| 货号 | 规格 | 价格 | 上海 | 北京 | 珠海 | 重庆 | 武汉 | 购买数量 |
|---|---|---|---|---|---|---|---|---|
S83593-2mg买3赠1 |
99.90% | ￥522.00 ￥460.00 |
4 | - | - | - | - |
|
S83593-5mg买3赠1 |
99.90% | ￥640.00 ￥570.00 |
4 | - | - | - | - |
|
S83593-10mg买3赠1 |
99.90% | ￥880.00 ￥790.00 |
3 | - | - | - | - |
|
S83593-25mg买3赠1 |
99.90% | ￥1900.00 ￥1710.00 |
4 | - | - | - | - |
|
S83593-50mg买3赠1 |
≥98% | ￥3200.00 ￥2880.00 |
货期：2-3天 | - | - | - | - |
|
S83593-100mg促销 |
≥98% | ￥5500.00 ￥4950.00 |
货期：2-3天 | - | - | - | - |
|
| 产品描述： | Branaplam (LMI070; NVS-SM1) is a highly potent, selective and orally active survival motor neuron-2 (SMN2) splicing modulator with an EC50 of 20 nM for SMN. Branaplam inhibits human-ether-a-go-go-related gene (hERG) with an IC50 of 6.3 μM. Branaplam elevates full-length SMN protein and extends survival in a severe spinal muscular atrophy (SMA) mouse model | ||||||||||||||||||||
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| 靶点： | IC50: 20 nM (SMN) EC50: 6.3 μM (hERG);thers; PotassiumChannel; DNA/RNASynthesis | ||||||||||||||||||||
| 体外研究： | Branaplam (LMI070; NVS-SM1) treatment induces changes in the levels of 175 genes in human fibroblasts | ||||||||||||||||||||
| 体内研究： | Branaplam (LMI070; NVS-SM1; 3, 10, 30 mg/kg; oral) produces dose-dependent elevations of SMN2-FL transcript and SMN protein in brain and spinal cord. Branaplam (1 mg/kg of IV; 3 mg/kg of PO) has a CL of 25 mL/min/kg and an AUC of 3.03 μM•h.A single Branaplam (oral; 30 mg/kg) results in significant and durable SMN protein elevation in brain for up to 160 hours in C/+ mice. Branaplam (oral; 0.03, 0.1, 0.3, 1, 3 mg/kg) improves body weight and extendes lifespan in n SMNΔ7 mice. Animal Model: C/+ SMA mouse model Dosage: 3, 10, 30 mg/kg Administration: Oral Result: Produced dose-dependent elevations of SMN2-FL transcript and SMN protein in brain and spinal cord. Animal Model: Male Sprague-Dawley rat Dosage: 1 mg/kg (IV);3 mg/kg (PO) (Pharmacokinetic Analysis) Administration: IV or PO Result: Had a CL of 25 mL/min/kg and an AUC of 3.03 μM•h. | ||||||||||||||||||||
| 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. | ||||||||||||||||||||
| 溶解性： | Soluble in DMSO | ||||||||||||||||||||
| 保存条件： | -20℃ | ||||||||||||||||||||
| 配置溶液浓度参考： |
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| 注意： | 部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
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营业执照(三证合一)
北京