1. Anti-infection
  2. Bacterial Antibiotic
  3. Macozinone

Macozinone  (Synonyms: PBTZ169)

目录号: HY-12903 纯度: 98.46%
COA 产品使用指南 技术支持

Macozinone (PBTZ169) 是一种杀菌型苯并噻嗪酮,也是有效的 DprE1 抑制剂。Macozinone 可通过与活性位点 Cys387 残基形成共价键来抑制必需的黄素蛋白 DprE1。Macozinone 有抗结核作用。

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Macozinone Chemical Structure

Macozinone Chemical Structure

CAS No. : 1377239-83-2

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Free Sample (0.1 - 0.2 mg)   Apply now  
10 mM * 1 mL in DMSO ¥990
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1 mg ¥360
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5 mg ¥900
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10 mg ¥1400
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25 mg ¥2800
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50 mg ¥4500
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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Macozinone (PBTZ169) is a bactericidal benzothiazinone and a potent DprE1 (decaprenylphosphoryl-β-d-ribose 2′-oxidase) inhibitor. Macozinone inhibits the essential flavoprotein DprE1 by forming a covalent bond with the active-site Cys387 residue. Macozinone has antituberculosis effect[1][2].

IC50 & Target

DprE1[1]

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HEK293 IC50
101.7 μM
Compound: PBTZ169
Inhibition of human ERG transfected in HEK293 cells by whole-cell patch clamp method
Inhibition of human ERG transfected in HEK293 cells by whole-cell patch clamp method
[PMID: 31408806]
HepG2 IC50
18.98 μg/mL
Compound: 2; PBTZ169
Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 48 hrs by MTT assay
Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 48 hrs by MTT assay
[PMID: 30336450]
Vero CC50
> 125 μM
Compound: PBTZ169
Cytotoxicity against African green monkey Vero cells after 72 hrs by MTT assay
Cytotoxicity against African green monkey Vero cells after 72 hrs by MTT assay
[PMID: 25754492]
Vero IC50
> 64 μg/mL
Compound: 2; PBTZ169
Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability after 48 hrs by MTT assay
Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability after 48 hrs by MTT assay
[PMID: 30336450]
Vero CC50
> 64 μg/mL
Compound: PBTZ169
Cytotoxicity against African green monkey Vero cells incubated for 72 hrs by MTT assay
Cytotoxicity against African green monkey Vero cells incubated for 72 hrs by MTT assay
[PMID: 33823392]
Vero CC50
1402.82 μM
Compound: PBTZ169
Cytotoxicity against African green monkey Vero cells assessed as cell viability after 72 hrs by MTT assay
Cytotoxicity against African green monkey Vero cells assessed as cell viability after 72 hrs by MTT assay
[PMID: 28626525]
Vero CC50
31 μg/mL
Compound: PBTZ169
Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability after 72 hrs by MTT assay
Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability after 72 hrs by MTT assay
[PMID: 30692025]
体外研究
(In Vitro)

Macozinone (PBTZ169) 在体外、离体和体内均对结核分枝杆菌具有高效作用[2]

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

Clinical Trial
分子量

456.48

Formula

C20H23F3N4O3S

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
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性数据
细胞实验: 

DMSO 中的溶解度 : 6.4 mg/mL (14.02 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 2.1907 mL 10.9534 mL 21.9068 mL
5 mM 0.4381 mL 2.1907 mL 4.3814 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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

  • 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: 98.46%

参考文献

Macozinone 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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1907 mL 10.9534 mL 21.9068 mL 54.7669 mL
5 mM 0.4381 mL 2.1907 mL 4.3814 mL 10.9534 mL
10 mM 0.2191 mL 1.0953 mL 2.1907 mL 5.4767 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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产品名称:
Macozinone
目录号:
HY-12903
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