2. Anti-infection Metabolic Enzyme/Protease
  3. HIV HIV Protease
  4. GRL-142

GRL-142 是一种能够穿透血脑屏障的强效 HIV-1 蛋白酶抑制剂。GRL-142 对野生型及多药耐药毒株均表现出极高的抑制活性 (IC50=0.0094 nM)。GRL-142 通过独特的骨架结合机制与 P2/P2'片段协同作用，利用氟介导的稳定相互作用维持生物活性构象，并能适应 p51 HIV-1 蛋白酶突变体，通过直接作用于瓣尖残基维持瓣闭合状态。GRL-142 破坏野生型蛋白酶的瓣-水氢键网络，从而有效阻断病毒复制。GRL-142 可用于研究 HIV-1 感染及其引发的神经认知障碍 (HAND)。

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GRL-142

GRL-142 Chemical Structure

1.  客户无需承担相应的运输费用。

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GRL-142 相关抗体

Top Publications Citing Use of Products

查看 HIV 亚型特异性产品:

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HIV HIV-1 HIV-2

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

GRL-142 is a potent HIV-1 protease inhibitor capable of crossing the blood-brain barrier. GRL-142 exhibits extremely high inhibitory activity against both wild-type and multidrug-resistant strains (IC50=0.0094 nM). GRL-142 acts synergistically with the P2/P2' segments via a unique scaffold binding mechanism, utilizes fluorine-mediated stable interactions to maintain its bioactive conformation, adapts to p51 HIV-1 protease mutants, and maintains the flap-closed state by directly acting on the flap tip residues. GRL-142 disrupts the flap-water hydrogen bond network of wild-type protease, thereby effectively blocking viral replication. GRL-142 can be used to study HIV-1 infection and the associated neurocognitive disorder (HAND)[1].
IC50 & Target

HIV-1

 

体外研究
(In Vitro)

GRL-142 对野生型 HIV-1 表现出超强抑制活性 (Ki =14 pM)，且对大多数耐药性 HIV-1 毒株仍保持高活性，但对高耐药性 p51 毒株的活性显著下降 (降幅最高达 436 倍)[1]。

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

GRL-142 相关抗体:
分子量

718.83

Formula

C34H40F2N4O7S2
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

GRL-142 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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.

Keywords:

GRL-142GRL142GRL 142HIVHIV ProteaseHuman immunodeficiency virusflap-tip residueflap-water hydrogen bonding networksp51 HIV-1 protease variantdrug-resistant HIV-1 strainsblood-brain barrierHIV-associated neurocognitive disordersS2/S2' subsitesmultidrug-resistant HIV-1 proteaseHIV-1 infectionwild-type HIV-1 proteaseInhibitorinhibitorinhibit

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