Ro 20-1724
(Synonyms: 4-(3-丁氧基-4-甲氧基苯基)咪唑啶-2-酮,4-(3-Butoxy-4-methoxybenzyl)-2-imidazolidinone) 目录号 : GC13842Ro 20-1724是一种选择性cAMP特异性磷酸二酯酶（PDE4）抑制剂，IC50值为1.930μM。
Cas No.:29925-17-5
Sample solution is provided at 25 µL, 10mM.
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Ro 20-1724 is a selective inhibitor of cAMP-specific phosphodiesterase (PDE4), with an IC50 value of 1.930μM [1]. Ro 20-1724 modulates brain cAMP utilization, thereby activating protein kinase A (PKA) and cAMP response element binding protein (CREB), and has been widely used to regulate brain function in animal models [2].
In vitro, Ro 20-1724 treatment for 2h significantly inhibited PDE4 activity in TSHR-CNG-HEK293 cells with an IC50 of 2.39μM[3]. Treatment with Ro 20-1724 at 100μM for 1 hour significantly inhibited IgE production in Peripheral blood mononuclear leukocytes (MNL) from patients with atopic dermatitis[4]. 100μM Ro 20-1724 promoted apoptosis of HL-60 cells within 5 hours[5].
In vivo, Ro 20-1724 treatment (500μg/kg/day; i.p.) for 21 days significantly attenuated streptozotocin-induced cognitive deficits and oxidative stress in rats[6]. In a mouse model of allergic asthma, oral administration of Ro 20-1724 at a dose of 3mg/kg/day for 10 days significantly reduced eosinophil influx into the lungs and reduced tumor necrosis factor-α, interleukin-4, and interleukin-5 levels in bronchoalveolar lavage fluid[7]. Intravenous infusion of Ro 20-1724 (10μg/kg/min) at a constant rate for one hour significantly attenuated endotoxin-induced changes in renal blood flow, renal vascular resistance, and glomerular filtration rate, and alleviated renal failure symptoms in rats[8].
References:
[1] Brackeen M F, Stafford J A, Cowan D J, et al. Design and synthesis of conformationally constrained analogs of 4-(3-butoxy-4-methoxybenzyl) imidazolidin-2-one (Ro 20-1724) as potent inhibitors of cAMP-specific phosphodiesterase[J]. Journal of medicinal chemistry, 1995, 38(24): 4848-4854.
[2] Kant G J, Meyerhoff J L, Lenox R H. In vivo effects of apomorphine and 4-(3-butoxy-4-methoxybenzyl)-2-imidazolidinone (Ro 20–1724) on cyclic nucleotides in rat brain and pituitary[J]. Biochemical Pharmacology, 1980, 29(3): 369-373.
[3] Titus S A, Li X, Southall N, et al. A cell-based PDE4 assay in 1536-well plate format for high-throughput screening[J]. SLAS Discovery, 2008, 13(7): 609-618.
[4] Cooper K D, Kang K, Chan S C, et al. Phosphodiesterase inhibition by Ro 20-1724 reduces hyper-IgE synthesis by atopic dermatitis cells in vitro[J]. Journal of investigative dermatology, 1985, 84(6): 477-482.
[5] Zhu W H, Majluf-Cruz A, Omburo G A. Cyclic AMP-specific phosphodiesterase inhibitor rolipram and RO-20-1724 promoted apoptosis in HL60 promyelocytic leukemic cells via cyclic AMP-independent mechanism[J]. Life sciences, 1998, 63(4): 265-274.
[6] Sharma V, Bala A, Deshmukh R, et al. Neuroprotective effect of RO-20-1724-a phosphodiesterase4 inhibitor against intracerebroventricular streptozotocin induced cognitive deficit and oxidative stress in rats[J]. Pharmacology Biochemistry and Behavior, 2012, 101(2): 239-245.
[7] Clayton R A, Dick C A J, Mackenzie A, et al. The effect of selective phosphodiesterase inhibitors, alone and in combination, on a murine model of allergic asthma[J]. Respiratory research, 2004, 5(1): 4.
[8] Begany D P, Carcillo J A, Herzer W A, et al. Inhibition of type IV phosphodiesterase by Ro 20-1724 attenuates endotoxin-induced acute renal failure[J]. The Journal of pharmacology and experimental therapeutics, 1996, 278(1): 37-41.
Ro 20-1724是一种选择性cAMP特异性磷酸二酯酶（PDE4）抑制剂，IC50值为1.930μM[1]。Ro 20-1724通过调节脑内cAMP利用，激活蛋白激酶A（PKA）和cAMP反应元件结合蛋白（CREB），已广泛应用于动物模型的脑功能调控研究[2]。
在体外，Ro 20-1724处理2小时可显著抑制TSHR-CNG-HEK293细胞中的PDE4活性，IC50值为2.39μM[3]。100μM的Ro 20-1724处理特应性皮炎患者来源的外周血单核白细胞（MNL）1小时能显著抑制IgE产生[4]。100μM的Ro 20-1724处理HL-60细胞5小时内可促进细胞凋亡[5]。
在体内，大鼠每日腹腔注射Ro 20-1724（500μg/kg/day；持续21天）可显著减轻链脲佐菌素诱导的认知缺陷和氧化应激[6]。过敏性哮喘小鼠模型每日口服3mg/kg剂量的Ro 20-1724（持续10天）能显著减少肺部嗜酸性粒细胞浸润，并降低支气管肺泡灌洗液中肿瘤坏死因子-α、白细胞介素-4和白细胞介素-5水平[7]。大鼠以恒定速率静脉输注Ro 20-1724（10μg/kg/分钟，持续1小时）可显著缓解内毒素诱导的肾血流量、肾血管阻力和肾小球滤过率变化，减轻肾功能衰竭症状[8]。
| Cell experiment [1]: | |
Cell lines | HL-60 cells |
Preparation Method | HL-60 cells were cultured in RPMI 1640 medium (containing 50ug/ml gentamycin) supplemented with 10% FBS at 37°C in humidified air with 5% CO2. Cells were sub-cultured twice a week. Cells in the exponential growth period were used in the experiment. The cells were replaced with fresh cells from frozen stocks of early passage every three months. To induce apoptosis, HL-60 cells at a concentration of 1.25×106/ml were treated with 100μM Ro 20-1724 in medium supplemented with 10% FBS for 1, 2, 3, 4, 5, and 6h, respectively. Each sample was assayed for cell viability with trypan blue stain. |
Reaction Conditions | 100μM; 1, 2, 3, 4, 5, and 6h |
Applications | Ro 20-1724 treatment promoted apoptosis of HL-60 cells within 5h. |
| Animal experiment [2]: | |
Animal models | Male Balb/c mice |
Preparation Method | Male Balb/c mice (6 weeks old, weight 20-25g) were provided with standard laboratory diet and tap water ad libitum and were maintained on a 12-h light/dark cycle at appropriate humidity and temperature. Mice were sensitized by intraperitoneal injection of 50μg ovalbumin (OVA) and 1mg aluminum hydroxide dissolved in 0.5ml sterile saline (0.9% sodium chloride) at an interval of 12 days (days 0 and 12). At 10, 14, and 18 days after the last immunization (days 22, 26, and 30), an aerosol of OVA formed by 1% (wt/v) OVA dissolved in sterile saline was sprayed into the mice for 30min using an ultrasonic nebulizer. In the control group, only sterile saline was sprayed into the mice by aerosol. Ro 20-1724 and sildenafil were dissolved in sterile saline containing 0.1% (v/v) Tween 20 and administered separately. During the last ten days of the sensitization regimen (days 20 to 30), all drugs were administered daily by oral gavage, with a final dose of 3mg/kg body weight. Finally, mouse samples were collected for analysis. |
Dosage form | 3mg/kg/day for 10 days; p.o. |
Applications | Ro 20-1724 treatment reduced leukocyte numbers and alleviated bronchial inflammation in mice. |
References: | |
| Cas No. | 29925-17-5 | SDF | |
| 别名 | 4-(3-丁氧基-4-甲氧基苯基)咪唑啶-2-酮,4-(3-Butoxy-4-methoxybenzyl)-2-imidazolidinone | ||
| 化学名 | (S)-4-(3-butoxy-4-methoxybenzyl)imidazolidin-2-one | ||
| Canonical SMILES | O=C(NC1)N[C@H]1CC(C=C2OCCCC)=CC=C2OC | ||
| 分子式 | C15H22N2O3 | 分子量 | 278.35 |
| 溶解度 | 25 mg/mL in DMSO, 30 mg/mL in DMF, 25 mg/mL in Ethanol | 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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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.5926 mL | 17.963 mL | 35.926 mL |
| 5 mM | 0.7185 mL | 3.5926 mL | 7.1852 mL |
| 10 mM | 0.3593 mL | 1.7963 mL | 3.5926 mL |
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动物平均体重 | g | |
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动物数量 | 只 |
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