bs-76861C

DATASHEET

Formulation Powder

Storage: Stable for 2 years after receipt when stored at -20°C.

Product Information:

CAS Number: 171596-29-5

Molecular formula: C22H19N3O4

Molecular weight: 389.4

Purity: >98%

Appearance: White to beige powder.

Solubility: Soluble in DMSO (20mg/ml) or DMF (25mg/ml).

InChiKey: WOXKDUGGOYFFRN-IIBYNOLFSA-N

SMILES: [H][C@@]12N(C(CN(C)C2=O)=O)[C@H](C3=CC=C(OCO4)C4=C3)C5=C(C(C=CC=C6)=C6N5)C1

SMILES: [H][C@]12CC3=C(NC4=C3C=CC=C4)[C@H](N1C(=O)CN(C)C2=O)C1=CC=C2OCOC2=C1

Description:

Tadalafil is a potent long-acting and selective inhibitor of the cGMP specific phosphodiesterase 5 (PDE5; IC50 = 1.2 nM). It is selective for PDE5 over PDE1-4 and 7-10 (IC50s = 9.2-280 µM), however, it does also inhibit PDE11 (IC50 = 11 nM). In vivo, tadalafil (10 mg/kg) decreases production of the proinflammatory cytokines TNF-alpha, IL-1beta, and IL-6 and improves renal function in a rat model of ischemia/reperfusion injury. Formulations containing tadalafil have been used to treat erectile dysfunction, pulmonary arterial hypertension, benign prostatic hyperplasia (BPH) and lower urinary tract dysfunction. Also delays tumor growth in a mouse model via inhibition of MDSC-mediated immunosuppression.