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Description: Potent and highly selective PDE5 inhibitor; orally bioavailable
Alternative Names: GF196960
Chemical Name: (6R,12aR)-6-(1,3-Benzodioxol-5-yl)-2,3,6,7,12,12a-hexahydro-2-methylpyrazino[1',2':1,6]pyrido[3,4-b]indole-1,4-dione
Purity: ≥99% (HPLC)
Biological Activity for Tadalafil
Tadalafil is a potent and highly selective PDE5 inhibitor (IC50 = 5 nM). Exhibits > 2000-fold selectivity for PDE5 over PDEs 1,2,3 and 4 and 1000-fold selectivity over PDE6. Reduces blood pressure in hypertensive rats. Also delays tumor growth in a mouse model via inhibition of MDSC-mediated immunosuppression. Orally bioavailable.
Compound Libraries for Tadalafil
Tadalafil is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen FDA-Approved Drugs. Find out more about compound libraries available from Tocris.
Technical Data for Tadalafil
| M. Wt | 389.4 |
| Formula | C22H19N3O4 |
| Storage | Store at -20°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 171596-29-5 |
| PubChem ID | 110635 |
| InChI Key | WOXKDUGGOYFFRN-IIBYNOLFSA-N |
| Smiles | [H][C@]12CC3=C([C@@H](C4=CC5=C(C=C4)OCO5)N1C(CN(C2=O)C)=O)NC6=CC=CC=C36 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for Tadalafil
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 38.94 | 100 |
Preparing Stock Solutions for Tadalafil
The following data is based on the product molecular weight 389.4. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.57 mL | 12.84 mL | 25.68 mL |
| 5 mM | 0.51 mL | 2.57 mL | 5.14 mL |
| 10 mM | 0.26 mL | 1.28 mL | 2.57 mL |
| 50 mM | 0.05 mL | 0.26 mL | 0.51 mL |
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Product Datasheets for Tadalafil
References for Tadalafil
References are publications that support the biological activity of the product.
Daugan et al (2003) The discovery of tadalafil: a novel and highly selective PDE5 inhibitor. 2: 2,3,6,7,12,12a-hexahydropyrazino[1',2':1,6]pyrido[3,4-b]indole-1,4-dione analogues. J.Med.Chem. 46 4533 PMID: 14521415
Serafini et al (2006) Phosphodiesterase-5 inhibition augments endogenous antitumor immunity by reducing myeloid-derived suppressor cell function. J.Exp.Med. 203 2691 PMID: 17101732
If you know of a relevant reference for Tadalafil, please let us know.
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Keywords: Tadalafil, Tadalafil supplier, phosphodiesterase, 5, PDE5, potent, highly, selective, inhibitors, inhibits, antihypertensive, anticancer, orally, bioavailable, GF196960, Phosphodiesterases, 6311, Tocris Bioscience
Citations for Tadalafil
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