1. Anti-infection
  2. Bacterial
  3. sALT629

sALT629 是一种有口服活性的抗结核剂,具有强效巨噬细胞内活性 (EC50 值为 1.5 μM)。sALT629 在四种碳源中均表现出广谱抗结核分枝杆菌 (Mycobacterium tuberculosis,Mtb) 活性,对耐药性结核分枝杆菌具有同等效力,且对缓慢复制和非复制的结核分枝杆菌均有活性。sALT629 与恶唑烷酮类药物,如 Linezolid (HY-10394) 和 Sutezolid (HY-10392) 联合使用时,展现出协同活性。sALT629 可用于结核病的研究。

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sALT629

sALT629 Chemical Structure

CAS No. : 484026-63-3

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

sALT629 is an orally active antitubercular agent with potent intramacrophage activity (EC50 = 1.5 μM). sALT629 shows broad-spectrum anti-Mycobacterium tuberculosis (Mtb) activities across four carbon sources, equipotent efficacy against drug-resistant Mtb, and activity against both slow-replicating and nonreplicating Mtb. sALT629 exhibits synergistic activity when combined with oxazolidinone drugs, such as Linezolid (HY-10394) and Sutezolid (HY-10392). sALT629 can be used for the research of tuberculosis[1].

体外研究
(In Vitro)

sALT629 (0.96-12.5 μM) 对四种碳源 (乙酸盐、丁酸盐、胆固醇、葡萄糖) 培养的 Mtb 均有抑制活性,对巨噬细胞内 Mtb 的 EC50为 1.5 μM,对耐多药 (MDR)、广泛耐药 (XDR) 及单药耐药 Mtb 菌株的 MIC 为 0.8-1.7 μM,对缓慢复制和非复制状态 Mtb 也具有活性[1]
sALT629 (1.7-13.6 μM;7 天) 在 7H12 胆固醇培养基中表现出剂量依赖性的杀菌活性[1]
sALT629 (20 μM;7 天) 在 Hu-Coates 100 天休眠模型中使 CFU 减少约 1.5 个对数级,在 Loebel 营养剥夺模型中使 CFU 减少约 0.5 个对数级[1]
sALT629 (>40 μM) 对 HEK293T 和 HepG2 细胞无明显细胞毒性,选择指数 SI 大于 23[1]
sALT629 与恶唑烷酮类药物 (Linezolid (HY-10394), Sutezolid (HY-10392)) 联合使用时呈协同作用 (FIC=0.5),与 TBD11、TBA-7371 (HY-19750) 和 Q203 (HY-101040) 等药物联合呈相加作用 (FIC=0.63-1.0),与 Isoniazid (HY-B0329) 等药物无明显相互作用 (FIC>1.0)[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

sALT629 (30-100 mg/kg 每日两次、或 200 mg/kg 每日一次,口服,连续 4 天) 对 CD-1 小鼠无明显毒性,无体重下降及临床生化、血液学指标异常[1]
sALT629 (100 mg/kg 每日两次、或 200 mg/kg 每日一次,口服,连续 4 天) 可使血浆浓度维持在 EC50 以上超过 24 小时,肺组织暴露量高于 EC50[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

275.31

Formula

C13H17N5O2

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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  • 稀释计算器

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× = ×
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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sALT629
目录号:
HY-179649
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