1276297-68-7
1276297-68-7
Chemical Structure
Thiorphan-d7
- CAS No.: 1276297-68-7
- Formula:C12H8D7NO3S
- Molecular Weight:260.36
IUPAC Name: (2-(mercaptomethyl)-3-(phenyl-d5)propanoyl-3,3-d2)glycine
InChIKey: LJJKNPQAGWVLDQ-XZJKGWKKSA-N
SMILES: OC(CNC(C(CS)C([2H])([2H])C1=C([2H])C([2H])=C([2H])C([2H])=C1[2H])=O)=O
Biological Activity: Thiorphan-d7 is the deuterium labeled Thiorphan[1]. Thiorphan is a selective NEP (neprilysin) inhibitor with an IC50 of 6.9 nM[2].
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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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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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References
- [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-216. [Content Brief]
- [2]. Whyteside AR, Turner AJ. Human neprilysin-2 (NEP2) and NEP display distinct subcellular localisations and substrate preferences. FEBS Lett. 2008 Jul 9;582(16):2382-6. [Content Brief]
Keywords
