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                同义名:
                    
                        
                            米诺地尔
                            
                             / U10858; Loniten
                            
                        
                    
                
                
                
                    
                     
                
            
Minoxidil是一种是 ATP 敏感的钾通道 (KATP) 开放剂,是有效的口服降压药,可促进血管扩张,减缓或停止脱发,并促进头发再生。Minoxidil 还是一种大豆脂氧合酶的有效抑制剂,其 IC50 值为 20 μM。
 
                                 
                                
                            

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| 产品名称 | Potassium Channel ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Tolbutamide | ✔ | 98% | |||||||||||||||||
| Glimepiride | ++++ SUR2B, IC50: 7.3 nM SUR1, IC50: 5.4 nM | 97% | |||||||||||||||||
| Dronedarone HCl | ✔ | 95% | |||||||||||||||||
| Gliquidone | ++ Potassium channel, IC50: 27.2 nM | 99% | |||||||||||||||||
| TRAM-34 | +++ IKCa1 (KCa3.1), Kd: 20 nM | 98% | |||||||||||||||||
| Glibenclamide | ✔ | 98% | |||||||||||||||||
| Amiodarone HCl | ✔ | 97% | |||||||||||||||||
| Gliclazide | ++ Potassium channel, IC50: 184 nM | 98% | |||||||||||||||||
| Repaglinide | ✔ | 98% | |||||||||||||||||
| Dofetilide | ✔ | 98% | |||||||||||||||||
| Nateglinide | ✔ | 99% | |||||||||||||||||
| Quinine HCl dihydrate | ✔ | 98% | |||||||||||||||||
| ML133 HCl | + Kir2.1, IC50: 290 nM | 99% | |||||||||||||||||
| 1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 | |||||||||||||||||||
| 描述 | Minoxidil (U10858) is an ATP-sensitive potassium (KATP) channel opener, a potent oral antihypertensive agent and a peripheral vasodilator that promotes vasodilation also affects hair growth. Minoxidil is also a potent inhibitor of soybean lipoxygenaseare with an IC50 of 20 μM. Minoxidil (0.01 mmoL/kg body weight; intraperitoneal injection; for 3.5 hours; fisher 344 rats) treatment inhibits carrageenan-induced rat paw oedema with an inhibitory potency (49%)[3]. Minoxidil induces generalized hypertrichosis when administered systemically, or localized hair regrowth when applied topically to sites of severe alopecia areata. In the presence of minoxidil, cultures showed a marked dose-dependent second peak of DNA synthesis 8-10 days after culture initiation in epidermal cells. In addition, two morphologically distinct cell types appeared[4]. Minoxidil is a potassium channel opener, causing hyperpolarization of cell membranes and it is also a vasodilator, by widening blood vessels and opening potassium channels, it allows more oxygen, blood and nutrients to the follicle. This can also cause follicles in the telogen phase to shed, usually soon to be replaced by new, thicker hairs in a new anagen phase. The most common adverse reactions of the topical formulation are limited to irritant and allergic contact dermatitis on the scalp[5]. | 
| Concentration | Treated Time | Description | References | |
| Human dermal papilla cells (HDPCs) | 0.0002 | 48 hours | Evaluate the effect of HL@Mi/NONOate on the proliferation of HDPCs. Results showed that the cell proliferation rate in the HL@Mi/NONOate group was 161.90%, significantly higher than the HL@Mi group (103.63%) and the control group. | Bioact Mater. 2023 Oct 11;32:190-205 | 
| Human Umbilical Vein Endothelial Cells (HUVECs) | 0.0002 | 48 hours | Evaluate the effect of HL@Mi/NONOate on the proliferation of HUVECs. Results showed that the cell proliferation rate in the HL@Mi/NONOate group was 153.77%, significantly higher than the HL@Mi group (115.18%) and the control group. | Bioact Mater. 2023 Oct 11;32:190-205 | 
| human dermal papilla cells (DPCs) | 0.5, 1, 2 mM | 4 hours | To investigate the induction of HIF-1α protein by minoxidil, results showed that 2 mM minoxidil significantly induced HIF-1α protein expression. | Int J Mol Sci. 2017 Dec 25;19(1):53 | 
| human keratinocytes (HaCaT cells) | 0.5, 1, 2 mM | 4 hours | To investigate the induction of HIF-1α protein by minoxidil, results showed that 2 mM minoxidil significantly induced HIF-1α protein expression. | Int J Mol Sci. 2017 Dec 25;19(1):53 | 
| Adipose-derived stem cells (ASCs) | 20 and 50 µM | 2 days and 7 days | Minoxidil did not alter ASC proliferation but increased migration and tube formation | Int J Mol Sci. 2018 Feb 28;19(3):691 | 
| Caco-2 cells | 80 µg/mL (382 µM) | 120 minutes | Evaluate the permeability of minoxidil across Caco-2 cell monolayers, showing that tight junction modifiers (quercetin and sodium decanoate) significantly affect its permeability. | Pharmaceutics. 2022 Jun 27;14(7):1360 | 
| Administration | Dosage | Frequency | Description | References | ||
| C57BL/6 mice | Androgenetic alopecia (AGA) model | Topical application | 5% Minoxidil | Once daily for 28 days | Compare the hair regeneration effects of V-R-MN and Minoxidil in AGA model mice, with the V-R-MN group showing faster hair regeneration onset and improved hair quality. | Bioact Mater. 2024 Apr 23;38:95-108 | 
| Wistar rats | Single-pass intestinal perfusion model | Intestinal perfusion | 80 µg/mL (382 µM) | 1 hour perfusion followed by an additional 1 hour of perfusion, sampling every 10 minutes | Evaluate the permeability of minoxidil in different intestinal segments, showing that tight junction modifiers significantly affect its permeability. | Pharmaceutics. 2022 Jun 27;14(7):1360 | 
| Rat | Skin permeation model | Topical application | 300 μg | Single dose, observed for 24 hours | Evaluate the skin permeation efficiency of HA-PLGA/MXD NPs, showing higher permeation efficiency of HA-PLGA NPs compared to PLGA NPs | Biomater Res. 2019 Oct 31;23:16 | 
| ICR mice | Topical application | 5% | Single application, lasting 4 hours | To investigate the effect of minoxidil on VEGF and HIF-1α levels in the skin, results showed that minoxidil significantly elevated VEGF and HIF-1α levels in mouse skins. | Int J Mol Sci. 2017 Dec 25;19(1):53 | 
| NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 | 
| NCT00283686 | Kidney, Polycystic | Phase 3 | Completed | - | United States, Colorado ... 展开 >> University of Colorado Health Sciences Center Denver (Aurora), Colorado, United States, 800045 United States, Georgia Emory University School of Medicine Atlanta, Georgia, United States, 30322 United States, Kansas University of Kansas Medical Center Kansas City, Kansas, United States, 66160 United States, Massachusetts Tufts University-New England Medical Center Boston, Massachusetts, United States, 02111 Beth Israel Deaconess Medical Center Boston, Massachusetts, United States, 02215 United States, Minnesota Mayo Clinic Rochester, Minnesota, United States, 55905 United States, Ohio Cleveland Clinic Foundation Cleveland, Ohio, United States, 44195 收起 << | 
| NCT00283686 | - | Completed | - | - | |
| NCT01227031 | - | Unknown | July 2011 | Taiwan ... 展开 >> Taipei Medical University-Wan Fang Hospital Not yet recruiting Taipei, Taiwan Contact: Ren-Yu Tsai 886-2-29307930 ext 2980 b671022@tmu.edu.tw 收起 << | |
| 计算器 | ||||
| 存储液制备 |  | 1mg | 5mg | 10mg | 
| 1 mM 5 mM 10 mM | 4.78mL 0.96mL 0.48mL | 23.89mL 4.78mL 2.39mL | 47.79mL 9.56mL 4.78mL | |
| CAS号 | 38304-91-5 | 
| 分子式 | C9H15N5O | 
| 分子量 | 209.25 | 
| SMILES Code | NC1=NC(N2CCCCC2)=CC(N)=[N+]1[O-] | 
| MDL No. | MFCD00063409 | 
| 别名 | 米诺地尔 ;U10858; Loniten; Minoxidil, Loniten, Rogaine, U 10858 | 
| 运输 | 蓝冰 | 
| InChI Key | ZIMGGGWCDYVHOY-UHFFFAOYSA-N | 
| Pubchem ID | 4201 | 
| 存储条件 | In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Keep in dark place, inert atmosphere, room temperature | 
| 溶解方案 | DMSO: 10 mg/mL(47.79 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO H2O: 1 mg/mL(4.78 mM),配合低频超声,并水浴加热至45℃助溶 无水乙醇: 7 mg/mL(33.45 mM),配合低频超声助溶,注意:无水乙醇开封后,易挥发,也会吸收空气中的水分,导致溶解能力下降,请避免使用开封较久的乙醇 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶 
 
 
 
 
 
 
 
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