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  3. Alloxan

Alloxan 是一种 26S20S 蛋白酶体 (proteasome) 抑制剂和糖尿病诱导剂。Alloxan 可直接抑制纯化蛋白酶体的胰凝乳蛋白酶样和胰蛋白酶样肽酶活性。Alloxan 可通过破坏蛋白酶体功能诱导泛素化蛋白积累。Alloxan 会被胰腺 β 细胞摄取,升高 ROS 水平,触发坏死,减少胰岛素生成并诱导 β 细胞死亡。Alloxan 会诱导大鼠子代出现椎体组织损伤、软骨细胞紊乱和生长迟缓。Alloxan 可用于 1 型糖尿病的相关研究。

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Alloxan

Alloxan Chemical Structure

CAS No. : 50-71-5

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MCE 顾客使用本产品发表的 1 篇科研文献

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Alloxan is a 26S and 20S proteasome (proteasome) inhibitor and diabetes inducer. Alloxan directly inhibits the chymotrypsin-like and trypsin-like peptidase activities of purified proteasomes. Alloxan induces the accumulation of ubiquitinated proteins by impairing proteasome function. Alloxan is taken up by pancreatic β cells, increases ROS levels, triggers necrosis, reduces insulin production and induces β cell death. Alloxan induces vertebral tissue damage, chondrocyte disorder and growth retardation in rat offspring. Alloxan can be used in research related to type 1 diabetes and diabetes[1][2][3].

体外研究
(In Vitro)

Alloxan (5 mM; 24 h) 会导致 NRK 细胞中泛素化蛋白显著积累,表明泛素-蛋白酶体系统功能受损[1]
Alloxan (10 mM; 0-7 hours) 可显著减慢 293 细胞中蛋白酶体特异性底物 GFP-CL1 的清除速度,证实泛素-蛋白酶体系统功能受损[1]
Alloxan (5 mM; 24 h) 可显著抑制 NRK 细胞核提取物中的胰凝乳蛋白酶样和胰蛋白酶样肽酶活性[1]
Alloxan (1 μM-333 mM) 在体外可剂量依赖性地抑制 NRK 细胞核提取物中的胰凝乳蛋白酶样和胰蛋白酶样肽酶活性,在 3.3 mM 时观察到最大抑制作用[1]
Alloxan (5 mM; 30 min) 可在体外 NRK 细胞核提取物中抑制 GST-Sp1 的蛋白酶体降解[1]
Alloxan (1 μM-333 mM) 在体外可直接且呈剂量依赖性地抑制纯化 26S proteasomes 的胰凝乳蛋白酶样和胰蛋白酶样肽酶活性[1]
Alloxan (1 μM-333 mM) 可在体外直接且呈剂量依赖性地抑制纯化 20S 蛋白酶体的胰凝乳蛋白酶样和胰蛋白酶样肽酶活性,表明其作用于蛋白酶体的催化核心[1]

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

Western Blot Analysis[1]

Cell Line: NRK (normal rat kidney) cells
Concentration: 5 mM
Incubation Time: 24 h
Result: Caused significant accumulation of ubiquitinated proteins, as shown by increased signal in anti-ubiquitin Western blotting.
体内研究
(In Vivo)

Alloxan (150 mg/kg;腹腔注射;单次注射) 可诱导糖尿病 (母鼠血糖>300 mg/dL),并会导致新生、3 周龄及 2 月龄子代出现明显的生长迟缓以及腰椎结构/超微结构损伤,同时还会造成胰腺 β 细胞损伤及胰岛素表达水平降低[2]
Alloxan (150 mg/kg; 腹腔注射; 单次给药) 可在瑞士白化小鼠中诱导稳定的高血糖状态,符合条件的动物可维持升高的血糖水平至少 21 天[3]

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

Animal Model: Albino rats (adult females, 3-month-old, 200-250 g; adult males, 3-month-old, 200-250 g; male offspring studied at newborn, 3-week-old, and 2-month-old ages; diabetes induced via single intraperitoneal injection of alloxan monohydrate in pregnant females)[2]
Dosage: 150 mg/kg
Administration: i.p.; single injection
Result: Reduced mean body weight to 4.57 g, crown-rump length to 4.00 cm, snout-rump length to 3.23 cm, crown-heel length to 4.15 cm, and 6th lumbar vertebra epiphyseal growth plate thickness to 221.60 μm in newborn offspring compared to controls.
Caused disorganized, vacuolated chondrocytes, empty lacunae, diminished matrix staining, and shrunken reserve/proliferative cells with irregular nuclei and damaged mitochondria in lumbar vertebrae of newborn offspring.
Increased maternal blood glucose to 311.75 mg/dL, reduced pancreatic islet number/surface area, induced atrophied islet cells with apoptotic nuclei, and caused very weak insulin immunostaining.
Reduced mean body weight to 22.67 g, crown-rump length to 7.37 cm, snout-rump length to 7.05 cm, crown-heel length to 9.35 cm, and 6th lumbar vertebra epiphyseal growth plate thickness to 314.70 μm in 3-week-old offspring compared to controls.
Caused decreased growth plate thickness, disorganized/vacuolated chondrocytes, empty lacunae, diminished matrix staining, and shrunken reserve cells with irregular nuclei/damaged mitochondria in lumbar vertebrae of 3-week-old offspring.
Reduced mean body weight to 144.33 g, crown-rump length to 12.00 cm, snout-rump length to 11.00 cm, crown-heel length to 15.87 cm, and 6th lumbar vertebra epiphyseal growth plate thickness to 317.03 μm in 2-month-old offspring compared to controls.
Caused decreased growth plate thickness, disorganized/vacuolated chondrocytes, empty lacunae, and diminished matrix staining in lumbar vertebrae of 2-month-old offspring.
Animal Model: Swiss albino mice (either sex, 32-34 grams, induced via single intraperitoneal injection of alloxan)[3]
Dosage: 150 mg/kg
Administration: i.p.; single dose
Result: Induced fasting blood glucose levels of ≥200 mg/dL 48 hours post-injection.
Maintained blood glucose levels around 262 mg/dL at day 0 and 234 mg/dL at day 21 in diabetic control mice.
分子量

142.07

Formula

C4H2N2O4

CAS 号
结构分类
初始来源
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
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  • 稀释计算器

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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.

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Alloxan
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HY-116823
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