NVS1.1 | eRF1 inhibitor | Probechem Biochemicals

Chemical Structure : NVS1.1

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NVS1.1 (eRF1 inhibitor)

货号: PC-21294Not For Human Use, Lab Use Only.

NVS1.1 is a potent readthrough promoter, promotes the rapid and specific degradation of eukaryotic release factor 1 (eRF1) and restores functional full-length proteins in cystic fibrosis and Hurler disease models.

规格	价格	库存	数量
50 mg		Get quote
100 mg		Get quote
200 mg		Get quote

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生物&药学活性

NVS1.1 is a potent readthrough promoter, promotes the rapid and specific degradation of eukaryotic release factor 1 (eRF1) and restores functional full-length proteins in cystic fibrosis and Hurler disease models.
NVS1.1 restores α-L-iduronidase (IDUA) enzyme activity and reduces the GAG levels in a dose-dependent manner in human patient-derived fibroblasts.
NVS1.1 stimulates premature termination codon (PTC) suppression by triggering rapid proteasomal degradation of the translation termination factor eRF1.
NVS1.1 blocks translation termination by trapping eRF1 in the A site, causing ribosome collisions.
NVS1.1 is efficacious in a rat Hurler IDUA-W401X animal model, shows good drug-like properties with favorable pharmacokinetics, metabolic stability, and suitability for oral administration.

物理化学性质&存储条件

分子量	361.84
分子式	C17H16ClN3O2S
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(R)-(2-chloro-5-(methylsulfonyl)-4-(1H-pyrazol-5-yl)phenyl)(phenyl)methanamine

参考文献

1. Gurzeler LA, et al. Cell Rep. 2023 Sep 26;42(9):113056.

2. Patent WO2014/091446A1