314045-39-1|BPTES|CsnPharm

CAS No.: 314045-39-1

BPTES Catalog No. CSN15790

Synonyms: BPTES

BPTES is an allosteric inhibitor of kidney-type glutaminase (GLS) with IC50 of 0.16 μM.

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 Glutaminase kidney-type

IC50:0.16μM
描述Glutaminase (GLS) is responsible for the hydrolysis of glutamine into glutamate and ammonia. BPTES is a potent and selective allosteric inhibitor of kidney-type GLS （KGS） with an IC50 value of 3.3 ± 0.7 μM^[6]. In both WT and mutant IDH1 expressing cells, BPTES at 10 μM resulted in 59% and 68% inhibition, respectively, of glutaminase activity. The administration of BPTES also diminished the levels of glutamate and α-KG. However, the levels of glycolytic intermediates, incudling fructose-1,6-bisphosphate, dihydroxy-acetone-phosphate, and 3-phosphoglycerate, were increased by BPTES treatment^[7]. In P493 cells, BPTES at 2 - 20 μM effectively suppressed cell proliferation under both aerobic and hypoxic conditions. When P493 cells were treated by 2 μM BPTES for 20h, the steady state ATP levels were significantly downregulated compared to control cells under both normoxia and hypoxia. The administration of tumor-bearing SCID mice with BPTES (12.5 mg/kg, once every other day) for 20 days significantly diminished tumor progression compared to DMSO-treated group^[8].

动物研究

剂量

Mice: 10 mg/kg^[3] (p.o.); 12.5 mg/kg^[4] (i.p.), 25 mg/kg^[5] (i.p.) Rat: 2 mg/kg^[5] (i.v.)

给药途径

p.o., i.p., i.v.

动物药代数据

Animal	Rats^[5]
Dose	2.0 mg/kg (i.v.) 10 mg/kg (p.o.)
Administration	i.v. p.o.
F	2% (p.o.)
AUC_0-inf	636 ± 90 (ng/ml)·h (i.v.) 73 ± 2 (ng/ml)·h (p.o.)
T_1/2	5.3 ± 1.4 h (i.v.) 2.0 ± 0.1 h (p.o.)
T_max	0.7 ± 0.3 h (p.o.)
CL	53 ± 7.6 ml/min/kg (i.v.)
C_max	40 ± 8.2 ng/ml (p.o.)
Vss	8.8 ± 1.6 L/kg (i.v.)

参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.9059 mL
- 9.5296 mL
- 19.0592 mL
- 5 mM
- 0.3812 mL
- 1.9059 mL
- 3.8118 mL
- 10 mM
- 0.1906 mL
- 0.9530 mL
- 1.9059 mL

技术信息

CAS号

314045-39-1

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C24H24N6O2S3

运输

蓝冰

分子量

524.68

别名

BPTES

溶解度

DMSO	13.0 mg/mL (24.8 mM) warming
Water	insoluble

动物实验配方

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BPTES Catalog No. CSN15790

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