2. Anti-infection
  3. Bacterial
  4. LeuRS-IN-1

LeuRS-IN-1 是一种有效的口服活性结核分枝杆菌 leucyl-tRNA 合成酶 (M.tb LeuRS)抑制剂。LeuRS-IN-1 对 M.tb LeuRS 的 IC50 和 Kd 值分别为 0.06 μM 和 0.075 μM。LeuRS-IN-1 抑制人细胞质 LeuRS (IC50=38.8 μM) 和 HepG2 蛋白合成 (EC50=19.6 μM)。

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LeuRS-IN-1 Chemical Structure

LeuRS-IN-1 Chemical Structure

CAS No. : 1364914-72-6

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LeuRS-IN-1 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

LeuRS-IN-1 is a potent, orally active M. tuberculosis leucyl-tRNA synthetase (M.tb LeuRS) inhibitor. LeuRS-IN-1 has IC50 and Kd values of 0.06 μM, 0.075 μM for M.tb LeuRS, respectively[1]. LeuRS-IN-1 inhibits human cytoplasmic LeuRS (IC50=38.8 μM), and HepG2 protein synthesis (EC50=19.6 μM)[2].

IC50 & Target[1][2]

M.tb LeuRS

0.06 μM (IC50)

M.tb LeuRS

0.075 μM (Kd)

human cytoplasmic LeuRS

38.8 μM (IC50)

HepG2 protein synthesis

19.6 μM (EC50)

体外研究
(In Vitro)

LeuRS-IN-1 (compound 13) has a MIC value of 0.02 μg/mL for M.tb H37Rv bacteria[1].
LeuRS-IN-1 (compound 3a) (48 h) induces HepG2 cell toxicity with an EC50 value of 65.8 μM[2].

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

LeuRS-IN-1 相关抗体:
体内研究
(In Vivo)

LeuRS-IN-1 (100 mg/kg; orally daily for 14 days) reduces lung CFU value in acute tuberculosis (TB) mice[1].
LeuRS-IN-1 (33 mg/kg; orally 5 days a week for 4 weeks) reduces lung and spleen CFU values in chronic TB mice[1].
Murine pharmacokinetic parameters[1]:

Administration Dose (mg/kg) Cmax (μg/ml)
at 5 min		 CL (ml/h/kg) Vss (ml/kg) MRT (h) AUC0-∞ 
(h · μg/ml)		 α-t1/2 
(h) (% AUC)		 β-t1/2 
(h) (% AUC)
i.v. 30 13.6 582 3,142 5.4 51.6 0.10 (2) 3.83 (98)
Administration Dose (mg/kg) Cmax (μg/ml) Tmax (h) AUC0-24 
(h · μg/ml)		 Terminal 
t1/2 (h)		 Bioavailability
(%) (h · μg/ml)		 Mouse PPB
(%)
p.o. 30 6.4 0.25 47.5 3.1 9.2 23

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

Animal Model: Murine GKO (C57BL/6-Ifngtm1ts) model of acute TB[1]
Dosage: 100 mg/kg
Administration: Orally daily for 14 days after 10 days of infection (start) with M. tuberculosis Erdman.
Result: Reduced lung CFU value in mice.
Animal Model: Murine BALB/c model of chronic TB infection[1]
Dosage: 33 mg/kg
Administration: Orally 5 days a week for 4 weeks after infection with M. tuberculosis Erdman with a low-dose aerosol 21 days prior (start).
Result: Reduced lung and spleen CFU values in mice.
分子量

241.48

Formula

C10H13BClNO3
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

LeuRS-IN-1 相关分类

  • 摩尔计算器

  • 稀释计算器

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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.

Keywords:

LeuRS-IN-11364914-72-6BacterialtuberculosisM. tuberculosisHepG2protein synthesishuman cytoplasmiccellsmiceInhibitorinhibitorinhibit

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