Avanafil dibenzenesulfonate

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CAS NO:

330784-48-0

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。

生物活性

Avanafil (TA-1790) dibenzenesulfonate is a potent and selectivephosphodiesterase-5 (PDE-5)inhibitor withIC₅₀values 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].

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].

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

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.