2. PROTAC Anti-infection
  3. PROTACs Enterovirus
  4. PROTAC EV-A71 Degrader-1

PROTAC EV-A71 Degrader-1 是一种靶向 EV-A71 3D 聚合酶的 PROTAC 降解剂，对多种肠道病毒具有广谱活性。PROTAC EV-A71 Degrader-1 可通过泛素-蛋白酶体和自噬-溶酶体途径诱导 EV-A71 3D 聚合酶降解，阻断病毒复制。PROTAC EV-A71 Degrader-1 可保护受感染小鼠免于死亡，减轻组织损伤，并具有安全性特征。PROTAC EV-A71 Degrader-1 可用于肠道病毒感染的研究。(粉色: EV-A71 配体 (HY-19339); 蓝色: E3 连接酶配体 (HY-W012479); 黑色: 连接子 (HY-W105744))。

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PROTAC EV-A71 Degrader-1

PROTAC EV-A71 Degrader-1 Chemical Structure

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PROTAC EV-A71 Degrader-1 相关抗体

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PROTAC EV-A71 Degrader-1 is a PROTAC degrader targeting EV-A71 3D polymerase, with broad-spectrum activity against a variety of enteroviruses. PROTAC EV-A71 Degrader-1 induces the degradation of EV-A71 3D polymerase through the ubiquitin-proteasome and autophagy-lysosome pathways, and blocks viral replication. PROTAC EV-A71 Degrader-1 protects infected mice from death, alleviates tissue damage, and exhibits safety profiles. PROTAC EV-A71 Degrader-1 can be used in the research of enterovirus infections. (Pink: EV-A71 ligand (HY-19339); Blue: E3 ligase ligand (HY-W012479); Black: linker (HY-W105744))[1].

体外研究
(In Vitro)

PROTAC EV-A71 Degrader-1 (compound N-6) (5-10 μM; 12-24 h) 可在 HEK293T 细胞中特异性降解 EV-A71 3Dpol，且具有较强的结合亲和力 (Kd = 8.08 nM)[1]。
PROTAC EV-A71 Degrader-1 (0.001-10 μM; 24-48 h) 可强效抑制 RD 细胞中 EV-A71 的复制，其 EC50 为 0.149 μM，细胞毒性较低 (CC50 = 28.073 μM)，选择性指数高达 188.409[1]。
PROTAC EV-A71 Degrader-1 (48 h) 在 RD 细胞中对 CV-A16、CV-B1、CV-A21 和 EV-D68 表现出广谱、纳摩尔级的抗肠道病毒活性[1]。

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

PROTAC EV-A71 Degrader-1 相关抗体:

Cell Viability Assay[1]

Cell Line: RD cells
Concentration: /
Incubation Time: 48 h
Result: Achieved half-maximal effective concentration (EC50) values of 0.078 μM against CV-A16, 0.052 μM against CV-B1, 0.096 μM against CV-A21, and 0.123 μM against EV-D68.
Had EC90 values of 0.192 μM for CV-A16, 0.188 μM for CV-B1, 0.532 μM for CV-A21, and 0.324 μM for EV-D68.
药代动力学
(Parmacokinetics)
Species Dose Route T1/2 Tmax Cmax AUC0-t AUC0-∞ CL F
Rat[1] 3 mg/kg i.v. 2.11 h 0.08 h 697 ng/mL 321 ng·h/mL 327 ng·h/mL 154 mL/min/kg /
Rat[1] 8 mg/kg i.p. 12.1 h 6.67 h 14.2 ng/mL 222 ng·h/mL 212 ng·h/mL 629 mL/min/kg 24.3 %
体内研究
(In Vivo)

PROTAC EV-A71 Degrader-1 (1-10 mg/kg；腹腔注射；每日 1 次；连续 4 天) 可使 60%感染 EV-A71 的新生 KM 小鼠免于死亡，减轻病毒诱导的体重下降及多器官组织病理学损伤，并具有良好的安全性特征[1]。

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

Animal Model: Kunming (KM) mice (female, 7 days old, EV-A71 infection model via intraperitoneal injection of 1.0 × 107 PFU mouse-adapted EV-A71 GZ-CII strain)[1]
Dosage: 1 mg/kg (mortality protection, body weight loss alleviation, histopathology improvement); 10 mg/kg (safety assessment)
Administration: i.p.; daily; 4 days
Result: Protected 60% of infected mice from mortality.
Significantly alleviated virus-induced body weight loss.
Attenuated histopathological damage in liver, skeletal muscle, kidney, intestine, and brain (including reduced hepatic steatosis, myocyte necrosis, renal tubular atrophy, intestinal vacuolar degeneration, and neuronal pyknosis).
Caused no acute toxicity or body weight reduction in neonatal mice at 10 mg/kg dose.
分子量

682.92

Formula

C39H50N6O3S
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

PROTAC EV-A71 Degrader-1 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:

PROTAC EV-A71 Degrader-1PROTACsEnterovirusRhinovirusHRVHRVsHEVHEVsCV-B1enterovirusesRD cellsautophagy-lysosomal pathwayHEK293T cellsEV-D68CV-A16CV-A21ubiquitin-proteasome pathwayEV-A71 3D polymeraseInhibitorinhibitorinhibit

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