2. Metabolic Enzyme/Protease
    Immunology/Inflammation
  3. Phosphodiesterase (PDE)
    NO Synthase
    Endogenous Metabolite
  4. Avanafil

Avanafil  (Synonyms: TA1790)

Cat. No.: HY-18252 Purity: ≥98.0%
COA Handling Instructions

Avanafil (TA-1790) 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 activates NO/cGMP/PKG signaling-pathway to decrease loss in BMD, bone atrophy, and oxidative stress. Avanafil inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Avanafil can be used for the research of erectile dysfunction and osteoporosis.

For research use only. We do not sell to patients.

Avanafil Chemical Structure

Avanafil Chemical Structure

CAS No. : 330784-47-9

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10 mM * 1 mL in DMSO USD 87 In-stock
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100 mg USD 125 In-stock
500 mg USD 185 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Avanafil:

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Avanafil

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Avanafil (TA-1790) 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 activates NO/cGMP/PKG signaling-pathway to decrease loss in BMD, bone atrophy, and oxidative stress. Avanafil inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Avanafil 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)

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[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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[1].
Avanafil (TA-1790) (10 µM; ICI; once, for 10 weeks) improves erectile responses in T2DM rats[2].

MCE 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
Molecular Weight

483.95

Appearance

Solid

Formula

C23H26ClN7O3
CAS No.
SMILES

COC1=C(Cl)C=C(CNC2=C(C(NCC3=NC=CC=N3)=O)C=NC(N4[[email protected]](CO)CCC4)=N2)C=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (103.32 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0663 mL 10.3316 mL 20.6633 mL
5 mM 0.4133 mL 2.0663 mL 4.1327 mL
10 mM 0.2066 mL 1.0332 mL 2.0663 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.17 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (5.17 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.17 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Keywords:

Avanafil330784-47-9TA1790TA 1790TA-1790Phosphodiesterase (PDE)NO SynthaseEndogenous MetaboliteNitric oxide synthasesNOSbone densitydexamethasoneosteoporosiserectile dysfunctioncorpus cavernosumInhibitorinhibitorinhibit

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