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Merck
CN

SML3836

Sigma-Aldrich

Delamanid

≥98% (HPLC)

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别名:
(2R)-2,3-Dihydro-2-methyl-6-nitro-2-{4-[4-[4-(trifluoromethoxy)phenoxy]-1-piperidinyl]phenoxy]methyl]-imidazo[2,1-b]oxazole, (R)-2-Methyl-6-nitro-2-{4-[4-(4-trifluoromethoxyphenoxy)piperidin-1-yl]phenoxymethyl}-2,3-dihydroimidazo[2,1-b]oxazole, Deltyba, OPC 67683, OPC-67683, OPC67683
经验公式(希尔记法):
C25H25F3N4O6
分子量:
534.48
MDL编号:
UNSPSC代码:
12352200
NACRES:
NA.21

质量水平

检测方案

≥98% (HPLC)

形式

powder

旋光性

[α]/D -8 to -12°, c = 0.5 in chloroform-d

颜色

white to beige

溶解性

DMSO: 2 mg/mL, clear

储存温度

-10 to -25°C

生化/生理作用

Delamanid (OPC-67683) is an orally active mycolic acid biosynthesis inhibitor that is effective against both drug-susceptible and drug-resistant strains of M. tuberculosis H37Rv in vitro (MIC = 6 ng/mL) and exhibits significant in vivo efficacy with ~15-fold higher potency than rifampicin (RFP) in mice infected with M. tuberculosis Kurono (fold of lung CFU reduction post 28 days = 41.5 with 5 mg RFP/kg or 0.313 mg delamanid/kg daily orally dosage, 11,000-fold reduction with 0.625 mg delamanid/kg daily orally dosage).

象形图

Health hazard

警示用语:

Warning

危险声明

危险分类

Repr. 2

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable

法规信息

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Delamanid Kills Dormant Mycobacteria In Vitro and in a Guinea Pig Model of Tuberculosis
Antimicrobial Agents and Chemotherapy, 61(6), e02402-e02416 (2017)
Hirofumi Sasaki et al.
Journal of medicinal chemistry, 49(26), 7854-7860 (2006-12-22)
In an effort to develop potent new antituberculosis agents that would be effective against both drug-susceptible and drug-resistant strains of Mycobacterium tuberculosis, we prepared a novel series of optically active 6-nitro-2,3-dihydroimidazo[2,1-b]oxazoles substituted at the 2-position with various phenoxymethyl groups and
Makoto Matsumoto et al.
PLoS medicine, 3(11), e466-e466 (2006-11-30)
Tuberculosis (TB) is still a leading cause of death worldwide. Almost a third of the world's population is infected with TB bacilli, and each year approximately 8 million people develop active TB and 2 million die as a result. Today's

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