Phosphoramidon (CAS 119942-99-3)

5.0(1)

备用名: Phosphoramidon sodium salt;N-(α-Rhamnopyranosyloxyhydroxyphosphinyl)-Leu-Trp disodium salt;N-(α-Rhamnopyranosylphosphono)-L-leucyl-L-tryptophan disodium salt

应用； Phosphoramidon is an inhibitor of NEP 24.11 and NEP2

CAS号码: 119942-99-3

纯度: ≥97%

分子量: 587.47

分子式: C₂₃H₃₂N₃O₁₀P•₂Na

仅供科研使用。不可用于诊断或治疗。

* 参考分析证明大量特定数据 (包括水含量).

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Phosphoramidon is an inhibitor of CD10 (neutral endopeptidase 24.11, NEP), metalloproteases (MMPs), and Neprilysin-2 (NEP2), which belong to a group of type II integral membrane glycoproteins. In addtion, the NEP enzyme has been shown to play a role in the regulation of neuropeptide signaling and in the metabolism of bioactive peptides via plasma membranes. NEP2 is a homologue of NEP with a high degree of sequence identity, however, research shows that they have different physiological actions. Studies show that phosphoramidon and thiorphan (sc-201287), another NEP inhibitor, can increase nitrile production. Additionally, LNCaP cell studies show that phosphoramidon can inhibit the metabolism of neurotensin (NT). Phosphoramidon is an inhibitor of endothelial converting enzyme (ECE).

参考文献

1. Hiranuma, T., et al. 1997. J. Pharmacol. Exp. Ther. 281: 769-774. PMID: 9152384
2. Zhang, X., et al. 1998. J. Cardiovasc. Pharmacol. 31: 623-629. PMID: 9554814
3. Moody, T.W., et al. 1998. Peptides. 19: 253-258. PMID: 9493857
4. Rose, C., et al. 2002. Biochem. J. 363: 697-705. PMID: 11964170
5. Whyteside, A.R., et al. 2008. FEBS Lett. 582: 2382-2386. PMID: 18539150

物理状态 :

Solid

溶解度 :

Soluble in water (1 mM), DMSO, and methanol. Insoluble in benzene, hexane, and chloroform.

保存 :

Store at -20° C

IC50 :

endothelin-converting enzyme (EC₅₀E): IC₅₀ = 0.68 µM

Ki 数据 :

neutral endopeptidase 24.11 (NEP, neprilysin; EC 3.4.24.11): K_i= 2 nM; neprilysin 2: K_i= ~2 nM

仅供科研使用。不可用于诊断或治疗。

德国水公害等级 :

PubChem CID :

16219931

MDL 号码 :

MFCD00077870

EC号码 :

252-996-3

Beilstein 注册 :

8105669

SMILES :

C[[email protected]]1[[email protected]@H]([[email protected]]([[email protected]]([[email protected]@H](O1)OP(=O)(N[[email protected]@H](CC(C)C)C(=O)N[[email protected]@H](CC2=CNC3=CC=CC=C32)C(=O)[O-])[O-])O)O)O.[Na+].[Na+]

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