QX77
目录号 : GC32962
QX77是一种分子伴侣介导的自噬 (Chaperone-mediated autophagy, CMA) 激活剂。
Cas No.:1798331-92-6
Sample solution is provided at 25 µL, 10mM.
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QX77 is a chaperone-mediated autophagy (CMA) activator[1]. QX77 can activate CMA to ameliorate intracellular trafficking defects[2], and also reduce ferroptosis and alleviate oxidative stress[3-4].
In vitro, when human pancreatic stellate cells (HPSCs) treated with TGF-β1 were co-treated with QX77 (5ng/mL) and 20ng/mL MFG-E8 for 24 hours, QX77 eliminated the inhibitory effect of MFG-E8 on the TGF-β1-induced upregulation of LAMP2A expression and downregulation of MEF2D expression. QX77 attenuated the mitigating effect of MFG-E8 on oxidative stress[5]. In SKOV3/DDP cells treated with DDP (6μg/mL), intervention with QX77 (10μM) for 12 hours enhanced cell viability and affected the expression and localization of autophagy-related proteins[6].
In vivo, in a diabetic rat model, intravitreal injection of QX77 (2.5mg/kg) was administered once per week starting from the first day of model establishment for a duration of 2 weeks. QX77 significantly improved diabetes-induced impairment of retinal physiological function, reduced the expression of ACSL4 protein, decreased MDA levels and the accumulation of the toxic lipid peroxidation product 4-HNE in the retina, and reduced the number of autophagosomes, demonstrating a protective effect against early diabetic retinopathy[4].
References:
[1] Rahman F, Johnson JL, Ait Kbaich M, et al. Reconstitution of Rab11-FIP4 Expression Rescues Cellular Homeostasis in Cystinosis. Mol Cell Biol. 2024;44(12):577-589.
[2] Li J, Zeng S, Sun Y, et al. Gluconic acid alleviates hypertrophic scar formation through binding PLOD1, reducing p-AKT signaling and activating autophagy. Phytomedicine. 2025 Jul 25;143:156825.
[3] Liu C, Sun W, Zhu T, et al. Glia maturation factor-β induces ferroptosis by impairing chaperone-mediated autophagic degradation of ACSL4 in early diabetic retinopathy. Redox Biol. 2022 Jun;52:102292.
[4] Ren Y, Cui Q, Zhang J, et al. Z Milk Fat Globule-EGF Factor 8 Alleviates Pancreatic Fibrosis by Inhibiting ER Stress-Induced Chaperone-Mediated Autophagy in Mice. Front Pharmacol. 2021 Aug 5;12:707259.
[5] Du P, Xu X, Wang Y. Hsa_circ_0000585 promotes chemoresistance to cis-platin in epithelial cells of ovarian cancer by modulating autophagy. Biochem Biophys Res Commun. 2023 Oct 20;678:186-192.
QX77是一种分子伴侣介导的自噬 (Chaperone-mediated autophagy, CMA) 激活剂[1]。QX77可以激活分子伴侣介导的自噬改善细胞内运输缺陷[2]。QX77还可以减少细胞铁死亡，减缓氧化应激[3-4]。
在体外，QX77（5ng/ml）与20ng/mL MFG-E8同时干预TGF-β1处理的人胰腺星状细胞（HPSCs）24小时，QX77消除了MFG-E8对TGF-β1诱导的LAMP2A表达上调和MEF2D表达下降的抑制作用。QX77削弱了MFG-E8对氧化应激的缓解效果[3]。QX77（10μM）干预DDP（6μg/ml）处理的SKOV3/DDP细胞12。QX77提升了细胞活力，并影响了自噬相关蛋白的表达与定位[5]。
在体内，QX77（2.5mg/kg）在糖尿病大鼠模型建立第一天开始，每周一次玻璃体内注射，持续处理2周。QX77显著改善了糖尿病引起的视网膜生理功能损伤，降低了视网膜中ACSL4蛋白的表达、MDA水平以及有毒脂质过氧化产物4-HNE的积累，并减少了自噬体的数量，对早期糖尿病视网膜病变具有保护作用[4]。
| Cell experiment [1]: | |
Cell lines | Human pancreatic stellate cells (HPSCs) |
Preparation Method | HPSCs were cultured in Ham's F-12K medium supplemented with 20% fetal bovine serum (FBS) at 37°C, 5% CO₂. HPSCs were treated with TGF-β1 (5ng/mL) to induce activation, with or without QX77 (5ng/mL) and recombinant human MFG-E8 (20ng/mL) for 24 hours. |
Reaction Conditions | 5ng/mL; 24h |
Applications | QX77 upregulated LAMP2A expression and reversed the inhibitory effects of MFG-E8 on TGF-β1-induced CMA in HPSCs. QX77 also eliminated MFG-E8's suppressive effects on collagen I and α-SMA expression, as well as MFG-E8's reduction of oxidative stress in activated HPSCs. |
| Animal experiment [2]: | |
Animal models | Sprague-Dawley (SD) rats |
Preparation Method | Diabetic rats were established by streptozotocin (STZ) injection. QX77 (2.5mg/kg) was intravitreally injected on the first day of detectable hyperglycemia and maintained for 2 weeks. Animals were sacrificed for retinal analysis. |
Dosage form | 2.5mg/kg; i.p. |
Applications | QX77 significantly rescued retinal physiological function by reducing ACSL4 protein expression and lipid peroxidation (MDA and 4-HNE levels) in the RPE-Bruch's membrane-choriocapillaris complex. |
References: | |
| Cas No. | 1798331-92-6 | SDF | |
| Canonical SMILES | CC(NC1=CC=C(C2=NC3=CC=C(Cl)C=C3OC2)C=C1)=O | ||
| 分子式 | C16H13ClN2O2 | 分子量 | 300.74 |
| 溶解度 | DMSO : ≥ 64 mg/mL (212.81 mM) | 储存条件 | Store at -20°C |
| General tips | 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°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.3251 mL | 16.6257 mL | 33.2513 mL |
| 5 mM | 665 μL | 3.3251 mL | 6.6503 mL |
| 10 mM | 332.5 μL | 1.6626 mL | 3.3251 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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