Propyl pyrazole triol (PPT)
(Synonyms: PPT) 目录号 : GC14370
Propyl pyrazole triol (PPT)是一种选择性雌激素受体α（ERα）激动剂，可通过在神经系统激活ERα，保护神经元免受氧化应激与炎症损伤。
Cas No.:263717-53-9
Sample solution is provided at 25 µL, 10mM.
Propyl pyrazole triol (PPT) is a selective estrogen receptor α (ERα) agonist that can shield neurons from oxidative stress and inflammatory damage through ERα activation in the nervous system[1]. The binding affinity of Propyl pyrazole triol to the two ERs (ERα and ERβ) shows more than a 400-fold preference for ERα[2]. Propyl pyrazole triol is shown as estradiol to modulate hippocampal N-methyl-d-aspartate (NMDA) receptors and AMP-activated protein kinase (AMPK) receptors in the cortex and striatum of ovariectomized rats[3].
In vitro, adult rat dorsal root ganglion neurons were exposed to 1, 10, or 100nM Propyl pyrazole triol. A 1h treatment elicited a concentration-dependent rise in AMPK phosphorylation, whereas a 24h exposure to 10nM Propyl pyrazole triol significantly increased total neurite outgrowth, elevated nuclear activating transcription factor 3 (ATF3) expression, and improved multiple parameters of mitochondrial function[4]. Treatment of aortic smooth-muscle cells with 100µM Propyl pyrazole triol raised cyclic GMP (cGMP) from a basal level of 0.84±0.28 to 2.05±0.3pmol/mg protein, while 50µM Propyl pyrazole triol reduced the intracellular calcium signal by 70.6±9.95%[5].
In vivo, starting two days after ovariectomy, rats received daily subcutaneous injections of 1mg/kg Propyl pyrazole triol for 14 days, which prevented the loss of uterine weight, blocked the rise in [3H]α-amino-3-hydroxy-5-methyl-4-isoxazoleproprionic acid (AMPA) binding in the striatum and nucleus accumbens, and reduced GluR2 mRNA in the prefrontal cortex and striatum[6]. Male rats received daily subcutaneous injections with 1mg/kg Fadrozole 1h before mating for 29 days and were given an additional single 1mg/kg Propyl pyrazole triol subcutaneous injection on Days 13 and 29 showed more mounting but reached sexual satiety sooner[7].
References:
[1] Zhang K, Hou B, Yan T, et al. Identification of therapeutic target genes for age-related hearing loss through systematic genome-wide mendelian randomization of druggable genes. Exp Gerontol. 2025;200:112676.
[2] Vijaykumar D, Al-Qahtani MH, Welch MJ, et al. Synthesis and biological evaluation of a fluorine-18 labeled estrogen receptor-alpha selective ligand: [18F] propyl pyrazole triol. Nucl Med Biol. 2003;30(4):397-404.
[3] Morissette M, Le Saux M, D'Astous M, et al. Contribution of estrogen receptors alpha and beta to the effects of estradiol in the brain. J Steroid Biochem Mol Biol. 2008;108(3-5):327-338.
[4] Mishra P, Albensi BC, Fernyhough P. Estradiol activates the CaMKKβ/AMPK pathway to enhance neurite outgrowth in cultured adult sensory neurons. Mol Cell Neurosci. 2025;133:104008.
[5] Alda JO, Valero MS, Pereboom D, et al. Endothelium-independent vasorelaxation by the selective alpha estrogen receptor agonist propyl pyrazole triol in rat aortic smooth muscle. J Pharm Pharmacol. 2009;61(5):641-646.
[6] Le Saux M, Estrada-Camarena E, Di Paolo T. Selective estrogen receptor-alpha but not -beta agonist treatment modulates brain alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptors. J Neurosci Res. 2006;84(5):1076-1084.
[7] Corre PHC, Mainwaring JM, Peralta KKZ, et al. Low dose of propyl-pyrazole-triol, an agonist of estrogen receptor alpha, administration stimulates the Coolidge effect in fadrozole-treated male rats. Horm Behav. 2024;161:105520.
Propyl pyrazole triol (PPT)是一种选择性雌激素受体α（ERα）激动剂，可通过在神经系统激活ERα，保护神经元免受氧化应激与炎症损伤[1]。其对ERα和ERβ的亲和力差异达400倍以上，显著偏好ERα[2]。与雌二醇类似，Propyl pyrazole triol可调节去卵巢大鼠海马N-甲基-d-天冬氨酸（NMDA）受体及大脑皮层与纹状体内的AMP活化蛋白激酶（AMPK）受体[3]。
在体外，成年大鼠背根神经节神经元分别暴露于1、10或100nM的Propyl pyrazole triol。1小时处理即可浓度依赖性地升高AMPK磷酸化水平；而24小时10nM的Propyl pyrazole triol处理显著促进总神经突生长、提高核内转录激活因子3（ATF3）表达，并改善多项线粒体功能指标[4]。对主动脉平滑肌细胞给予100µM的Propyl pyrazole triol，可使环磷酸鸟苷（cGMP）由基线0.84±0.28升至2.05±0.3pmol/mg蛋白；50µM的Propyl pyrazole triol则可降低细胞内钙信号70.6±9.95%[5]。
在体内，大鼠于卵巢切除术后第2天开始每日皮下注射1mg/kg的Propyl pyrazole triol，连续14天，可阻止子宫重量丢失和纹状体与伏隔核中[3H]α-氨基-3-羟基-5-甲基-4-异恶唑丙酸（AMPA）结合的增加，并降低前额叶皮层与纹状体中GluR2 mRNA的表达[6]。雄性大鼠于交配前29天每日皮下注射1mg/kg芳香化酶抑制剂Fadrozole，并于第13、29天额外单次皮下注射1mg/kg的Propyl pyrazole triol，大鼠爬背次数增加但更快达到性饱足[7]。
| Cell experiment [1]: | |
Cell lines | Adult rat dorsal root ganglion (DRG) neurons |
Preparation Method | DRG neurons from 2-month-old adult male and female SD rats (weight 200-250g) were dissected, isolated, and dissociated. Propyl pyrazole triol were added at specific time points to maintain a consistent total culture period of 24h for all experiments. For 24h treatments, agents were added at the time of seeding. |
Reaction Conditions | 1, 10, 100nM; 1, 24h |
Applications | Exposure of DRG neurons to increasing concentrations of Propyl pyrazole triol for 1h dose-dependently elevated AMP-activated protein kinase (AMPK) phosphorylation, whereas a 24h treatment with 10nM Propyl pyrazole triol significantly increased total neurite outgrowth, augmented nuclear activating transcription factor 3 (ATF3) expression, and enhanced multiple indices of mitochondrial function. |
| Animal experiment [2]: | |
Animal models | Adult female Sprague-Dawley rats |
Preparation Method | The experiment consisted of rats divided into five groups of 10 animals each. The first group comprised intact control rats at random stages of the estrous cycle treated with vehicle [4% ethanol, 4% polyethylene glycol 600 (PEG-600), 1% gelatin, and 0.9% NaCl]. The other group comprised ovariectomized rats. Ovariectomy was performed on animals under anesthesia with a 1.5% isoflurane-air mixture. Treatments began 2 days after ovariectomy with one daily subcutaneous injection (0.5ml/rat) for 14 days of vehicle, 1mg/kg Propyl pyrazole triol. |
Dosage form | 1mg/kg; subcutaneous injection |
Applications | Sixteen days after ovariectomy, uterine weight in ovariectomized rats dropped by 85% compared with intact rats, whereas Propyl pyrazole triol treatment raised uterine weight above that of intact rats. In the prefrontal cortex and striatum, ovariectomy did not alter GluR2 mRNA, but Propyl pyrazole triol treatment reduced it by 31% and 20%, respectively. In the striatum and nucleus accumbens, ovariectomy increased [3H]α-amino-3-hydroxy-5-methyl-4-isoxazoleproprionic acid (AMPA) binding, and Propyl pyrazole triol treatment prevented this increase in each region. |
References: | |
| Cas No. | 263717-53-9 | SDF | |
| 别名 | PPT | ||
| 化学名 | 4-(1,5-bis(4-hydroxyphenyl)-4-propyl-1H-pyrazol-3(2H)-ylidene)cyclohexa-2,5-dienone | ||
| Canonical SMILES | OC1=CC=C(C=C1)C(N(C(C=C2)=CC=C2O)N/3)=C(CCC)C3=C(C=C4)/C=CC4=O | ||
| 分子式 | C24H22N2O3 | 分子量 | 386.45 |
| 溶解度 | ≤10mg/ml in ethanol;20mg/ml in DMSO | 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。 |
||
| 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.5877 mL | 12.9383 mL | 25.8766 mL |
| 5 mM | 0.5175 mL | 2.5877 mL | 5.1753 mL |
| 10 mM | 0.2588 mL | 1.2938 mL | 2.5877 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
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
