Avanafil

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Avanafil (TA-1790) 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 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 抑制环单磷酸鸟苷 (cGMP) 水解，从而提高 cGMP 水平。

A potent and highly selective PDE5 inhibitor (IC50=5.2 nM) for erectile dysfunction; shows no significant effect on PDE1, PDE6 and PDE11.Sexual Dysfunction Approved(In Vitro):Avanafil (TA-1790) (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.(In Vivo):Avanafil (TA-1790) (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) (10 μM; ICI; once, for 10 weeks) improves erectile responses in T2DM rats.

Avanafil (TA-1790) (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.

Avanafil (TA-1790) (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) (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.

TA1790 | TA 1790 | TA-1790

Angiogenesis

PDE

PDE5

Endocrinology

Sexual Dysfunction

330784-47-9

483.9507

C23H26ClN7O3

>98% (HPLC)

10 mM in DMSO

O=C(C1=CN=C(N2[C@H](CO)CCC2)N=C1NCC3=CC=C(OC)C(Cl)=C3)NCC4=NC=CC=N4

5-Pyrimidinecarboxamide, 4-[[(3-chloro-4-methoxyphenyl)methyl]amino]-2-[(2S)-2-(hydroxymethyl)-1-pyrrolidinyl]-N-(2-pyrimidinylmethyl)-

(-20℃)

With Ice Pack

≥ 2 years