Tadalafil
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Tadalafil也被称为IC351或Cialis，是磷酸二酯酶5（PDE5）的强效的、可逆的和竞争性的小分子抑制剂，PDE5是肺血管中主要的PDE形式，可以水解环磷酸鸟苷（cGMP），参与肺动脉高压（PAH）的病理性过程。Tadalafil的抑制作用是PDE5特异性的，选择性作用于PDE5，比对PDE1、PDE4、PDE7、PDE8、PDE9和PDE10的选择性大10000倍，比PDE6的大780倍。通过口服给药用于治疗勃起功能障碍，在肺血管中，Tadalafil通过抑制PDE5，增加cGMP的水平，改善PAH的血管收缩。
参考文献：
Fusae Sawamura, Masami Kato, Kazushisa Fujita, Takahiro Nakazawa and Anthony Bearsworth. Tadalafil, a long-acting inhibitor of PDE5, improves pulmonary hemodynamics and survival rate of monocrotaline-induced pulmonary artery hypertension in rats. J Pharmacol Sci111, 235-243 (2009)
H Porst. IC351 (tadalafil, Cialis): update on clinical experience. Internation Journal of Impotence Research (2002) 14, Suppl 1, S57-S64
S. Thomas Forgue, Beverley E. Patterson, Alun W. Bedding, Christopher D. Payne, Diane L. Phillips, Rebecca E. Wrishko and Malcolm I. Mitchell. Tadalafil pharmacokinetics in healthy subjects. Br J Clin Pharmacol (2005); 61(3): 280-288
| Storage | Store at -20°C |
| M.Wt | 389.4 |
| Cas No. | 171596-29-5 |
| Formula | C22H19N3O4 |
| Synonyms | Cialis,ICOS 351,Ic351,IC 351,IC-351 |
| Solubility | insoluble in H2O; insoluble in EtOH; ≥16.6 mg/mL in DMSO |
| Chemical Name | (6R,12aR)-6-(benzo[d][1,3]dioxol-5-yl)-2-methyl-2,3,12,12a-tetrahydropyrazino[1',2':1,6]pyrido[3,4-b]indole-1,4(6H,7H)-dione |
| SDF | Download SDF |
| Canonical SMILES | O=C1N(C)CC(N([C@@H]2C(C=C3)=CC4=C3OCO4)[C@]1([H])CC5=C2NC6=CC=CC=C56)=O |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
| 细胞实验 [1]: | |
|
细胞系 |
人肝细胞 |
|
溶解方法 |
该化合物在DMSO中的溶解度大于16.6mg/mL。若获取更高浓度的溶液，可在37℃下孵育10分钟，随后在超声波浴中摇匀。-20℃以下可储存数月。 |
|
反应条件 |
1 μM |
|
应用 |
Tadalafil (1 μM)提高了人肝细胞中CYP3A蛋白的表达。 |
| 动物实验 [2,3]: | |
|
动物模型 |
双侧海绵状神经切断术（BCN）诱导阴茎损伤和低氧合的大鼠模型，海绵体神经切除小鼠 |
|
给药剂量 |
2 mg/kg，每天给药，持续三周 |
|
应用 |
在假手术大鼠的阴茎切片中，Tadalafil (2 mg/kg)几乎完全恢复了阴茎氧合，并且消除了神经切断术诱发的增加，显著挽救了肌肉/纤维的比例。Tadalafil减少凋亡细胞的数量，并增加小鼠中2种存活相关激酶Akt和细胞外信号调节激酶1/2的磷酸化。 |
|
注意事项 |
由于实验环境的不同，实际溶解度可能与理论值略有不同，请测试室内所有化合物的溶解度。 |
|
References: [1]. Ring B J, Patterson B E, Mitchell M I, et al. Effect of tadalafil on cytochrome P450 3A4–mediated clearance: studies in vitro and in vivo[J]. Clinical Pharmacology & Therapeutics, 2005, 77(1): 63-75. [2]. Morelli A, Vignozzi V, Filippi S, et al. Effect of Chronic Tadalafil Administration on Penile Hypoxia Induced by Cavernous Neurotomy in the Rat[J]. The Journal of Sexual Medicine, 2006, 3: 46. [3]. Lysiak J J, Yang S K, Klausner A P, et al. Tadalafil increases Akt and extracellular signal-regulated kinase 1/2 activation, and prevents apoptotic cell death in the penis following denervation[J]. The Journal of urology, 2008, 179(2): 779-785. | |
质量控制和MSDS
- 批次:
化学结构
