中文名 | SAG |
英文名 | SAG |
别名 | SMO RECEPTOR激动剂(SAG) 3-氯-N-[反式-4-(甲基氨基)环己基]-N-[[3-(4-吡啶基)苯基]甲基]-苯并[B]噻吩-2-甲酰胺 |
英文别名 | SAG CS-1655 SAG (Smo agonist) SAG (cyclopamine antagonist) Smoothened Agonist (SAG) free base 3-Chloro-N-[trans-4-(MethylaMino)cyclohexyl]-N-[[3-(4-pyridinyl)phenyl]Methyl]- 3-chloro-N-((1r,4r)-4-(methylamino)cyclohexyl)-N-(3-(pyridin-4-yl)benzyl)benzo[b]thiophene-2-carboxamide 3-Chloro-N-[trans-4-(methylamino)cyclohexyl]-N-[[3-(4-pyridinyl)phenyl]methyl]- benzo[b]thiophene-2-carboxamide |
CAS | 912545-86-9 |
化学式 | C28H28ClN3OS |
分子量 | 490.06 |
密度 | 1.30±0.1 g/cm3(Predicted) |
沸点 | 688.6±55.0 °C(Predicted) |
溶解度 | 溶于DMSO (高达20 mg/ml) 、DMF (高达20 mg/ml) 或乙醇 (高达20 mg/ml)。 |
酸度系数 | 10?+-.0.40(Predicted) |
存储条件 | Keep in dark place,Inert atmosphere,Store in freezer, under -20°C |
稳定性 | 光敏 |
敏感性 | Light Sensitive |
外观 | 冻干固体 |
颜色 | white to beige |
体外研究 | SAG (0.1 nM-100 μM; 30 h) induces firefly luciferase expression in Shh-LIGHT2 cells with an EC 50 of 3 nM and then inhibits expression at higher concentrations. SAG (1-1000 nM; 1 h) competes for the binding of BODIPY-cyclopamine to Smo-expressing Cos-1 cells, yielding an apparent dissociation constant (K d ) of 59 nM for the SAG/Smo complex. SAG (100 nM) inhibits the inhibitory effect of ShhN-induced pathway activation by Robotnikinin. SAG (250 nM; 48 h) significantly increases SMO mRNA and protein expression in MDAMB231 cells. SAG (250 nM; 24 and 48 h) increases CAXII mRNA expression in MDAMB231 cells at 24h in normoxic and hypoxic conditions in MDAMB231 cells. SAG (250 nM; 24 h) increases MDAMB231 cells migration. |
体内研究 | SAG (1.0 mM) induces more osteogenesis mainly at the defect borders and a significant increase in BV/TV at the eight week timepoint in CD-1 mice. SAG (15-20 mg/kg; i.p.) induces pre-axial polydactyly prevalently in a dose-dependent manner in mice. Animal Model: Pregnant C57BL/6J mice Dosage: 15, 17, 20 mg/kg Administration: A single i.p. Result: Effective in ca. 80% of the embryos and increased Gli1 and Gli2 mRNA expression in the limb bud, with Gli1 mRNA being the most upregulated at the dose of 20 mg/kg. |
危险品运输编号 | UN 2811 6.1 / PGIII |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.041 ml | 10.203 ml | 20.406 ml |
5 mM | 0.408 ml | 2.041 ml | 4.081 ml |
10 mM | 0.204 ml | 1.02 ml | 2.041 ml |
5 mM | 0.041 ml | 0.204 ml | 0.408 ml |
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