2. Cell Cycle/DNA Damage Anti-infection
  3. DNA/RNA Synthesis RSV
  4. GS-646089

GS-646089 是一种广谱抗病毒核苷类似物，对呼吸道合胞病毒 (RSV)、人偏肺病毒 (hMPV)、鼻病毒 (enterovirus) 及肠道病毒均表现出显著的抑制活性。GS-646089 靶向 RNA 聚合酶 (RdRp) 的 IC50 为 43-46 nM。GS-646089 通过在细胞内转化为三磷酸代谢产物，与 ATP 竞争性掺入新生 RNA 链并作为即时链终止剂，从而阻断病毒复制。GS-646089 是双前药 GS-7682 (HY-161877) 的母体化合物，已用于急性呼吸道病毒感染及相关病原体感染研究。

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GS-646089

GS-646089 Chemical Structure

CAS No. : 1770840-57-7

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GS-646089 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

GS-646089 is a broad-spectrum antiviral nucleoside analog that exhibits significant inhibitory activity against respiratory syncytial virus (RSV), human metapneumovirus (hMPV), rhinovirus (enterovirus) and enteroviruses. The IC50 of GS-646089 targeting RNA-dependent RNA polymerase (RdRp) ranges from 43 to 46 nM. GS-646089 blocks viral replication by being converted into a triphosphate metabolite intracellularly, which competes with ATP for incorporation into nascent RNA strands and acts as an immediate chain terminator. GS-646089 is the parent compound of the double prodrug GS-7682 (HY-161877), and is used in studies of acute respiratory viral infections and infections caused by related pathogens[1][2][3].
IC50 & Target

RNASE L

 

体外研究
(In Vitro)

GS-646089 (compound 2) 可在原代 NHBE 细胞和 HEp-2 细胞中抑制 RSV 复制，其 EC50 值分别为 6.23 μM 和 6.83 μM；且在浓度高达 50 μM 时，对 HEp-2 细胞和 MT4 细胞无细胞毒性[1]。
GS-646089 的活性三磷酸代谢产物 (2-NTP) 可强效抑制 RSV RNP 复合物，IC50 为 0.050 μM，且对人线粒体聚合酶和 DNA 聚合酶具有高选择性[1]。
GS-646089 可强效抑制无细胞 RSV-A2 RNP 复合物及 RdRp 酶活性，IC50 分别为 46 nM 和 43 nM[2]。
GS-646089 可抑制 NHBE 细胞中 RSV 的复制，EC50 约为 2-7 μM，且在最高 50 μM 的浓度下无细胞毒性[3]。
GS-646089 在 HEp-2 细胞中抑制 RSV 复制，其 EC50 约为 2-7 μM；且在最高 50 μM 的浓度下，对 HEp-2 或 MT4 细胞均无细胞毒性[3]。
GS-646089 (10 μM; 2 h) 产生低水平的细胞内活性 2-NTP 代谢物，表明该核苷的首次磷酸化作用受限[3]。

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

GS-646089 相关抗体:
药代动力学
(Parmacokinetics)
Species Dose Route T1/2 Spinal Cord Concentration Cmax AUC0-24
Monkey[1] 5 mg/kg i.v. 8.71 ± 3.01 h / 0.961 ± 0.379 μM 6.03 ± 3.75 μM·h
Monkey[1] 4.0 mg/kg i.t. 38.8 ± 4.0 h / 0.14 ± 0.05 μM 2.55 ± 0.61 μM·h
Monkey[1] 5.9 mg/kg i.t. 14.7 ± 2.6 h / 0.22 ± 0.09 μM 3.39 ± 1.11 μM·h
Cynomolgus Monkey[2] 5 mg/kg i.v. 8.71 ± 3.01 h / / /
Cynomolgus Monkey[3] 5 mg/kg i.v. 8.71 ± 3.01 h 4.28 ± 1.32 / /
体内研究
(In Vivo)

GS-646089 (compound 2) (1.6-7.6 mg/kg; i.t.; 每日 1 次; 6 d) 是吸入用 GS-7682 的活性代谢产物，可使 RSV 感染的非洲绿猴的 RSV BAL 病毒载量平均降低 3.6 log10，显著抑制下呼吸道病毒复制[1]。
GS-646089 (1.6-7.6 mg/kg; 气管内雾化吸入; 每日 1 次；6 d) 在感染后第 5 天可使非洲绿猴支气管肺泡灌洗液 (BAL) 中的 RSV A2 病毒载量平均降低 3.6 log10，且至第 11 天时病毒载量仍持续低于溶媒对照组[3]。

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

Animal Model: AGM (infected with RSV A2 on day 0)[1]
Dosage: 1.6 mg/kg; 7.6 mg/kg
Administration: i.t.; once daily; 6 days
Result: Detected high levels of active GS-646089 metabolite (2-NTP) in lung tissue.
Achieved an average 3.6 log10 reduction in BAL viral load compared to vehicle control on day 5.
Resulted in significant reductions in RSV RNA copies in BAL fluid samples collected between 3 and 11 days post-infection.
Showed moderate viral rebound 2 to 4 days after final dose, but viral loads remained lower in treated AGMs through day 11.
Failed to produce statistically significant reductions in nasal swab viral loads.
Animal Model: Chlorocebus aethiops[3]
Dosage: 1.6 mg/kg; 7.6 mg/kg
Administration: intratracheal nebulized aerosol; once daily; 6 days
Result: Achieved an average 3.6 log10 reduction in BAL viral load compared to vehicle controls on day 5 post-infection.
Showed significant reductions in RSV RNA copies in BAL samples collected between 3 and 11 days post-infection.
Exhibited moderate rebound in BAL viral loads 2-4 days after final dose, but viral loads remained lower than vehicle controls until day 11.
Did not achieve statistically significant viral load reductions in nasal swabs.
分子量

291.26

Formula

C12H13N5O4
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

GS-646089 相关分类

  • 摩尔计算器

  • 稀释计算器

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  • Do most proteins show cross-species activity?

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Keywords:

GS-6460891770840-57-7GS646089GS 646089DNA/RNA SynthesisRSVRespiratory syncytial virusacute respiratory viral infectionsRSV infectionRSV RdRpenterovirushMPV infectionhMPVrhinovirus infectionrhinovirusenterovirus infectionInhibitorinhibitorinhibit

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