Tadalafil

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Cat.No. 6311 - Tadalafil | C22H19N3O4 | CAS No. 171596-29-5
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)
Datasheet
Citations
Literature

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.

Select a batch to recalculate based on the batch molecular weight:
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

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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


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