Tadalafil
Based on 9 publication(s) in Google Scholar
Tadalafil (IC-351) is a PDE5 inhibitor with an IC50 value of 1.8 nM.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.95%
- CAS. Nr.: 171596-29-5
- Formel: C22H19N3O4
- Molecular Weight:389.40
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
Publications Citing Use of MedChemExpress (MCE) Tadalafil
More- Transl Psychiatry. 2024 Dec 18;14(1):494. [Abstract]
- Cancer Metab. 2022 Dec 6;10(1):22. [Abstract]
- Int J Mol Sci. 2022 Apr 27;23(9):4806. [Abstract]
- Biol Direct. 2024 Aug 2;19(1):61. [Abstract]
- Analyst. 2026 Jun 15;151(12):3550-3561. [Abstract]
- Biochem Biophys Res Commun. 2021 Apr 2:547:9-14. [Abstract]
- Biomed Pharmacother. 2025 Jun:187:118104. [Abstract]
- bioRxiv. 2024 Jun 1:2024.05.27.596052. [Abstract]
- Patent. US20210052581A1.
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Cell Proliferation/Viability Assay
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RT-PCR
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In Vivo Efficacy Study
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WB
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IHC
Biologische Aktivität
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PDE5 |
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Cell Line
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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
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[PMID: 39149110] |
| A549 | IC50 |
12.2 μM
Compound: Tadalafil
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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
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[PMID: 39149110] |
| A549 | IC50 |
23.5 μM
Compound: Tadalafil
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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
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[PMID: 39149110] |
| A549 | IC50 |
353.7 μM
Compound: Tadalafil
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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
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[PMID: 39149110] |
| A549 | IC50 |
73.9 μM
Compound: Tadalafil
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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
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[PMID: 39149110] |
| HT-29 | IC50 |
>100 μM
Compound: Tadalafil
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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
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[PMID: 20206015] |
| MRC5 | IC50 |
>64 μM
Compound: 1
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Cytotoxicity against human MRC5 SV2 cells after 72 hrs
Cytotoxicity against human MRC5 SV2 cells after 72 hrs
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[PMID: 21504142] |
| MRC5 | CC50 |
>64 μM
Compound: 1
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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
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[PMID: 22204607] |
| NCI-H1299 | IC50 |
127.3 μM
Compound: Tadalafil
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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
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[PMID: 39149110] |
| NCI-H1299 | IC50 |
274 μM
Compound: Tadalafil
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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
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[PMID: 39149110] |
| NCI-H1299 | IC50 |
358.8 μM
Compound: Tadalafil
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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
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[PMID: 39149110] |
| NCI-H1299 | IC50 |
7.8 μM
Compound: Tadalafil
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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
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[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
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[PMID: 39149110] |
| NCI-H661 | IC50 |
21 μM
Compound: Tadalafil
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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
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[PMID: 39149110] |
| NCI-H661 | IC50 |
242.8 μM
Compound: Tadalafil
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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
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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
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[PMID: 39149110] |
| NCI-H661 | IC50 |
875.7 μM
Compound: Tadalafil
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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
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[PMID: 39149110] |
| NCI-H661 | IC50 |
9.9 μM
Compound: Tadalafil
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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
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[PMID: 39149110] |
| Sf9 | IC50 |
37 nM
Compound: 2
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Inhibitory activity against phosphodiesterase 11 (PDE11) obtained from recombinant Sf9 expression
Inhibitory activity against phosphodiesterase 11 (PDE11) obtained from recombinant Sf9 expression
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[PMID: 12668004] |
| Sf9 | IC50 |
>10000 nM
Compound: Tadalafil
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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
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[PMID: 31021628] |
| Sf9 | IC50 |
>10000 nM
Compound: Tadalafil
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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
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[PMID: 31021628] |
| Sf9 | IC50 |
>10000 nM
Compound: Tadalafil
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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
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[PMID: 31021628] |
| Sf9 | IC50 |
>10000 nM
Compound: Tadalafil
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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
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[PMID: 31021628] |
| Sf9 | IC50 |
>10000 nM
Compound: Tadalafil
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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
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[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
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[PMID: 31021628] |
| 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
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[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
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[PMID: 31021628] |
| Sf9 | IC50 |
402 nM
Compound: Tadalafil
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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
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[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
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[PMID: 31021628] |
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.
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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 171596-29-5
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Appearance Solid
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Molecular Weight 389.40
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Formel C22H19N3O4
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Color White to off-white
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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
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Synonyms
IC-351
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months
Publications (9)
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Journal Impact Factor
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Most Recent
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Transl Psychiatry
Exploring PDE5A upregulation in bipolar disorder: insights from single-nucleus RNA sequencing of human basal ganglia. [Abstract]2024 Dec 18;14(1):494. PMID: 39695100 -
Cancer Metab
Tadalafil increases the antitumor activity of 5-FU through inhibiting PRMT5-mediated glycolysis and cell proliferation in colorectal cancer. [Abstract]2022 Dec 6;10(1):22. PMID: 36474242
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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Int J Mol Sci
Novel Chemicals Derived from Tadalafil Exhibit PRMT5 Inhibition and Promising Activities against Breast Cancer. [Abstract]2022 Apr 27;23(9):4806. PMID: 35563196 -
Biol Direct
Phosphodiesterase type 5 inhibitor tadalafil reduces prostatic fibrosis via MiR-3126-3p/FGF9 axis in benign prostatic hyperplasia. [Abstract]2024 Aug 2;19(1):61. PMID: 39095835 -
Analyst
Evaluation of vardenafil's metabolic stability in human liver microsomes through ultra-fast UPLC-MS/MS for quantitative analysis, including assessments of greenness, ADME properties, DEREK alerts, and metabolic lability. [Abstract]2026 Jun 15;151(12):3550-3561. PMID: 42132584 -
Biochem Biophys Res Commun
2021 Apr 2:547:9-14. PMID: 33588236 -
Biomed Pharmacother
Drug repositioning: Identification of potent inhibitors of NS3 protease and NS5 RdRp for control of DENV infection. [Abstract]2025 Jun:187:118104. PMID: 40300391 -
bioRxiv
Exploring Integrin α5β1 as a Potential Therapeutic Target for Pulmonary Arterial Hypertension: Insights from Comprehensive Multicenter Preclinical Studies. [Abstract]2024 Jun 1:2024.05.27.596052. PMID: 38854025 -
Lösungsmittel & Löslichkeit
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.
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.
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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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.
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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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Reinheit & Dokumentation
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Data Sheet (284 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
Verweise
[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
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.
| 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 |