理化性质和储存条件
| Molecular Weight (MW) | 348.41 |
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| Formula | C20H20N4O2 |
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| CAS No. | 2009273-60-1 (GNE-6776) |
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| Storage | -20℃ for 3 years in powder form |
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| -80℃ for 2 years in solvent |
| Solubility (In vitro) | DMSO: ≥ 300 mg/mL |
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| Water: N/A |
| Ethanol: N/A |
| Chemical Name | 6'-Amino-4'-ethyl-5'-(4-hydroxyphenyl)-N-methyl-[3,3'-bipyridine]-6-carboxamide |
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| Synonyms | GNE-6776; GNE 6776; GNE6776 |
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| SMILES Code | O=C(C1=CC=C(C2=C(CC)C(C3=CC=C(O)C=C3)=C(N)N=C2)C=N1)NC |
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实验参考方法
GNE-6776 HCl (GNE6776), the hydrochloride salt of GNE-6776 which is an analog of GNE-6640, is a novel potent and selective inhibitor of USP7 (ubiquitin-specific protease-7) with potential anticancer activity.
| In Vitro |
GNE-131 (Compound 13) shows moderate clearance in human liver
microsomes and excellent functional activity against human NaV1.7 with
an IC50 of 0.003±0.001 μM. GNE-131 shows excellent potency, good in
vitro metabolic stability[1].
|
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| In Vivo |
GNE-131 shows low in vivo clearance in mouse, rat, and dog.
GNE-131 also displays excellent efficacy in a transgenic mouse model of
induced pain[1].
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| References |
[1]. Design of Conformationally Constrained Acyl Sulfonamide
Isosteres: Identification of N-([1,2,4]Triazolo[4,3-
a]pyridin-3-yl)methane-sulfonamides as Potent and Selective hNaV1.7
Inhibitors for the Treatment of Pain. J Med Chem. 2018 Jun
14;61(11):4810-4831 |
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