ACHN-975 TFA|cas:1410809-37-8|西域试剂

ACHN-975 TFA,95.0%

产品编号：Bellancom-19936A| CAS NO：1410809-37-8| 分子式：C₂₂H₂₄F₃N₃O₆| 分子量：483.44

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-19936A		￥6100.00	杭州北京（现货）
Bellancom-19936A		￥10500.00	杭州北京（现货）

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ACHN-975 TFA

产品介绍

ACHN-975 是细菌酶 LpxC 的选择性抑制剂，表现出亚纳摩尔级 LpxC 抑制活性。ACHN-975 对多种革兰氏阴性菌的 MIC 值低于 1 μg/mL。

生物活性

ACHN-975 TFA is a selective LpxC inhibitor and exhibits a subnanomolar LpxC inhibitory activity. ACHN-975 TFA is against a wide range of gram-negative bacterias with low MIC values (≤1 μg/mL).

体外研究

ACHN-975 is against Enterobacteriaceae spp with an IC₅₀ of 0.02 nM.
ACHN-975 is against Enterobacteriaceae spp, Pa, and Ab with MIC90 values of 1, 0.5, and >64 μg/mL, respectively.
ACHN-975 is potently against the P. aeruginosa isolates tested, inhibiting 100% of the isolates at an MIC of ≤2 μg/ml. It against Pseudomonas aeruginosa with an MIC₅₀ and MIC₉₀ of 0.06 and 0.25 μg/ml, respectively.
ACHN-975 is against six P. aeruginosa isolates, it against P. aeruginosa APAE1064, APAE1232, and APAE1064 isolates with MIC values of 0.12, 0.06 and 0.06 μg/ml, respectively.
LpxC is highly conserved in gram-negative bacteria and catalyzes the first committed step of lipid A biosynthesis. LpxC is the bacterial enzyme Zinc-dependent metalloamidase UDP-3-O-[(R)-3-hydroxymyristoyl]-N-acetylglucosamine deacetylase.

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

体内研究

ACHN-975 TFA (intraperitoneal administration; 5-30 mg/kg; single dose) leads to a steady reduction in bacterial titers in the first 4 h following treatment for all dosing groups. The sampling shows that the level of free drug in this model drops below the ACHN-975 MIC for this isolate (0.25 μg/ml) by 2 h after treatment with the 10 mg/kg dose and by 4 h after treatment with the 30 mg/kg dose.

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

Animal Model:	Neutropenic mouse thigh model with P. aeruginosa ATCC 27853
Dosage:	5-30 mg/kg
Administration:	Intraperitoneal administration; single dose
Result:	Had a bactericidal activity and was against the P. aeruginosa ATCC27853 strain in vivo.

体内研究

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

Animal Model:	Neutropenic mouse thigh model with P. aeruginosa ATCC 27853
Dosage:	5-30 mg/kg
Administration:	Intraperitoneal administration; single dose
Result:	Had a bactericidal activity and was against the P. aeruginosa ATCC27853 strain in vivo.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (206.85 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.0685 mL	10.3425 mL	20.6851 mL
5 mM	0.4137 mL	2.0685 mL	4.1370 mL
10 mM	0.2069 mL	1.0343 mL	2.0685 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

参考文献