Avanafil dibenzenesulfonate (Synonyms: TA1790 dibenzenesulfonate)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白、同位素标记物,专注于信号通路和疾病研究领域。
Avanafil dibenzenesulfonate  (Synonyms: TA1790 dibenzenesulfonate)

Avanafil (TA-1790) dibenzenesulfonate 是一种有效的选择性磷酸二酯酶-5 (PDE-5) 抑制剂,抑制 PDE-5、PDE-6、PDE-4、PDE-10、PDE-8、PDE-7、PDE-2 和 PDE-1 的 IC50 值分别为 5.2 nM、630 nM、5700 nM、6200 nM、12000 nM、27000 nM、51000 nM 和 53000 nM。Avanafil dibenzenesulfonate 激活 NO/cGMP/PKG 信号通路,减少骨密度损失,骨萎缩和氧化应激。Avanafil dibenzenesulfonate 抑制环单磷酸鸟苷 (cGMP) 水解,从而提高 cGMP 水平。Avanafil dibenzenesulfonate 可用于勃起功能障碍和骨质疏松的研究。

Avanafil dibenzenesulfonate                                          (Synonyms: TA1790 dibenzenesulfonate)

Avanafil dibenzenesulfonate Chemical Structure

CAS No. : 330784-48-0

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Avanafil dibenzenesulfonate 的其他形式现货产品:

Avanafil

Avanafil dibenzenesulfonate 相关产品

同靶点产品:

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生物活性

Avanafil (TA-1790) dibenzenesulfonate is a potent and selective phosphodiesterase-5 (PDE-5) inhibitor with IC50 values of 5.2 nM, 630 nM, 5700 nM, 6200 nM, 12000 nM, 27000 nM, 51000 nM and 53000 nM for PDE-5, PDE-6, PDE-4, PDE-10, PDE-8, PDE-7, PDE-2 and PDE-1, respectively. Avanafil dibenzenesulfonate activates NO/cGMP/PKG signaling-pathway to decrease loss in BMD, bone atrophy, and oxidative stress. Avanafil dibenzenesulfonate inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Avanafil dibenzenesulfonate can be used for the research of erectile dysfunction and osteoporosis[1][2][3].

IC50 & Target[3]

PDE5

5.2 nM (IC50)

PDE6

630 nM (IC50)

PDE4

5700 nM (IC50)

PDE10

6200 nM (IC50)

PDE7

27000 nM (IC50)

PDE2

51000 nM (IC50)

PDE1

53000 nM (IC50)

体外研究
(In Vitro)

Avanafil (TA-1790) dibenzenesulfonate (0.01-1000 µM) enhances by 45% for electrical field stimulation (1-20 Hz)-induced relaxation responses in corpus cavernosum strips from the diabetic group[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Avanafil dibenzenesulfonate 相关抗体:

体内研究
(In Vivo)

Avanafil (TA-1790) dibenzenesulfonate (10 mg/kg; p.o.; daily, for 30 d; male rat) increases angiogenesis in bone tissue via the activation of NO, cGMP and PKG (NO/cGMP/PKG) signaling-pathway and significantly decreases dexamethasone-induced loss in BMD, bone atrophy, and oxidative stress[1].
Avanafil (TA-1790) dibenzenesulfonate (10 µM; ICI; once, for 10 weeks) improves erectile responses in T2DM rats[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male rat model of glucocorticoid-induced osteoporosis (GIOP)[1]
Dosage: 10 mg/kg
Administration: Oral administration; daily, for 30 days
Result: Decreased the level of eNOS, NO, PDE-5, PICP, MDA, CoQ10/CoQ10H and 8-OHdG/108dG. Increased the level of cGMP, PKG, Cortisol and CTCP.
Animal Model: Male rat model of glucocorticoid-induced osteoporosis (GIOP)[1]
Dosage: 10 mg/kg
Administration: Oral administration; daily, for 30 days
Result: Increased right femur trabecular bone thickness and epiphyseal bone width.
Animal Model: Male T2DM Sprague Dawley rats[2]
Dosage: 10 µM
Administration: Intracavernous injection; once, for 10 weeks
Result: Increased in ICP/MAP in response to nerve stimulation and increased total ICP values.

Clinical Trial

分子量

800.30

Formula

C35H38ClN7O9S2

CAS 号

330784-48-0

结构分类
  • Others
初始来源
  • 内源性代谢物
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
Data Sheet (544 KB) 产品使用指南 (1538 KB)

参考文献
  • [1]. Huyut Z, et, al. Effects of the Phosphodiesterase-5 (PDE-5) Inhibitors, Avanafil and Zaprinast, on Bone Remodeling and Oxidative Damage in a Rat Model of Glucocorticoid-Induced Osteoporosis. Med Sci Monit Basic Res. 2018 Mar 13;24:47-58.  [Content Brief]

    [2]. Yilmaz D, et, al. The effect of intracavernosal avanafil, a newer phosphodiesterase-5 inhibitor, on neonatal type 2 diabetic rats with erectile dysfunction. Urology. 2014 Feb;83(2):508.e7-12.  [Content Brief]

    [3]. Kotera J, et, al. Avanafil, a potent and highly selective phosphodiesterase-5 inhibitor for erectile dysfunction. J Urol. 2012 Aug;188(2):668-74.  [Content Brief]

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