76721-89-6
Chemical Structure
Thiorphan
- CAS No.: 76721-89-6
- Formula:C12H15NO3S
- Molecular Weight:253.32
IUPAC Name: (2-benzyl-3-mercaptopropanoyl)glycine
InChIKey: LJJKNPQAGWVLDQ-UHFFFAOYSA-N
SMILES: SCC(C(NCC(O)=O)=O)CC1=CC=CC=C1
Biological Activity: 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].
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Thiorphan | 99.94% | 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. | ||||||||||||||||||||
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Thiorphan-d7 | Thiorphan-d7 is the deuterium labeled Thiorphan. Thiorphan is a selective NEP (neprilysin) inhibitor with an IC50 of 6.9 nM. | |||||||||||||||||||||
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- [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. [Content Brief]
- [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. [Content Brief]
- [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. [Content Brief]
Keywords
