ARUK3001185 | Notum inhibitor | Probechem Biochemicals

Chemical Structure : ARUK3001185

CAS No.: 2411969-39-4

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ARUK3001185 (ARUK 3001185)

货号: PC-72827Not For Human Use, Lab Use Only.

ARUK3001185 is a potent, selective, brain-penetrant inhibitor of Wnt-deactivating enzyme Notum carboxylesterase activity with IC50 of 6.7 nM in OPTS biochemical assay.

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10 mg	￥2780	In stock
25 mg	￥4580	In stock
50 mg	￥7280	In stock
100 mg		Get quote

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生物&药学活性

ARUK3001185 is a potent, selective, brain-penetrant inhibitor of Wnt-deactivating enzyme Notum carboxylesterase activity with IC50 of 6.7 nM in OPTS biochemical assay.

ARUK3001185 restored Wnt signaling in the presence of Notum (EC50 110 nM) in a in a cell-based TCF/LEF (Luciferase) reporter assay.

ARUK3001185 demonstrated high selectivity against a panel of serine hydrolases, kinases, and representative drug targets.

ARUK3001185 displayed good brain penetration suitable for oral dosing in rodent models of disease.

物理化学性质&存储条件

分子量	282.047
分子式	C9H4Cl2F3N3
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	1-(2,4-dichloro-3-(trifluoromethyl)phenyl)-1H-1,2,3-triazole

参考文献

1. William Mahy, et al. J Med Chem. 2020 Nov 12;63(21):12942-12956.

2. Elliott D Bayle, et al. J Med Chem. 2021 Apr 22;64(8):4289-4311.

3. Zhao Y, et al. Future Med Chem. 2021 Jun;13(11):1001-1015.

4. University of Oxford: WO2020043866 (2020).

ARUK3001185 (ARUK 3001185)

生物&药学活性

物理化学性质&存储条件

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ARUK3001185 (ARUK 3001185)

生物&药学活性

物理化学性质&存储条件

参考文献

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