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别名 YH53, YH 53
YH-53 是一种高效的肽模拟 3CLpro 抑制剂,具有独特的苯并噻唑酮药效团,对 SARS-CoV-1 和 SARS-CoV-2 主蛋白酶均表现出低纳摩尔级抑制活性,并能有效阻断 SARS-CoV-2 的复制,为抗病毒及 COVID-19 研究提供了一种在结构和机制上均得到验证的化合物。


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YH-53 是一种高效的肽模拟 3CLpro 抑制剂,具有独特的苯并噻唑酮药效团,对 SARS-CoV-1 和 SARS-CoV-2 主蛋白酶均表现出低纳摩尔级抑制活性,并能有效阻断 SARS-CoV-2 的复制,为抗病毒及 COVID-19 研究提供了一种在结构和机制上均得到验证的化合物。
| 规格 | 价格 | 库存 | 数量 |
|---|---|---|---|
| 1 mg | ¥ 1,650 | 8-10周 | |
| 5 mg | ¥ 4,130 | 8-10周 | |
| 10 mg | ¥ 5,880 | 8-10周 | |
| 25 mg | ¥ 8,750 | 8-10周 | |
| 50 mg | ¥ 11,800 | 8-10周 | |
| 100 mg | ¥ 15,900 | 8-10周 | |
| 1 mL x 10 mM (in DMSO) | ¥ 4,560 | 8-10周 |
| 产品描述 | YH-53 is a potent peptidomimetic 3CLpro inhibitor featuring a unique benzothiazolyl ketone pharmacophore that displays low-nanomolar inhibition of SARS-CoV-1 and SARS-CoV-2 main proteases and effectively blocks SARS-CoV-2 replication, thereby providing a structurally distinctive and mechanistically validated compound for antiviral and COVID-19 research. |
| 体外活性 | YH-53 (1-25 μM; for 24 h) potently reduces copies of total RNA with increased concentrations in VeroE6/TMPRSS2 cells [1]. YH-53 (1, 5, 10, 15, 20, 25 μM; for 48 h) with 10 μM completely blocks the viral proliferation against SARS-CoV-2 were examined by a cytopathic effect (CPE) assay in Vero cells [1]. YH-53 (10, 100 μM; for 24 h) has no cytotoxicity with a CC 50 value of >100 μM in vero cells [1]. YH-53 (10 μM) moderately inhibits CYP1A2, CYP2D6, and CYP2C8 (26.6%, 38.0%, 66.4%, respectively). YH-53 has no inhibition on CYP2C9 and CYP3A4 [1]. YH-53 inhibits SARS-CoV 3CL pro with an IC 50 of 0.74 μM. RT-PCR [1] Cell Line: VeroE6/TMPRSS2 cells Concentration: 1, 5, 10, 15, 20, 25 μM Incubation Time: 24 hours Result: Efficiently reduced copies of total RNA. |
| 体内活性 | YH-53 (0.1 mg/kg; iv) exhibits a T 1/2 of 2.97 hours, an AUC 0–∞ of 19.7 ng h/mL, a V d of 3.51 L/kg in rats [1]. YH-53 (0.5 mg/kg; oral) exhibits a T 1/2 of 9.64 hours, an AUC 0–∞ of 3.49 ng h/mL, a C max of 1.08 ng/mL in rats [1]. Animal Model: Rats [1] Dosage: 0.1 mg/kg (Pharmacokinetic Analysis) Administration: IV Result: Had a T 1/2 of 2.97 hours, an AUC 0–∞ of 19.7 ng h/mL, a V d of 3.51 L/kg. |
| 别名 | YH53, YH 53 |
| 分子量 | 575.68 |
| 分子式 | C30H33N5O5S |
| CAS No. | 1471484-62-4 |
| Smiles | O(C)C1=C2C(NC(C(N[C@H](C(N[C@H](C(=O)C3=NC=4C(S3)=CC=CC4)C[C@H]5C(=O)NCC5)=O)CC(C)C)=O)=C2)=CC=C1 |
| 颜色 | White |
| 物理性状 | Solid |
| 存储 | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||||||||||||
| 溶解度信息 | DMSO: 40 mg/mL (69.48 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||
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DMSO
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以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。
对于不同动物的给药剂量换算,您也可以参考 更多