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Branaplam {[allProObj[0].p_purity_real_show]}

货号：A758913 同义名： LMI070;NVS-SM1

LMI070 is a highly potent, selective and orally active small molecule SMN2 splicing modulator.

Branaplam 化学结构 CAS号：1562338-42-4
Branaplam 化学结构
CAS号：1562338-42-4
Branaplam 3D分子结构
CAS号：1562338-42-4
Branaplam 化学结构 CAS号：1562338-42-4
Branaplam 3D分子结构 CAS号：1562338-42-4
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Branaplam 纯度/质量文件 产品仅供科研

货号：A758913 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 DNA synthesis ↓ helicase ↓ RdRp ↓ ribonucleotide reductase ↓ tRNA synthetase ↓ YB-1 ↓ 其他靶点 纯度
Fexinidazole ✔ 98%
Daptomycin ✔ 98%
Blasticidin S·HCl ✔ 98%
Metronidazole ✔ 98%
Daunorubicin HCl +++

DNA synthesis, Ki: 20 nM

 		98%
Triglycidyl isocyanurate ✔ p53 98+%
Nedaplatin ✔ 99%+
Bendamustine ✔ 98+%
Trifluridine ✔ 98%
Robinetin ✔ 99%+
Carboplatin ✔ 99%
Cidofovir ✔ 99%
Cisplatin ✔ 99%
Cytarabine ++++

DNA synthesis, IC50: 16 nM

 		98%
Acelarin ++++

DNA synthesis, EC50: 0.2 nM

 		99%+
Oxaliplatin ✔ 98%
YK-4-279 ✔ 99%+
ML216 +

BLM636-1298, IC50: 0.97 μM

BLMfull-length, IC50: 2.98 μM

 		99%+
RK-33 ✔ 98%
Brr2-IN-3 ✔ 99%+
Phen-DC3 Trifluoromethanesulfonate ✔ 98%
Favipiravir ✔ 97%
Suramin sodium salt ++

RdRp, IC50: 0.26 μM

 		99%+
Clofarabine ++

Ribonucleotide reductase, IC50: 65 nM

 		97%
Didox ✔ 98%
(E)-3-AP ✔ 97%
Halofuginone +++

prolyl-tRNA synthetase, Ki: 18.3nM

 		99%+
BC-LI-0186 +++

Leucyl-tRNA synthetase, IC50: 46.11 nM

Leucyl-tRNA synthetase, Kd: 42.1 nM

 		98%
SU056 +

YB-1, IC50: 1.73 μM

 		98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Branaplam 生物活性

描述 Branaplam, identified as LMI070 or NVS-SM1, is distinguished by its potent, selective, and orally bioavailable qualities as an SMN2 splicing modulator, displaying an EC50 of 20 nM. It inhibits the hERG channel with an IC50 of 6.3 μM, enhances full-length SMN protein levels, and improves survival in a severe spinal muscular atrophy (SMA) mouse model[1].[2].
体内研究

Branaplam induces dose-dependent increases in SMN2-FL transcript and SMN protein in both brain and spinal cord at doses of 3, 10, and 30 mg/kg orally[1].

With a clearance rate (CL) of 25 mL/min/kg and an area under the curve (AUC) of 3.03 μM·h when administered at 1 mg/kg intravenously (IV) and 3 mg/kg orally (PO)[2].

A single oral dose of 30 mg/kg of Branaplam results in a significant and lasting elevation of SMN protein in the brain for up to 160 hours in C/+ mice[1].

Lastly, oral administration of Branaplam at doses ranging from 0.03 to 3 mg/kg leads to improvements in body weight and extends the lifespan of SMNΔ7 mice[1].
体外研究

Branaplam treatment alters the expression of 175 genes in human fibroblasts[1].

Branaplam 参考文献

[1]Palacino J, et al. SMN2 splice modulators enhance U1-pre-mRNA association and rescue SMA mice. Nat Chem Biol. 2015 Jul;11(7):511-517.

[2]Cheung AK, et al. Discovery of Small Molecule Splicing Modulators of Survival Motor Neuron-2 (SMN2) for the Treatment of Spinal Muscular Atrophy (SMA). J Med Chem. 2018 Dec 27;61(24):11021-11036.

Branaplam 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.54mL

0.51mL

0.25mL

12.71mL

2.54mL

1.27mL

25.41mL

5.08mL

2.54mL

Branaplam 技术信息

CAS号1562338-42-4
分子式C22H27N5O2
分子量 393.482
别名 LMI070;NVS-SM1
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Sealed in dry,Store in freezer, under -20°C
溶解度

DMSO: 30 mg/mL(76.24 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方

Tags: Branaplam | LMI070;NVS-SM1 | DNA/RNA Synthesis | AmBeed-信号通路专用抑制剂 | Branaplam 纯度/质量文件 | Branaplam 亚型比较 | Branaplam 生物活性 | Branaplam 参考文献 | Branaplam 实验方案 | Branaplam 技术信息

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