Avanafil

SKU: orb1225285

Description

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.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 330784-47-9
• MW: 483.9507
• Purity: >98% (HPLC)
• Formula: C₂₃H₂₆ClN₇O₃
• SMILES: O=C(C1=CN=C(N2[C@H](CO)CCC2)N=C1NCC3=CC=C(OC)C(Cl)=C3)NCC4=NC=CC=N4
• Target: PDE
• Solubility: 10 mM in DMSO

Bioactivity

• 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. 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.
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• 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.
  Read more...

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

TA1790 | TA 1790 | TA-1790

Quick Database Links

Gene Symbol

PDE