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/ Vardenafil HCl Trihydrate/伐地那非盐酸盐水合物

Vardenafil HCl Trihydrate/伐地那非盐酸盐水合物 {[allProObj[0].p_purity_real_show]}

货号：A194638 同义名： 盐酸瓦地那非三水合物 / Vardenafil(hydrochloride hydrate); BAY38-9456

Vardenafil HCl Trihydrate是一种PDE抑制剂，IC50分别为0.7 nM（对PDE5）和180 nM（对PDE1）。

Vardenafil HCl Trihydrate/伐地那非盐酸盐水合物 化学结构 CAS号：330808-88-3
Vardenafil HCl Trihydrate/伐地那非盐酸盐水合物 化学结构
CAS号：330808-88-3
Vardenafil HCl Trihydrate/伐地那非盐酸盐水合物 3D分子结构
CAS号：330808-88-3
Vardenafil HCl Trihydrate/伐地那非盐酸盐水合物 化学结构 CAS号：330808-88-3
Vardenafil HCl Trihydrate/伐地那非盐酸盐水合物 3D分子结构 CAS号：330808-88-3
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Vardenafil HCl Trihydrate/伐地那非盐酸盐水合物 纯度/质量文件 产品仅供科研

货号：A194638 标准纯度： {[allProObj[0].p_purity_real_show]}
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产品名称 PDE ↓ PDE1 ↓ PDE10A ↓ PDE2 ↓ PDE3 ↓ PDE4 ↓ PDE5 ↓ PDE6 ↓ 其他靶点 纯度
Doxofylline ✔ 99+%
Deltarasin +++

PDEδ , Kd: 38 nM

 		95%
7-(2,3-Dihydroxypropyl)theophylline ✔ 98%
Aminophylline +

PDE, IC50: 0.12 mM

 		98+%
Anagrelide HCl ✔ 99%+
Irsogladine ✔ AChR,mAChR 99%
PF-8380 +++

Autotaxin, IC50: 2.8 nM

 		99%+
Dipyridamole ✔ 98%
Balipodect ++++

PDE10A, IC50: 0.3 nM

 		99%+
Luteolin +

PDE1, Ki: 15.0 μM

 		++

PDE2, Ki: 6.4 μM

 		+

PDE3, Ki: 13.9 μM

 		+

PDE4, Ki: 11.1 μM

 		+

PDE5, Ki: 9.5 μM

 		98%
Milrinone ++

PDE2, IC50: 5.2 μM

 		++

PDE3, IC50: 2.1 μM

 		ATPase 99%
Pimobendan ++

PDE3, IC50: 0.32 μM

 		98%
Cilostazol ++

PDE3, IC50: 0.2 μM

 		98%
Fenspiride HCl +

PDE3, pIC50: 3.44

 		+

PDE4, pIC50: 4.16

 		99% (HPLC)
(S)-(+)-Rolipram ++

PDE4, IC50: 0.75 μM

 		99% (HPLC)
Apremilast +++

PDE4, IC50: 74 nM

 		98%
GSK256066 ++++

PDE4B, IC50: 3.2 pM

 		98+%
Roflumilast ++++

PDE4A1, IC50: 0.7 nM

PDE4A4, IC50: 4.3 nM

 		99%
Rolipram +++

PDE4B, IC50: 130 nM

 		99%+
Cilomilast +++

LPDE4, IC50: 100 nM

HPDE4, IC50: 120 nM

 		99%
Avanafil ++++

PDE5, IC50: 1 nM

 		98%
Vardenafil HCl Trihydrate ++++

PDE5, IC50: 0.7 nM

 		98%
Tadalafil ++++

PDE5, IC50: 1.8 nM

 		98%
Icariin ++

PDE5, IC50: 0.432 μM

 		98%
Sildenafil ✔ +++

PDE6, IC50: 33 nM

 		98%
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。

Vardenafil HCl Trihydrate/伐地那非盐酸盐水合物 生物活性

靶点

  • PDE5

    PDE5, IC50:0.7 nM
描述 Phosphodiesterase-5 (PDE5) is 1 of 11 mammalian PDE families known to date. PDE5 is a cGMP-specific PDE and is abundant in most smooth muscle tissues as well as in platelets, gastrointestinal epithelial cells, and Purkinje cells of the cerebellum[3]. Vardenafil specifically inhibits the hydrolysis of cGMP by PDE5 with an IC50 of 0.7 nM. In contrast, the IC50 of vardenafil for PDE1 is 180 nM; for PDE6, 11 nM; for PDE2, PDE3 and PDE4, more than 1000 nM[4]. Vardenafil significantly enhanced the sodium nitroprusside (SNP)-induced relaxation of human trabecular smooth muscle at 3 nM. It also significantly potentiated both ACh-induced and transmural electrical stimulation-induced relaxation of trabecular smooth muscle[4]. In vivo studies in rabbits showed that orally administered vardenafil dose-dependently potentiated erectile responses to intravenously administered SNP. The minimal effective dose that significantly potentiated erection was 0.1 mg/kg. The selectivity for PDE5, the potentiation of NO-induced relaxation and cGMP accumulation in human trabecular smooth muscle and the ability to enhance NO-induced erection in vivo indicated that vardenafil had the appropriate properties to be a potential compound for the treatment of erectile dysfunction[4]. Rats treated with vardenafil showed an improved object discrimination performance. Compared with sildenafil, vardenafil appeared to be even more potent in this respect since it already produced a high discrimination performance at a dose of 0.3 mg/kg[5].

Vardenafil HCl Trihydrate/伐地那非盐酸盐水合物 细胞实验

Cell Line
Concentration Treated Time Description References
Human T84 colonic epithelial cells 30 µM 1 h To assess ST activity by measuring the induction of cGMP. Cells. 2023 Feb 10;12(4):567.
Normal esophageal fibroblasts (NOFs) 50 µM 72 h TGF-β1-treated NOFs expressed higher α-SMA, and Vardenafil pretreatment abrogated the TGF-β1-induced expression of α-SMA. Cell Rep Med. 2022 Jun 21;3(6):100541.
Cancer-associated fibroblasts (CAFs) 50 µM 72 h Vardenafil-treated CAFs showed a 50% reduction in α-SMA expression by Western blot and immunocytochemistry. Cell Rep Med. 2022 Jun 21;3(6):100541.
Human T84 colonic epithelial cells 30 µM 1 h To assess ST activity, T84 cells were pre-incubated with Vardenafil and Zardaverine, then treated with purified toxins or ETEC isolate supernatants for 2 h before cell lysis and cGMP measurement Cells. 2023 Feb 10;12(4):567.

Vardenafil HCl Trihydrate/伐地那非盐酸盐水合物 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Mice Patient-derived xenograft (PDX) model of esophageal adenocarcinoma Oral 16 mg/kg Twice daily for 5 days Vardenafil in combination with chemotherapy significantly reduced tumor volume and suppressed markers of CAF differentiation. Cell Rep Med. 2022 Jun 21;3(6):100541.
Mice F508del-CFTR mutant mice Intraperitoneal injection 0.14 mg/kg Single dose Vardenafil restores chloride transport across the nasal mucosa in F508del-CFTR mutant mice and attenuates lung inflammation by reducing cell infiltrates and pro-inflammatory cytokine expression. Front Pharmacol. 2012 Sep 18;3:167
Rats Zucker diabetic fatty (ZDF) rats Oral 10 mg/kg Once daily from 7 weeks to 32 weeks of age Vardenafil effectively prevented the development of diabetes-associated heart failure with preserved ejection fraction (HFpEF) by maintaining diastolic function, restoring cGMP levels and PKG activation, lowering apoptosis, and alleviating nitro-oxidative stress, myocardial hypertrophy, and fibrotic remodeling. Eur J Heart Fail. 2017 Mar;19(3):326-336

Vardenafil HCl Trihydrate/伐地那非盐酸盐水合物 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01063855 Erectile Dysfunction ... 展开 >> Sexual Dysfunction 收起 << Phase 3 Completed - -
NCT01063855 - Completed - -
NCT00767598 Pharmacokinetics of Three PDE5... 展开 >>Is Healthy Subjects Genetic Polymorphic CYP3A5 收起 << Phase 1 Completed - -

Vardenafil HCl Trihydrate/伐地那非盐酸盐水合物 参考文献

[1]Blount MA, Beasley A, et al. Binding of tritiated sildenafil, tadalafil, or vardenafil to the phosphodiesterase-5 catalytic site displays potency, specificity, heterogeneity, and cGMP stimulation. Mol Pharmacol. 2004 Jul;66(1):144-52.

[2]Prickaerts J, van Staveren WC, et al. Effects of two selective phosphodiesterase type 5 inhibitors, sildenafil and vardenafil, on object recognition memory and hippocampal cyclic GMP levels in the rat. Neuroscience. 2002;113(2):351-61.

[3]Blount MA, Beasley A, Zoraghi R, Sekhar KR, Bessay EP, Francis SH, Corbin JD. Binding of tritiated sildenafil, tadalafil, or vardenafil to the phosphodiesterase-5 catalytic site displays potency, specificity, heterogeneity, and cGMP stimulation. Mol Pharmacol. 2004 Jul;66(1):144-52. doi: 10.1124/mol.66.1.144. PMID: 15213306.

[4]Saenz de Tejada I, Angulo J, Cuevas P, Fernández A, Moncada I, Allona A, Lledó E, Körschen HG, Niewöhner U, Haning H, Pages E, Bischoff E. The phosphodiesterase inhibitory selectivity and the in vitro and in vivo potency of the new PDE5 inhibitor vardenafil. Int J Impot Res. 2001 Oct;13(5):282-90. doi: 10.1038/sj.ijir.3900726. PMID: 11890515.

[5]Prickaerts J, van Staveren WC, Sik A, Markerink-van Ittersum M, Niewöhner U, van der Staay FJ, Blokland A, de Vente J. Effects of two selective phosphodiesterase type 5 inhibitors, sildenafil and vardenafil, on object recognition memory and hippocampal cyclic GMP levels in the rat. Neuroscience. 2002;113(2):351-61. doi: 10.1016/s0306-4522(02)00199-9. PMID: 12127092.

Vardenafil HCl Trihydrate/伐地那非盐酸盐水合物 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.73mL

0.35mL

0.17mL

8.63mL

1.73mL

0.86mL

17.27mL

3.45mL

1.73mL

Vardenafil HCl Trihydrate/伐地那非盐酸盐水合物 技术信息

CAS号330808-88-3
分子式C23H39ClN6O7S
分子量 579.11
SMILES Code O=C1N=C(C2=CC(S(=O)(N3CCN(CC)CC3)=O)=CC=C2OCC)NN4C1=C(C)N=C4CCC.[H]Cl.[H]O[H].[H]O[H].[H]O[H]
MDL No. MFCD08458876
别名 盐酸瓦地那非三水合物 ;Vardenafil(hydrochloride hydrate); BAY38-9456; Vivanza; Staxyn; Levitra; Vardenafil HCl; Vardenafil hydrochloride trihydrate
运输蓝冰
InChI Key FBCDRHDULQYRTB-UHFFFAOYSA-N
Pubchem ID 135413545
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Inert atmosphere, room temperature

Tags: Vardenafil HCl Trihydrate | Vardenafil (hydrochloride hydrate);BAY38-9456;Vivanza;Staxyn;Levitra;Vardenafil HCl;Vardenafil HCl Trihydrate | 盐酸瓦地那非三水合物 | Phosphodiesterase Inhibitor | PDE | AmBeed-信号通路专用抑制剂 | Vardenafil HCl Trihydrate/伐地那非盐酸盐水合物 纯度/质量文件 | Vardenafil HCl Trihydrate/伐地那非盐酸盐水合物 亚型比较 | Vardenafil HCl Trihydrate/伐地那非盐酸盐水合物 生物活性 | Vardenafil HCl Trihydrate/伐地那非盐酸盐水合物 临床数据 | Vardenafil HCl Trihydrate/伐地那非盐酸盐水合物 参考文献 | Vardenafil HCl Trihydrate/伐地那非盐酸盐水合物 实验方案 | Vardenafil HCl Trihydrate/伐地那非盐酸盐水合物 技术信息

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