Thiorphan

General Information

Thiorphan Impurities and Thiorphan 

Daicel Pharma offers superior quality Thiorphan impurities, such as S-Methylthiorphan and S-Methylthiorphan S-Oxide. It is vital for evaluating Thiorphan quality, stability, and biological safety. Furthermore, Daicel Pharma specializes in the custom synthesis of Thiorphan impurities and ensures their worldwide delivery.

Thiorphan [CAS: 76721-89-6] is an N-acyl amino acid. It is a metabolite of Racecadotril. It inhibits enzymes, neutral endopeptidase (NEP) and enkephalin-degrading enzymes (enkephalinases). Thiorphan helps treat acute diarrhea in adults and infants. In addition, it regulates the cardiovascular system. Thiorphan has neuroprotective properties against excitotoxic damage.

Thiorphan: Use and Commercial Availability  

Thiorphan is an active metabolite of the drug- Racecadotril, an antidiarrheal agent. It is effective in morphine-induced analgesia. Thiorphan prevents the degradation of the opioid peptide enkephalin, which regulates pain sensation (nociception). Further, Thiorphan acts as an NEP inhibitor and helps lower blood pressure. Racecadotril, also known as Acetorphan, is administered orally to patients.

Thiorphan Structure and Mechanism of Action

The chemical name of Thiorphan is N-[2-(Mercaptomethyl)-1-oxo-3-phenylpropyl]glycine. The chemical formula for Thiorphan is C12H15NO3S, and its molecular weight is approximately 253.32 g/mol.

As a Neprilysin (NEP) enzyme inhibitor, Thiorphan can break down biologically active natriuretic peptides (NPs). These peptides are responsible for maintaining sodium and fluid balance in cardiac homeostasis.

Thiorphan Impurities and Synthesis

Impurities may form during the synthesis of Thiorphan 1, which affects drug safety and efficacy. These impurities form during the synthesis, storage, or degradation of Thiorphan. So, Thiorphan impurities must be controlled and monitored throughout the drug’s lifecycle.

Daicel Pharma offers a comprehensive Certificate of Analysis (CoA) for Thiorphan impurities, which includes S-Methylthiorphan and S-Methylthiorphan S-Oxide. The issued CoA is from a cGMP-compliant analytical facility. It contains characterization data such as 1H NMR, 13C NMR, IR, MASS, and HPLC purity2. We give additional spectral data on request. Daicel Pharma can prepare any unidentified Thiorphan impurity or degradation product. In addition, Daicel Pharma offers highly purified deuterium-labeled standards of Thiorphan-D5 for bioanalytical research and BA/BE studies. We also provide a complete characterization report on delivery.