Tadalafil (Synonyms: IC-351)

Name: Tadalafil
Brand: MedChemExpress
SKU: HY-90009A
Rating: 5.0 (8 reviews)

Cat. No.: HY-90009A Purity: 99.95%: Data Sheet
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Tadalafil (IC-351) is a PDE5 inhibitor with an IC₅₀ value of 1.8 nM.

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

CAS No. : 171596-29-5

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
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5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
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Based on 8 publication(s) in Google Scholar

Other Forms of Tadalafil:

8 Publications Citing Use of MCE Tadalafil

Cell Proliferation/Viability Assay

RT-PCR

In Vivo Efficacy Study

IHC

: Tadalafil purchased from MedChemExpress. Usage Cited in: Cancer Metab. 2022 Dec 6;10(1):22. [Abstract]; Tadalafil (TAD; 10, 20, 50 µM) for 24 h was evaluated by MTT assay.

: Tadalafil purchased from MedChemExpress. Usage Cited in: Cancer Metab. 2022 Dec 6;10(1):22. [Abstract]; Fold change relative to control of glycolytic enzymes in HCT116 cells treated with or without Tadalafil (TAD; 25 µM) for 24 h.

: Tadalafil purchased from MedChemExpress. Usage Cited in: Cancer Metab. 2022 Dec 6;10(1):22. [Abstract]; Tumor volume and mass of nude mice were remarkably reduced after administrated with Tadalafil (2 mg/kg, p.o.) and 5-FU combination.

: Tadalafil purchased from MedChemExpress. Usage Cited in: Cancer Metab. 2022 Dec 6;10(1):22. [Abstract]; Western blotting analysis to assess LDHA levels in tumor samples treated with 5-FU and Tadalafil (2 mg/kg, p.o.) (TAD).

: Tadalafil purchased from MedChemExpress. Usage Cited in: Cancer Metab. 2022 Dec 6;10(1):22. [Abstract]; IHC staining showed that the expression of LDHA was significantly declined in combination of Tadalafil (2 mg/kg, p.o.) with 5-FU.

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Biological Activity
Purity & Documentation
References
Customer Review

Description

Tadalafil (IC-351) is a PDE5 inhibitor with an IC₅₀ value of 1.8 nM.

IC₅₀ & Target

PDE5

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	105.5 μM Compound: Tadalafil	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	12.2 μM Compound: Tadalafil	Potentiation of cisplatin-induced cytotoxicity against human A549 cells assessed as cisplatin IC50 at 1:4 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 1:4 ratio of cisplatin to compound measured after 48 hrs by MTT assay	[PMID: 39149110]
A549	IC₅₀	23.5 μM Compound: Tadalafil	Potentiation of raloxifene-induced cytotoxicity against human A549 cells assessed as raloxifene IC50 at 1:2 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 1:2 ratio of raloxifene to compound measured after 48 hrs by MTT assay	[PMID: 39149110]
A549	IC₅₀	353.7 μM Compound: Tadalafil	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	73.9 μM Compound: Tadalafil	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]
HT-29	IC₅₀	> 100 μM Compound: Tadalafil	Growth inhibition of human HT-29 cells after 72 hrs by cell titer glo assay Growth inhibition of human HT-29 cells after 72 hrs by cell titer glo assay	[PMID: 20206015]
MRC5	CC₅₀	> 64 μM Compound: 1	Cytotoxicity against human MRC5 SV2 cells after 72 hrs using resazurin by fluorimetry Cytotoxicity against human MRC5 SV2 cells after 72 hrs using resazurin by fluorimetry	[PMID: 22204607]
MRC5	IC₅₀	> 64 μM Compound: 1	Cytotoxicity against human MRC5 SV2 cells after 72 hrs Cytotoxicity against human MRC5 SV2 cells after 72 hrs	[PMID: 21504142]
NCI-H1299	IC₅₀	127.3 μM Compound: Tadalafil	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	274 μM Compound: Tadalafil	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	358.8 μM Compound: Tadalafil	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	7.8 μM Compound: Tadalafil	Potentiation of cisplatin-induced cytotoxicity against human NCI-H1299 cells assessed as cisplatin IC50 at 1:35 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 1:35 ratio of cisplatin to compound measured after 48 hrs by MTT assay	[PMID: 39149110]
NCI-H1299	IC₅₀	8.6 μM Compound: Tadalafil	Potentiation of raloxifene-induced cytotoxicity against human NCI-H1299 cells assessed as raloxifene IC50 at 1:20 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 1:20 ratio of raloxifene to compound measured after 48 hrs by MTT assay	[PMID: 39149110]
NCI-H661	IC₅₀	21 μM Compound: Tadalafil	Potentiation of raloxifene-induced cytotoxicity against human NCI-H661 cells assessed as raloxifene IC50 at 1:7 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 1:7 ratio of raloxifene to compound measured after 48 hrs by MTT assay	[PMID: 39149110]
NCI-H661	IC₅₀	242.8 μM Compound: Tadalafil	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	280.9 μM Compound: Tadalafil	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	875.7 μM Compound: Tadalafil	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	9.9 μM Compound: Tadalafil	Potentiation of cisplatin-induced cytotoxicity against human NCI-H661 cells assessed as cisplatin IC50 at 1:14 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 1:14 ratio of cisplatin to compound measured after 48 hrs by MTT assay	[PMID: 39149110]
Sf9	IC₅₀	2.35 nM Compound: Tadalafil	Inhibition of N-terminal GST-tagged human PDE5A1 expressed in baculovirus infected sf9 cells using [3H]cGMP as substrate measured after 30 mins by scintillation proximity assay Inhibition of N-terminal GST-tagged human PDE5A1 expressed in baculovirus infected sf9 cells using [3H]cGMP as substrate measured after 30 mins by scintillation proximity assay	[PMID: 31021628]
Sf9	IC₅₀	22.1 nM Compound: Tadalafil	Inhibition of N-terminal GST-tagged human PDE11A4 expressed in baculovirus infected sf9 cells using [3H]cGMP as substrate measured after 30 mins by scintillation proximity assay Inhibition of N-terminal GST-tagged human PDE11A4 expressed in baculovirus infected sf9 cells using [3H]cGMP as substrate measured after 30 mins by scintillation proximity assay	[PMID: 31021628]
Sf9	IC₅₀	37 nM Compound: 2	Inhibitory activity against phosphodiesterase 11 (PDE11) obtained from recombinant Sf9 expression Inhibitory activity against phosphodiesterase 11 (PDE11) obtained from recombinant Sf9 expression	[PMID: 12668004]
Sf9	IC₅₀	402 nM Compound: Tadalafil	Inhibition of N-terminal GST-tagged human PDE6C expressed in baculovirus infected sf9 cells using [3H]cGMP as substrate measured after 30 mins by scintillation proximity assay Inhibition of N-terminal GST-tagged human PDE6C expressed in baculovirus infected sf9 cells using [3H]cGMP as substrate measured after 30 mins by scintillation proximity assay	[PMID: 31021628]
Sf9	IC₅₀	> 10000 nM Compound: Tadalafil	Inhibition of N-terminal GST-tagged full length human PDE8A1 expressed in baculovirus infected sf9 cells using [3H]cAMP as substrate measured after 30 mins by scintillation proximity assay Inhibition of N-terminal GST-tagged full length human PDE8A1 expressed in baculovirus infected sf9 cells using [3H]cAMP as substrate measured after 30 mins by scintillation proximity assay	[PMID: 31021628]
Sf9	IC₅₀	> 10000 nM Compound: Tadalafil	Inhibition of N-terminal GST-tagged full length human PDE9A2 expressed in baculovirus infected sf9 cells using [3H]cGMP as substrate measured after 30 mins by scintillation proximity assay Inhibition of N-terminal GST-tagged full length human PDE9A2 expressed in baculovirus infected sf9 cells using [3H]cGMP as substrate measured after 30 mins by scintillation proximity assay	[PMID: 31021628]
Sf9	IC₅₀	> 10000 nM Compound: Tadalafil	Inhibition of N-terminal GST-tagged human PDE1 expressed in baculovirus infected sf9 cells using [3H]cAMP as substrate measured after 30 mins by scintillation proximity assay Inhibition of N-terminal GST-tagged human PDE1 expressed in baculovirus infected sf9 cells using [3H]cAMP as substrate measured after 30 mins by scintillation proximity assay	[PMID: 31021628]
Sf9	IC₅₀	> 10000 nM Compound: Tadalafil	Inhibition of N-terminal GST-tagged human PDE10A expressed in baculovirus infected sf9 cells using [3H]cAMP as substrate measured after 30 mins by scintillation proximity assay Inhibition of N-terminal GST-tagged human PDE10A expressed in baculovirus infected sf9 cells using [3H]cAMP as substrate measured after 30 mins by scintillation proximity assay	[PMID: 31021628]
Sf9	IC₅₀	> 10000 nM Compound: Tadalafil	Inhibition of N-terminal GST-tagged human PDE3 expressed in baculovirus infected sf9 cells using [3H]cAMP as substrate measured after 30 mins by scintillation proximity assay Inhibition of N-terminal GST-tagged human PDE3 expressed in baculovirus infected sf9 cells using [3H]cAMP as substrate measured after 30 mins by scintillation proximity assay	[PMID: 31021628]
Sf9	IC₅₀	> 10000 nM Compound: Tadalafil	Inhibition of N-terminal GST-tagged human PDE4 expressed in baculovirus infected sf9 cells using [3H]cAMP as substrate measured after 30 mins by scintillation proximity assay Inhibition of N-terminal GST-tagged human PDE4 expressed in baculovirus infected sf9 cells using [3H]cAMP as substrate measured after 30 mins by scintillation proximity assay	[PMID: 31021628]
Sf9	IC₅₀	> 10000 nM Compound: Tadalafil	Inhibition of N-terminal GST-tagged human PDE7 expressed in baculovirus infected sf9 cells using [3H]cAMP as substrate measured after 30 mins by scintillation proximity assay Inhibition of N-terminal GST-tagged human PDE7 expressed in baculovirus infected sf9 cells using [3H]cAMP as substrate measured after 30 mins by scintillation proximity assay	[PMID: 31021628]
Sf9	IC₅₀	> 10000 nM Compound: Tadalafil	Inhibition of human PDE2A1 expressed in baculovirus infected sf9 cells using [3H]cAMP as substrate measured after 30 mins by scintillation proximity assay Inhibition of human PDE2A1 expressed in baculovirus infected sf9 cells using [3H]cAMP as substrate measured after 30 mins by scintillation proximity assay	[PMID: 31021628]

In Vitro

Biochemical potencies (affinities) of these compounds for PDE5 determined by IC(50), K(D) (isotherm), K(D) (dissociation rate), and K(D) ((1/2) EC(50)), respectively, were the following: sildenafil (3.7 +/- 1.4, 4.8 +/- 0.80, 3.7 +/- 0.29, and 11.7 +/- 0.70 nM), tadalafil (1.8 +/- 0.40, 2.4 +/- 0.60, 1.9 +/- 0.37, and 2.7 +/- 0.25 nM); and vardenafil (0.091 +/- 0.031, 0.38 +/- 0.07, 0.27 +/- 0.01, and 0.42 +/- 0.10 nM). Thus, absolute potency values were similar for each inhibitor, and relative potencies were vardenafil >> tadalafil > sildenafil^[1].
0.5 ml tadalafil solutions with different concentrations were added (0.2, 0.1, 0.05 and 0.025 μg ml-1, respectively) into semen samples. In both groups, samples treated with 0.2 μg ml-1 tadalafil had significant increase in sperm motility after 2 h incubation^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

The Tadalafil-treated group showed enhanced erectile function (intracavernosal pressure/mean arterial pressure) at 0.3, 0.5, 1, 3, and 5 Hz compared with diabetic group values at the respective frequencies that approached control values^[3].
Oral administration of tadalafil (20 mg) or sildenafil (100 mg) was given. In both groups, computer-assisted semen analysis parameters showed no significant difference. After the administration of tadalafil (2 h) and sildenafil (1 h), there was no significant difference observed in premature acrosome reaction incidence rate^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

Molecular Weight

389.40

Formula

C₂₂H₁₉N₃O₄

CAS No.

171596-29-5

Appearance

Solid

Color

White to off-white

SMILES

O=C([C@@]1([H])CC2=C([C@@H](C3=CC=C(OCO4)C4=C3)N15)NC6=C2C=CC=C6)N(C)CC5=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Solvent & Solubility

In Vitro:

DMSO : ≥ 52 mg/mL (133.54 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.5681 mL	12.8403 mL	25.6805 mL
5 mM	0.5136 mL	2.5681 mL	5.1361 mL
10 mM	0.2568 mL	1.2840 mL	2.5681 mL

View the Complete Stock Solution Preparation Table

* 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

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 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.42 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:

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

Please enter your animal formula composition:

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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.95%

Select Batch:

Data Sheet (285 KB) SDS (393 KB)

COA (263 KB) HNMR (288 KB) RP-HPLC (258 KB) MS (68 KB)

Handling Instructions (2659 KB)

References

[1]. Blount MA, et al. Binding of tritiated sildenafil, tadalafil, or vardenafil to the phosphodiesterase-5 catalytic site displays potency,specificity, heterogeneity, and cGMP stimulation. Mol Pharmacol. 2004 Jul;66(1):144-52. [Content Brief]

[2]. Yang Y, et al. Effect of acute tadalafil on sperm motility and acrosome reaction: in vitro and in vivo studies. Andrologia. 2013 Apr 14. [Epub ahead of print] [Content Brief]

[3]. Mostafa ME, et al. Effect of Chronic Low-dose Tadalafil on Penile Cavernous Tissues in Diabetic Rats. Urology. 2013 Jun;81(6):1253-60. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.5681 mL	12.8403 mL	25.6805 mL	64.2013 mL
	5 mM	0.5136 mL	2.5681 mL	5.1361 mL	12.8403 mL
	10 mM	0.2568 mL	1.2840 mL	2.5681 mL	6.4201 mL
	15 mM	0.1712 mL	0.8560 mL	1.7120 mL	4.2801 mL
	20 mM	0.1284 mL	0.6420 mL	1.2840 mL	3.2101 mL
	25 mM	0.1027 mL	0.5136 mL	1.0272 mL	2.5681 mL
	30 mM	0.0856 mL	0.4280 mL	0.8560 mL	2.1400 mL
	40 mM	0.0642 mL	0.3210 mL	0.6420 mL	1.6050 mL
	50 mM	0.0514 mL	0.2568 mL	0.5136 mL	1.2840 mL
	60 mM	0.0428 mL	0.2140 mL	0.4280 mL	1.0700 mL
	80 mM	0.0321 mL	0.1605 mL	0.3210 mL	0.8025 mL
	100 mM	0.0257 mL	0.1284 mL	0.2568 mL	0.6420 mL

Tadalafil Related Classifications

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.

Keywords:

Tadalafil171596-29-5IC-351IC351IC 351Phosphodiesterase (PDE)ApoptosisInhibitorinhibitorinhibit

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Tadalafil (Synonyms: IC-351)

Customer Review

Other Forms of Tadalafil:

Tadalafil Related Antibodies

8 Publications Citing Use of MCE Tadalafil

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Phosphodiesterase (PDE) Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Tadalafil Related Antibodies

Molarity Calculator

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Complete Stock Solution Preparation Table

Tadalafil Related Classifications

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