Thiorphan

Thiorphan is a selective neprilysin (NEP) inhibitor with an IC50 of 6.9 nM. Thiorphan competitively binds to NEP and blocks its activity, preventing the degradation of neuropeptides such as substance P (SP) and neurokinin NKA. In the field of neonatal brain injury research, Thiorphan can increase the levels of SP and NKA, activate NK1 and NK2 receptors and downstream transduction pathways, and inhibit excessive activation of NMDA receptors. Thus, Thiorphan can protect neocortical neurons from excitotoxic cell death. Thiorphan may also inhibit NEP from enhancing bronchoconstriction and can be used in the study of respiratory diseases[1][2][3].

Product Specifications

CAS Number

[76721-89-6]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Neprilysin

Type

Reference compound

Related Pathways

Metabolic Enzyme/Protease

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/thiorphan.html

Purity

99.94

Solubility

DMSO : 175 mg/mL (ultrasonic)

Smiles

SCC(C(NCC(O)=O)=O)CC1=CC=CC=C1

Molecular Formula

C12H15NO3S

Molecular Weight

253.32

Precautions

H302, H315, H319, H335

References & Citations

[1]Whyteside AR, et al. Human neprilysin-2 (NEP2) and NEP display distinct subcellular localisations and substrate preferences. FEBS Lett. 2008 Jul 9;582 (16) :2382-6.|[2]Cheung D, et al. The effect of an inhaled neutral endopeptidase inhibitor, thiorphan, on airway responses to neurokinin A in normal humans in vivo. Am Rev Respir Dis. 1992 Jun;145 (6) :1275-80.|[3]Medja F, et al. Thiorphan, a neutral endopeptidase inhibitor used for diarrhoea, is neuroprotective in newborn mice. Brain. 2006 Dec;129 (Pt 12) :3209-23.