LDC4297 是CDK7的选择性抑制剂，IC50值为 0.13 nM。LDC4297 抑制人巨细胞病毒 (HCMV) 复制，EC50值为 24.5 nM。LDC4297 具有广谱的抗病毒活性，对疱疹病毒，腺病毒，痘病毒，逆转录病毒和正粘病毒的EC50值为 0.02-1.21 μM。LDC4297 可用于感染的研究。
| 生物活性 | LDC4297 is a selective inhibitor ofCDK7with anIC50value of 0.13 nM. LDC4297 inhibits human cytomegalovirus (HCMV) replication with anEC50value of 24.5 nM. LDC4297 shows broad antiviral activities toHerpesviridae,Adenoviridae,Poxviridae,RetroviridaeandOrthomyxoviridaewithEC50value of 0.02-1.21 μM. LDC4297 can be used for the research ofinfection[1]. |
| IC50& Target[1] | CDK7 0.13 nM (IC50) | HSV-1 | HSV-2 | HSV-1 0.02 μM (EC50) | HSV-2 0.27 μM (EC50) |
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体外研究
(In Vitro) | LDC4297 (0-10 μM; 6 d) dose-dependently inhibits HCMV replication with an EC50value of 24.5 nM[1].LDC4297 (0-10 μM; 4 d) shows anti-proliferative activity to primary cultures of fibroblasts derived from human (HFF) with a GI50value of 4.5 μM[1].LDC4297 (20 μM; 12-96 h) shows anti-HCMV activity through a multifaceted mode of action that involves an interference with virus-induced Rb phosphorylation[1].LDC4297 (0-10 μM; 7 d) shows broad antiviral activities to HCMV, GPCMV, MCMV, HVV-6A, HSV-1, HSV-2, VZV, EBV, HAdV-2, Vaccinia virus, HIV-1 (nl4-3), HIV-1 (4LIG7) and Influenza A virus with EC50values of 0.02, 0.05, 0.07, 0.04, 0.02, 0.27, 0.06, 1.21, 0.25, 0.77, 1.04, 1.13 and 0.99 μM, respectively[1].
Western Blot Analysis[1] | Cell Line: | Primary cultures of fibroblasts derived from human (HFF) with virus infection | | Concentration: | 20 μM | | Incubation Time: | 12, 24, 48 and 96 hours | | Result: | Showed inhibitory effect towards viral protein synthesis at the stage of immediate early (IE) gene expression and the drug-mediated reduction of IE1p72 levels partially recovered over time. Exerted an inhibitory effect on human cytomegalovirus (HCMV) induced an up-regulation of protein expression or protein phosphorylation, and reduced Rb expression in the uninfected control cells at 24 h. |
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体内研究
(In Vivo) | LDC4297 (100 mg/kg; p.o. once) shows promising pharmacokinetic analyses[1].
| Animal Model: | CD1 mice[1] | | Dosage: | 100 mg/kg | | Administration: | Oral gavage; 100 mg/kg once | | Result: | Showed a half-life of 1.6 h, and the time to a mean peak plasma concentration of 1,297.6 ng/mL is reached 0.5 h after administration with a continued presence in plasma for at least 8 h and a bioavailability of 97.7%. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : ≥ 60 mg/mL(138.72 mM) *"≥" means soluble, but saturation unknown. 配制储备液 | 1 mM | 2.3120 mL | 11.5602 mL | 23.1203 mL | | 5 mM | 0.4624 mL | 2.3120 mL | 4.6241 mL | | 10 mM | 0.2312 mL | 1.1560 mL | 2.3120 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (5.78 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (5.78 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (5.78 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (5.78 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 3. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (5.78 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (5.78 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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