产品
编 号:F757524
分子式:C35H38ClN7O9S2
分子量:800.3
产品类型
结构图
CAS No: 330784-48-0
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产品详情
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.
体内研究:
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.Avanafil (TA-1790) dibenzenesulfonate (10 μM; ICI; once, for 10 weeks) improves erectile responses in T2DM rats.Animal Model:Male rat model of glucocorticoid-induced osteoporosis (GIOP)
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)
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
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.
体外研究:
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.