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

ACHN-975 是細(xì)菌酶 LpxC 的選擇性抑制劑,表現(xiàn)出亞納摩爾級(jí) LpxC 抑制活性。ACHN-975 對(duì)多種革蘭氏陰性菌的 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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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ¥5658
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1 mg ¥2240
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5 mg ¥5320
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Customer Review

Other Forms of ACHN-975 TFA:

MCE 顧客使用本產(chǎn)品發(fā)表的 1 篇科研文獻(xiàn)

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

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]

體外研究
(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.

體內(nèi)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 號(hào)
性狀

固體

顏色

Light yellow to yellow

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.

儲(chǔ)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)

溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn): 

DMSO 中的溶解度 : 100 mg/mL (206.85 mM; 超聲助溶; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響,請(qǐng)使用新開封的 DMSO)

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)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
查看完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液;一旦配成溶液,請(qǐng)分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(nèi)使用,-20°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(nèi)使用。

  • 摩爾計(jì)算器

  • 稀釋計(jì)算器

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

質(zhì)量
=
濃度
×
體積
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動(dòng)物溶解方案計(jì)算器
請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息:

給藥劑量

mg/kg

動(dòng)物的平均體重

g

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

由于實(shí)驗(yàn)過程有損耗,建議您多配一只動(dòng)物的量
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
純度 & 產(chǎn)品資料

純度: 99.57%

參考文獻(xiàn)

ACHN-975 TFA 相關(guān)分類

完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液;一旦配成溶液,請(qǐng)分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(nèi)使用,-20°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)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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產(chǎn)品名稱:
ACHN-975 TFA
目錄號(hào):
HY-19936A
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