Referencia número: HY-18252

Avanafil

(Synonyms: TA1790)

1 Cited Publications

Revisión del cliente

Based on 1 publication(s) in Google Scholar

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.

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Pureza: 98.00%
No. CAS: 330784-47-9
Fòrmula: C₂₃H₂₆ClN₇O₃
Peso molecular:483.95

Almacenamiento:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Avanafil Chemical Structure

No. CAS: 330784-47-9

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Actividad biológica
- Descripciòn
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Ensayo clínico
Chemical Information
Publications (1)
Solvente y solubilidad
- In Vitro
- In Vivo
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

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)

Ver todos los productos específicos de isoformas NO Synthase :

Ver todos los productos específicos de isoformas Endogenous Metabolite :

Ver todos los productos específicos de isoformas Phosphodiesterase (PDE) :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	12.3 μM Compound: Avanafil	Potentiation of cisplatin-induced cytotoxicity against human A549 cells assessed as cisplatin IC50 at 1:7 ratio of cisplatin to compound measured after 48 hrs by MTT assay Potentiation of cisplatin-induced cytotoxicity against human A549 cells assessed as cisplatin IC50 at 1:7 ratio of cisplatin to compound measured after 48 hrs by MTT assay	[PMID: 39149110]
A549	IC₅₀	127.3 μM Compound: Avanafil	Antiproliferative activity against human A549 cells measured after 24 hrs by MTT assay Antiproliferative activity against human A549 cells measured after 24 hrs by MTT assay	[PMID: 39149110]
A549	IC₅₀	131.2 μM Compound: Avanafil	Antiproliferative activity against human A549 cells measured after 72 hrs by MTT assay Antiproliferative activity against human A549 cells measured after 72 hrs by MTT assay	[PMID: 39149110]
A549	IC₅₀	170.5 μM Compound: Avanafil	Antiproliferative activity against human A549 cells measured after 48 hrs by MTT assay Antiproliferative activity against human A549 cells measured after 48 hrs by MTT assay	[PMID: 39149110]
A549	IC₅₀	23.3 μM Compound: Avanafil	Potentiation of raloxifene-induced cytotoxicity against human A549 cells assessed as raloxifene IC50 at 1:4 ratio of raloxifene to compound measured after 48 hrs by MTT assay Potentiation of raloxifene-induced cytotoxicity against human A549 cells assessed as raloxifene IC50 at 1:4 ratio of raloxifene to compound measured after 48 hrs by MTT assay	[PMID: 39149110]
NCI-H1299	IC₅₀	15 μM Compound: Avanafil	Potentiation of raloxifene-induced cytotoxicity against human NCI-H1299 cells assessed as raloxifene IC50 at 1:5 ratio of raloxifene to compound measured after 48 hrs by MTT assay Potentiation of raloxifene-induced cytotoxicity against human NCI-H1299 cells assessed as raloxifene IC50 at 1:5 ratio of raloxifene to compound measured after 48 hrs by MTT assay	[PMID: 39149110]
NCI-H1299	IC₅₀	161.6 μM Compound: Avanafil	Antiproliferative activity against human NCI-H1299 cells measured after 24 hrs by MTT assay Antiproliferative activity against human NCI-H1299 cells measured after 24 hrs by MTT assay	[PMID: 39149110]
NCI-H1299	IC₅₀	169.1 μM Compound: Avanafil	Antiproliferative activity against human NCI-H1299 cells measured after 72 hrs by MTT assay Antiproliferative activity against human NCI-H1299 cells measured after 72 hrs by MTT assay	[PMID: 39149110]
NCI-H1299	IC₅₀	184.4 μM Compound: Avanafil	Antiproliferative activity against human NCI-H1299 cells measured after 48 hrs by MTT assay Antiproliferative activity against human NCI-H1299 cells measured after 48 hrs by MTT assay	[PMID: 39149110]
NCI-H1299	IC₅₀	7.1 μM Compound: Avanafil	Potentiation of cisplatin-induced cytotoxicity against human NCI-H1299 cells assessed as cisplatin IC50 at 1:9 ratio of cisplatin to compound measured after 48 hrs by MTT assay Potentiation of cisplatin-induced cytotoxicity against human NCI-H1299 cells assessed as cisplatin IC50 at 1:9 ratio of cisplatin to compound measured after 48 hrs by MTT assay	[PMID: 39149110]
NCI-H661	IC₅₀	16.4 μM Compound: Avanafil	Potentiation of raloxifene-induced cytotoxicity against human NCI-H661 cells assessed as raloxifene IC50 at 1:5 ratio of raloxifene to compound measured after 48 hrs by MTT assay Potentiation of raloxifene-induced cytotoxicity against human NCI-H661 cells assessed as raloxifene IC50 at 1:5 ratio of raloxifene to compound measured after 48 hrs by MTT assay	[PMID: 39149110]
NCI-H661	IC₅₀	186.2 μM Compound: Avanafil	Antiproliferative activity against human NCI-H661 cells measured after 48 hrs by MTT assay Antiproliferative activity against human NCI-H661 cells measured after 48 hrs by MTT assay	[PMID: 39149110]
NCI-H661	IC₅₀	264 μM Compound: Avanafil	Antiproliferative activity against human NCI-H661 cells measured after 24 hrs by MTT assay Antiproliferative activity against human NCI-H661 cells measured after 24 hrs by MTT assay	[PMID: 39149110]
NCI-H661	IC₅₀	78.52 μM Compound: Avanafil	Antiproliferative activity against human NCI-H661 cells measured after 72 hrs by MTT assay Antiproliferative activity against human NCI-H661 cells measured after 72 hrs by MTT assay	[PMID: 39149110]
NCI-H661	IC₅₀	8.2 μM Compound: Avanafil	Potentiation of cisplatin-induced cytotoxicity against human NCI-H661 cells assessed as cisplatin IC50 at 1:9 ratio of cisplatin to compound measured after 48 hrs by MTT assay Potentiation of cisplatin-induced cytotoxicity against human NCI-H661 cells assessed as cisplatin IC50 at 1:9 ratio of cisplatin to compound measured after 48 hrs by MTT assay	[PMID: 39149110]

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].

MedChemExpress (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].

MedChemExpress (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.

Ensayo clínico

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

No. CAS 330784-47-9
Appearance Solid
Peso molecular 483.95
Fòrmula C₂₃H₂₆ClN₇O₃
Color White to off-white
SMILES

COC1=C(Cl)C=C(CNC2=C(C(NCC3=NC=CC=N3)=O)C=NC(N4[C@H](CO)CCC4)=N2)C=C1
Synonyms

TA1790
Structure Classification
- Others
Initial Source
- Endogenous metabolite
Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (1)

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Chemrxiv

2021, Jun 10.

Solvente y solubilidad

In Vitro:

DMSO : 14.29 mg/mL (29.53 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Calculadora de molaridad

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (282 KB)
SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instrucciones de manejo (2659 KB)

Referencias

[1]. Huyut Z, et, al. Effects of the Phosphodiesterase-5 (PDE-5) Inhibitors, Avanafil and Zaprinast, on Bone Remodeling and Oxidative Damage in a Rat Model of Glucocorticoid-Induced Osteoporosis. Med Sci Monit Basic Res. 2018 Mar 13;24:47-58. [Content Brief]

[2]. Yilmaz D, et, al. The effect of intracavernosal avanafil, a newer phosphodiesterase-5 inhibitor, on neonatal type 2 diabetic rats with erectile dysfunction. Urology. 2014 Feb;83(2):508.e7-12. [Content Brief]

[3]. Kotera J, et, al. Avanafil, a potent and highly selective phosphodiesterase-5 inhibitor for erectile dysfunction. J Urol. 2012 Aug;188(2):668-74. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.0663 mL	10.3316 mL	20.6633 mL	51.6582 mL
	5 mM	0.4133 mL	2.0663 mL	4.1327 mL	10.3316 mL
	10 mM	0.2066 mL	1.0332 mL	2.0663 mL	5.1658 mL
	15 mM	0.1378 mL	0.6888 mL	1.3776 mL	3.4439 mL
	20 mM	0.1033 mL	0.5166 mL	1.0332 mL	2.5829 mL
	25 mM	0.0827 mL	0.4133 mL	0.8265 mL	2.0663 mL

Keywords

Avanafil

1 Cited Publications

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Avanafil

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Publications Citing Use of MedChemExpress (MCE) Avanafil

Ver todos los productos específicos de isoformas NO Synthase

Ver todos los productos específicos de isoformas Endogenous Metabolite

Ver todos los productos específicos de isoformas Phosphodiesterase (PDE)

Actividad biológica

Chemical Information

Publications (1)

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

Avanafil Related Classifications

HY-18252 Related Classifications