.0% to 90.0% depending on dosing and administration routes..

Note: Summary generated by AI. Data source: ChEMBL

生物活性

产品描述	Rg3039 (PF-06687859) is a potent DcpS inhibitor. DcpS is a therapeutic target for spinal muscular atrophy. Spinal muscular atrophy (SMA) is caused by deletion or mutation of both copies of the SMN1 gene which produces an essential protein known as SMN. RG3039 improves motor function in SMA mice. RG3039 also showed activity to improve survival, function and motor unit pathologies in two SMA mouse models.
靶点活性	DcpS:0.069 nM.
别名	PF-06687859

化学信息

分子量	432.35
分子式	C₂₁H₂₃Cl₂N₅O
CAS No.	1005504-62-0
Smiles	Nc1nc(N)c2c(OCC3CCN(Cc4c(Cl)cccc4Cl)CC3)cccc2n1
密度	1.375 g/cm3 (Predicted)

储存&溶解度

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

溶解度信息

H2O: < 0.1 mg/mL (insoluble)

DMSO: 2.69 mg/mL (6.22 mM), Sonication is recommended.

溶液配制表

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.3129 mL	11.5647 mL	23.1294 mL	115.6470 mL
5 mM	0.4626 mL	2.3129 mL	4.6259 mL	23.1294 mL

计算器

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稀释计算器
配液计算器
分子量计算器

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：

比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10只，您使用的配方为 10% DMSO + 40% PEG300 + 5% Tween 80 + 45% Saline / PBS / ddH₂O，那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 100 μL DMSO （母液浓度为 20 mg/mL ）, 如您需要配置的浓度超过该产品的溶解度，请先与我们联系。