NS-3-008 hydrochloride
NS-3-008hydrochloride是一种口服活性的G0s2转录抑制剂，IC50为2.25μM。NS-3-008hydrochloride可用于慢性肾脏疾病。
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包装价格促销价数量
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5mg￥875.00700.00- +
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10mg￥1300.001040.00- +
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50mg￥3887.003110.00- +
- 货号: ajcx31212
- CAS: 1172854-54-4
- 别名:
- 分子式: C14H24ClN3
- 分子量: 269.81
- 纯度: ＞98%
- 溶解度: DMSO: 125 mg/mL (463.29 mM); Water: 125 mg/mL (463.29 mM)
- 储存: Store at -20°C
- 库存: 现货
Background
NS-3-008 hydrochloride is an orally active transcriptional inhibitor of G0/G1 switch 2 (G0s2) with an IC50 of 2.25 μM. NS-3-008 hydrochloride can be used for chronic kidney disease[1].
NS-3-008 binds to Hsd17b4; knockdown of Hsd17b4 decreased G0s2 mRNA levels, whereas overexpression of Hsd17b4 induced G0s2 mRNA expression. The inhibitory effects of NS-3-008 are blocked by knockdown of Hsd17b4 or deletion of the Stat5 binding site in the G0s2 promoter. NS-3-008 decreases the nuclear phosphorylation of Stat5[1].
NS-3-008 (5 mg/kg; oral administration; daily; for 4 weeks; wild-type 5/6Nx mice) treatment results in decreased levels of G0s2 and Ccl2 mRNA in the kidneys. The phosphorylation of Stat5 and p65 protein is decreased, and SUN concentrations and renal caspase 3/7 activity decreased in 5/6Nx mice treated with NS-03-08. The F4/80-positive area and F4/80 protein levels are decreased in 5/6Nx mice treated with NS-3-008[1].
[1]. Matsunaga N, et al. Inhibition of G0/G1 Switch 2 Ameliorates Renal Inflammation in Chronic Kidney Disease. EBioMedicine. 2016 Nov;13:262-273.
