Thiorphan

• Description:

  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].

• 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.

• Shipping Conditions:

  Blue Ice

• Storage Conditions:

  -20°C (Powder, protect from light)

• Scientific Category:

  Reference compound1

• Clinical Information:

  No Development Reported

• CAS Number:

  [76721-89-6]