Biological Activity
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.
Technical Data
| 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.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 38.94 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 389.4. Batch specific molecular weights may vary from batch to batch due to solvent 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
References
References are publications that support the products' biological activity.
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
Keywords: Tadalafil, supplier, phosphodiesterase, 5, PDE5, potent, highly, selective, inhibitors, inhibits, antihypertensive, anticancer, orally, bioavailable, GF196960, Phosphodiesterases, Tocris Bioscience
