1. Metabolic Enzyme/Protease
  2. Endogenous Metabolite
  3. MK-6186

MK-6186是一种新型非核苷类反转录酶抑制剂,具有亚纳摩尔级别的活性,针对野生型病毒及两种最常见的NNRTI耐药RT突变体(K103N和Y181C)。MK-6186对K103N和Y181C突变病毒表现出卓越的抗病毒活性。MK-6186在针对12种常见的NNRTI相关突变病毒时,仅有2种相对罕见的突变体(Y188L和V106I/Y188L)表现出高耐药性,FC值超过100,其余病毒的FC值均低于10。此外,MK-6186在面对携带NNRTI耐药突变的96个临床病毒孤立株时,大部分(70%)病毒对依非韦伦(EFV)显示出超过10倍的耐药性,而仅有29%的突变病毒对MK-6186的耐药性超过10倍。

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MK-6186 Chemical Structure

MK-6186 Chemical Structure

CAS No. : 1034474-19-5

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1 mg ¥2941
1 - 2 周
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  • 生物活性

  • 纯度 & 产品资料

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生物活性

MK-6186 is a novel non-nucleoside reverse transcriptase inhibitor with sub-nanomolar activity against wild-type viruses and the two most common NNRTI-resistant RT mutants (K103N and Y181C). MK-6186 exhibits excellent antiviral activity against K103N and Y181C mutant viruses. When MK-6186 targets 12 common NNRTI-associated mutant viruses, only two relatively rare mutants (Y188L and V106I/Y188L) show high resistance, with FC values exceeding 100, while the FC values of the remaining viruses are all below 10. In addition, when MK-6186 faces 96 clinical virus isolates carrying NNRTI-resistant mutations, most (70%) viruses show more than 10-fold resistance to efavirenz (EFV), while only 29% of mutant viruses show more than 10-fold resistance to MK-6186[1].

分子量

435.27

Formula

C21H12Cl2N6O

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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  • 稀释计算器

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  • 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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MK-6186
目录号:
HY-167690
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