1. Anti-infection
  2. Bacterial
  3. ACHN-975 TFA

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。

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ACHN-975 TFA Chemical Structure

ACHN-975 TFA Chemical Structure

CAS No. : 1410809-37-8

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥5658
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1 mg ¥2240
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5 mg ¥5320
In-stock
10 mg ¥8400
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Customer Review

Other Forms of ACHN-975 TFA:

MCE 顾客使用本产品发表的 1 篇科研文献

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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)[1].

IC50 & Target

IC50: LpxC[1]

体外研究
(In Vitro)

ACHN-975 is against Enterobacteriaceae spp with an IC50 of 0.02 nM[1].
ACHN-975 is against Enterobacteriaceae spp, Pa, and Ab with MIC90 values of 1, 0.5, and >64 μg/mL, respectively[1].
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[2].
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[2].
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[1].

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

体内研究
(In Vivo)

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[2].

MCE 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[2]
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.
Clinical Trial
分子量

483.44

Formula

C22H24F3N3O6

CAS 号
性状

固体

颜色

Light yellow to yellow

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)

溶解性数据
In Vitro: 

DMSO 中的溶解度 : 100 mg/mL (206.85 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

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
查看完整储备液配制表

* 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。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: 99.57%

参考文献

ACHN-975 TFA 相关分类

完整储备液配制表

* 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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0685 mL 10.3425 mL 20.6851 mL 51.7127 mL
5 mM 0.4137 mL 2.0685 mL 4.1370 mL 10.3425 mL
10 mM 0.2069 mL 1.0343 mL 2.0685 mL 5.1713 mL
15 mM 0.1379 mL 0.6895 mL 1.3790 mL 3.4475 mL
20 mM 0.1034 mL 0.5171 mL 1.0343 mL 2.5856 mL
25 mM 0.0827 mL 0.4137 mL 0.8274 mL 2.0685 mL
30 mM 0.0690 mL 0.3448 mL 0.6895 mL 1.7238 mL
40 mM 0.0517 mL 0.2586 mL 0.5171 mL 1.2928 mL
50 mM 0.0414 mL 0.2069 mL 0.4137 mL 1.0343 mL
60 mM 0.0345 mL 0.1724 mL 0.3448 mL 0.8619 mL
80 mM 0.0259 mL 0.1293 mL 0.2586 mL 0.6464 mL
100 mM 0.0207 mL 0.1034 mL 0.2069 mL 0.5171 mL
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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ACHN-975 TFA
目录号:
HY-19936A
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