SAG
| 中文名称 | SAG |
|---|---|
| 中文同义词 | 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;SMO RECEPTOR激动剂(SAG);SAG 二盐酸盐 |
| 英文名称 | SAG |
| 英文同义词 | 3-Chloro-N-[trans-4-(methylamino)cyclohexyl]-N-[[3-(4-pyridinyl)phenyl]methyl]- benzo[b]thiophene-2-carboxamide;SAG;3-Chloro-N-[trans-4-(MethylaMino)cyclohexyl]-N-[[3-(4-pyridinyl)phenyl]Methyl]-;SAG (cyclopamine antagonist);SAG (Smo agonist);3-chloro-N-((1r,4r)-4-(methylamino)cyclohexyl)-N-(3-(pyridin-4-yl)benzyl)benzo[b]thiophene-2-carboxamide;Smoothened Agonist (SAG) HCl;SAG.HCI |
| CAS号 | 912545-86-9 |
| 分子式 | C28H28ClN3OS |
| 分子量 | 490.06 |
| EINECS号 | |
| 相关类别 | 小分子抑制剂，天然产物;小分子抑制剂;细胞生物学试剂;抑制剂;试剂盒-Elisa试剂盒;Heterocyclic Compounds;Heterocycles;Intermediates & Fine Chemicals;Pharmaceuticals;Sulfur & Selenium Compounds;Inhibitors |
| Mol文件 | 912545-86-9.mol |
| 结构式 |  |
SAG 性质
| 沸点 | 688.6±55.0 °C(Predicted) |
|---|---|
| 密度 | 1.30±0.1 g/cm3(Predicted) |
| 储存条件 | Keep in dark place,Inert atmosphere,Store in freezer, under -20°C |
| 溶解度 | 可溶于 DMSO（高达 20 mg/ml）、DMF（高达 20 mg/ml）或乙醇（高达 20 mg/ml）。 |
| 酸度系数(pKa) | 10?+-.0.40(Predicted) |
| 形态 | 冻干固体 |
| 颜色 | 白色至米色 |
| 敏感性 | Light Sensitive |
| 稳定性 | 感光 |
EC50: 3 nM (Smo)
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.
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. |
安全信息
| 危险品运输编号 | UN 2811 6.1 / PGIII |
|---|---|
| 海关编码 | 2934999090 |
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/04/30 | HY-12848 | SAG SAG | 912545-86-9 | 1mg | 600元 |
| 2024/04/30 | HY-12848 | SAG SAG | 912545-86-9 | 5mg | 1800元 |