貨號	規(guī)格	價格	上海	北京	武漢	南京
S83593-2mg	99.9%	￥523.60 S83593-2mg ￥523.60 現貨	4 4	-	-	-
S83593-5mg	99.9%	￥640.00 S83593-5mg ￥640.00 現貨	4 4	-	-	-
S83593-10mg	99.9%	￥880.00 S83593-10mg ￥880.00 現貨	4 4	-	-	-
S83593-25mg	99.9%	￥1900.00 S83593-25mg ￥1900.00 現貨	5 5	-	-	-
S83593-50mg	≥98%	￥3200.00 S83593-50mg ￥3200.00 2-3天	0 貨期：2-3天	-	-	-
S83593-100mg	≥98%	￥5500.00 S83593-100mg ￥5500.00 2-3天	0 貨期：2-3天	-	-	-

產品介紹

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

產品描述：

靶點：

IC50: 20 nM (SMN) EC50: 6.3 μM (hERG);thers;?PotassiumChannel;?DNA/RNASynthesis

體外研究：

Branaplam (LMI070; NVS-SM1) treatment induces changes in the levels of 175 genes in human fibroblasts

體內研究：

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.

參考文獻：

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

保存條件：

-20℃

配置溶液濃度參考：

	1mg	5mg	10mg
1 mM	2.541 ml	12.707 ml	25.414 ml
5 mM	0.508 ml	2.541 ml	5.083 ml
10 mM	0.254 ml	1.271 ml	2.541 ml
50 mM	0.051 ml	0.254 ml	0.508 ml

注意：

部分產品我司僅能提供部分信息，我司不保證所提供信息的權威性，僅供客戶參考交流研究之用。

參考文獻

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