Paclobutrazol
(Synonyms: 多效唑；氯丁唑) 目录号 : GC47854
Paclobutrazol是一种高效的植物生长调节剂，通过抑制赤霉素（一种负责茎伸长和其他生长过程的植物激素）的生物合成发挥作用。
Cas No.:76738-62-0
Sample solution is provided at 25 µL, 10mM.
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Paclobutrazol is a highly efficient plant growth regulator that functions by inhibiting the biosynthesis of gibberellins, which are plant hormones responsible for stem elongation and other growth processes[1]. Paclobutrazol can be absorbed by plant roots and transported to the stem, making it an important tool for modulating plant structure and enhancing agricultural productivity[2]. Studies have shown that the inhibitory effect of Paclobutrazol on gibberellin production varies among different plant species but generally lies in the low micromolar range [3]. Additionally, Paclobutrazol has been found to cause embryotoxicity in zebrafish[4].
In vitro, pre-treatment of HepaRG hepatocytes with Paclobutrazol (90–360µM) for 72 hours significantly reduced cell viability, increased oxidative stress levels, and elevated the apoptosis rate. Moreover, Paclobutrazol impaired autophagy by inhibiting the AMPK/mTOR signaling pathway, thereby exacerbating apoptosis[5]. Pre-treatment of free endosperm cells from Cucurbita maxima with Paclobutrazol (9.5nM) significantly inhibited the activity of ent-kaurene oxidase. Additionally, the azido derivative of Paclobutrazol (AZP) bound to cytochrome P450 in Cucurbita maxima microsomes and induced a Type II spectral change, with an apparent binding constant of 0.24±0.04µM[6].
In vivo, exposure of zebrafish (Danio rerio) to Paclobutrazol (10mg/L) for 14 days significantly induced oxidative stress, increased the levels of malondialdehyde (MDA) and protein carbonyl (PC), and decreased the activities of superoxide dismutase (SOD) and catalase (CAT). Paclobutrazol also exhibited neurotoxicity in zebrafish[7]. Paclobutrazol (32.5mg/kg and 260mg/kg) was administered via gavage to 6–8-week-old Sprague-Dawley rats for 28 days. Paclobutrazol significantly reduced the levels of thyroid hormone T4 in rat serum, increased thyroid follicular cell inflammation and follicular deformation, and disrupted the function of the thyroid endocrine system[8].
References:
[1] Xu Y, Zhu Y, Wang X, et al. PACLOBUTRAZOL-RESISTANCE4 positively regulates cell expansion to promote tendril elongation in cucumber. Plant Physiol. 2023 Aug 3;192(4):2756-2767.
[2] Urfan M, Hakla HR, Sharma S, et al. Paclobutrazol improves surface water use efficiency by regulating allometric trait behavior in maize. Chemosphere. 2022 Nov;307(Pt 3):135958.
[3] Zhang Y, He Z, Xing P, et al. Effects of paclobutrazol seed priming on seedling quality, photosynthesis, and physiological characteristics of fragrant rice. BMC Plant Biol. 2024 Jan 17;24(1):53.
[4] Hussain A, Audira G, Siregar P, et al. Waterborne Exposure of Paclobutrazol at Environmental Relevant Concentration Induce Locomotion Hyperactivity in Larvae and Anxiolytic Exploratory Behavior in Adult Zebrafish.
[5] Luo Y, Lu S, Sun X, et al. Paclobutrazol exposure induces apoptosis and impairs autophagy in hepatocytes via the AMPK/mTOR signaling pathway. J Biochem Mol Toxicol. 2021 Oct;35(10):e22874.
[6] Hallahan DL, Heasman AP, Grossel MC, et al. Synthesis and biological activity of an azido derivative of paclobutrazol, an inhibitor of gibberellin biosynthesis. Plant Physiol. 1988 Dec;88(4):1425-9.
[7] Guo D, Luo L, Kong Y, et al. Enantioselective neurotoxicity and oxidative stress effects of paclobutrazol in zebrafish (Danio rerio). Pestic Biochem Physiol. 2022 Jul;185:105136.
[8] Liu H, Xu Y, Wang Y, et al. Study on endocrine disruption effect of paclobutrazol and uniconazole on the thyroid of male and female rats based on lipidomics. Ecotoxicol Environ Saf. 2022 Apr 1;234:113386.
Paclobutrazol是一种高效的植物生长调节剂，通过抑制赤霉素（一种负责茎伸长和其他生长过程的植物激素）的生物合成发挥作用[1]。Paclobutrazol可被植物根部吸收并转运至茎部，是调节植物结构和提高农业生产力的重要工具[2]。研究发现，Paclobutrazol对赤霉素生产的抑制作用在不同植物种类中有所不同，但通常处于低微摩尔范围[3]。此外，Paclobutrazol会引起斑马鱼胚胎毒性[4]。
在体外，Paclobutrazol（90–360μM）预处理HepaRG肝细胞72小时后，细胞活性显著下降，氧化应激水平升高，细胞凋亡率增加。此外，Paclobutrazol还通过抑制AMPK/mTOR信号通路，损害细胞自噬功能，进而加剧细胞凋亡[5]。Paclobutrazol（9.5nM）预处理南瓜（Cucurbita maxima）游离胚乳细胞后，能够显著抑制ent-kaurene氧化酶的活性。此外，Paclobutrazol的叠氮衍生物（AZP）能够与南瓜胚乳微粒体中的细胞色素P450结合，并诱导II型光谱变化，结合常数为0.24±0.04μM [6]。
在体内，Paclobutrazol（10mg/L）暴露于斑马鱼（Danio rerio）14天，显著诱导氧化应激，增加丙二醛（MDA）和蛋白羰基（PC）含量，并降低超氧化物歧化酶（SOD）和过氧化氢酶（CAT）活性。同时，Paclobutrazol显示出对斑马鱼具有神经毒性[7]。Paclobutrazol（32.5mg/kg和260mg/kg）通过灌胃给药，处理6–8周龄的Sprague-Dawley大鼠，持续28天。Paclobutrazol显著降低了大鼠血清中甲状腺激素T4水平，增加了甲状腺滤泡细胞炎症和滤泡变形，干扰了甲状腺内分泌系统的功能[8]。
| Cell experiment [1]: | |
Cell lines | HepaRG hepatocytes |
Preparation Method | HepaRG cells were seeded on 96-well plates at a density of 8×10⁴ cells/well and cultured in RPMI 1640 medium supplemented with 10% fetal bovine serum and 1% penicillin-streptomycin under a humidified atmosphere containing 5% CO₂ at 37°C until they reached the logarithmic growth phase. Paclobutrazol (90, 180, and 360µM) was dissolved in DMSO and incubated in FBS‐freecomplete medium for 72h. |
Reaction Conditions | 90, 180, and 360µM; 72h |
Applications | Paclobutrazol inhibited cell viability in a dose-dependent manner, induced apoptosis, and impaired autophagy via the AMPK/mTOR signaling pathway. |
| Animal experiment [2]: | |
Animal models | Sprague-Dawley rats |
Preparation Method | Rats were randomly divided into five groups (n = 16) and exposed to Paclobutrazol via gavage for 28 days. The doses were designed based on previous studies and were equal to 1/5 and 1/40 of the LD50 of Paclobutrazol. For paclobutrazol, both male and female rats were exposed to low dose of 32.5mg/kg (Paclobutrazol) and high dose of 260mg/kg (H-Paclobutrazol). The control group received 0.5% CMC-Na solution (2ml/200g). |
Dosage form | 32.5mg/kg (low dose) and 260mg/kg (high dose); via gavage. |
Applications | Paclobutrazol significantly reduced the levels of thyroid hormone T4 in rat serum, increased thyroid follicular cell inflammation and follicular deformation, and disrupted the function of the thyroid endocrine system. |
References: | |
| Cas No. | 76738-62-0 | SDF | |
| 别名 | 多效唑；氯丁唑 | ||
| Canonical SMILES | ClC1=CC=C(C[C@]([C@@H](O)C(C)(C)C)([H])N2N=CN=C2)C=C1 | ||
| 分子式 | C15H20ClN3O | 分子量 | 293.8 |
| 溶解度 | DMF: 10 mg/ml,DMSO: 10 mg/ml,Ethanol: 10 mg/ml,Ethanol:PBS(pH 7.2) (1:1): 0.5 mg/ml | 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 | 3.4037 mL | 17.0184 mL | 34.0368 mL |
| 5 mM | 0.6807 mL | 3.4037 mL | 6.8074 mL |
| 10 mM | 0.3404 mL | 1.7018 mL | 3.4037 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: >97.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet