Macozinone | PBTZ169 | DprE1 Inhibitor | AmBeed-信号通路专用抑制剂

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Macozinone {[allProObj[0].p_purity_real_show]}

货号：A713021 同义名： PBTZ169

PBTZ169 is a drug candicate that inhibits decaprenylphosphoryl-β-d-ribose 2′-oxidase (DprE1), more efficiently than BTZ043.

Macozinone 化学结构
CAS号：1377239-83-2

Macozinone 3D分子结构
CAS号：1377239-83-2

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Macozinone 纯度/质量文件产品仅供科研

货号：A713021 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • Science, 2025, 387(6729): eadp5637. Ambeed. [ A875019 ]; • Nat. Electron., 2025, 8, 66-74. Ambeed. [ A100095 ]; • Adv. Mater., 2025, 2416621. Ambeed. [ A255324 , A420052 ]; • Adv. Mater., 2025, 2410493. Ambeed. [ A838608 ]; • Adv. Mater., 2025, 2420319. Ambeed. [ A106129 ]; 更多 >

Macozinone 生物活性

描述

The essential flavo-enzyme DprE1, decaprenylphosphoryl-β-D-ribose 2-epimerase, produces the sole source of the D-arabinose required for biosynthesis of the key cell wall components arabinogalactan and lipoarabinomannan. PBTZ169, belonging to a new series of piperazine-containing benzothiazinones (PBTZ), is a potent DprE1 inhibitor. PBTZ169 was found to be three- to seven-fold more active than BTZ043 against M. tuberculosis, Mycobacterium bovis BCG, Mycobacterium marinum, Mycobacterium smegmatis, Corynebacterium diphtheriae and Corynebacterium glutamicum. PBTZ169 was found to be 10-times less cytotoxic (TD₅₀ of 58 μg/ml) compared to BTZ043 (TD₅₀ of 5 μg/ml). On incubation with human or mouse microsomes, PBTZ169 showed medium clearance values. Inhibition of M. tuberculosis DprE1 by PBTZ169 was monitored by determining the residual enzyme activity following incubation with a range of concentrations of this compound. Full inhibition of DprE1 was obtained following 5 min incubation with 5 μM PBTZ169. Treatment of infected zebrafish embryos with increasing concentrations of PBTZ169 led to a decrease in the bacterial burden after 5 days. Almost no bacteria were present when infected zebrafish embryos were treated with 25 or 50 nM PBTZ169^[3].

作用机制

The crystal structure of the DprE1-PBTZ169 complex reveals formation of a semimercaptal adduct with Cys387 in the active site^[3].

Macozinone 参考文献

[1]Makarov V, Neres J, et al. The 8-Pyrrole-Benzothiazinones Are Noncovalent Inhibitors of DprE1 from Mycobacterium tuberculosis. Antimicrob Agents Chemother. 2015 Aug;59(8):4446-52.

[2]Makarov V, Lechartier B, et al. Towards a new combination therapy for tuberculosis with next generation benzothiazinones. EMBO Mol Med. 2014 Mar;6(3):372-83.

[3]Makarov V, Lechartier B, Zhang M, et al. Towards a new combination therapy for tuberculosis with next generation benzothiazinones. EMBO Mol Med. 2014;6(3):372‐383

Macozinone 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.19mL

0.44mL

0.22mL

10.95mL

2.19mL

1.10mL

21.91mL

4.38mL

2.19mL

Macozinone 技术信息

CAS号	1377239-83-2
分子式	C₂₀H₂₃F₃N₄O₃S
分子量	456.48
SMILES Code	O=C1N=C(N2CCN(CC3CCCCC3)CC2)SC4=C([N+]([O-])=O)C=C(C(F)(F)F)C=C14
MDL No.	MFCD28902203

别名	PBTZ169
运输	蓝冰
InChI Key	BJDZBXGJNBMCAV-UHFFFAOYSA-N
Pubchem ID	57331386

存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Sealed in dry,2-8°C

溶解方案

细胞实验：

DMSO: 5 mg/mL(10.95 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

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计算溶液所需的质量，体积或浓度。 Ambeed 摩尔浓度计算器基于以下方程式：

浓度 (mol/L) × 体积 (L) × 分子量 (g/mol)=质量 (g)

浓度

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