EIDD-2749 (4'-Fluorouridine) 是一种口服有效的RdRp抑制剂。EIDD-2749 能有效抑制RSV和SARS-CoV-2的复制。EIDD-2749 还表现出抗HCV和淋巴细胞性脉络丛脑膜炎病毒 (LCMV) 的活性。EIDD-2749 是一种很有潜力的COVID-19口服治疗候选剂,也适用于其他 RNA 病毒的研究。
生物活性 | EIDD-2749 (4'-Fluorouridine) is an orally activeRdRpinhibitor. EIDD-2749 effectively blocks the replication ofRSVandSARS-CoV-2. EIDD-2749 also exhibits activity againstHCVandlymphocytic choriomeningitis virus(LCMV). EIDD-2749 is a promising oral therapeutic candidate forCOVID-19and is also suitable for research on other RNA viruses[1][2][3]. |
IC50& Target | RdRp, RSV,SARS-CoV-2, HCV, COVID-19, LCMV[1][2][3]. |
体外研究 (In Vitro) | EIDD-2749 induces a delayed stalling of phosphodiester bond formation by RSV and SARS-CoV-2 RdRP[1]. EIDD-2749 is rapidly anabolizes, metabolically stable, and potently antiviral in disease-relevant well-differentiated HAE cultures[1]. EIDD-2749 shows a ≥17-fold increase in anti-RSV potency relative to that on HEp-2 cells; however, the low cytotoxicity levels remains unchanged (CC50169 mM), resulting in a high SI (SI = EC50/CC50) of ≥1877[1]. EIDD-2749 inhibits SARS-CoV-2 with an EC50value of 0.2-0.6 M[2]. EIDD-2749 has an EC50of 1.86 μM in theVero E6 cell line, cytotoxicity with a CC50of 380 μM, and stability in human plasma[3].
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体内研究 (In Vivo) | EIDD-2749 (0.2, 1, 5 mg/kg; p.o.; single daily for 4 days) shows good orally efficacious in RSV infection mice model in a dose-dependent manner[1]. EIDD-2749 shows high efficacious to SARS-CoV-2 infection and is effective with a single daily dose versus molnupiravir administered twice daily in vivo[2].
Animal Model: | Balb/cJ mice (RSV infection model)[1]. | Dosage: | 0.2, 1, 5 mg/kg | Administration: | Oral administration; single daily for 4 days | Result: | Resulted in a statistically significant reduction in lung virus load. |
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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: H2O : 62.5 mg/mL(238.38 mM;Need ultrasonic) DMSO : 25 mg/mL(95.35 mM;Need ultrasonic) 配制储备液 1 mM | 3.8140 mL | 19.0701 mL | 38.1403 mL | 5 mM | 0.7628 mL | 3.8140 mL | 7.6281 mL | 10 mM | 0.3814 mL | 1.9070 mL | 3.8140 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 90%corn oil Solubility: ≥ 25 mg/mL (95.35 mM); Clear solution
此方案可获得 ≥ 25 mg/mL (95.35 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 250.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。 2. 请依序添加每种溶剂: 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (9.54 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (9.54 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。 3. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (9.54 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (9.54 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。 *以上所有助溶剂都可在本网站选购。
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