GRI977143; GRI-977143
| 中文名称 | GRI977143; GRI-977143 |
|---|---|
| 中文同义词 | 2-[3-(1,3-二氧代-1H,3H-苯并[DE]异喹啉-2-基)-丙基磺酰基]-苯甲酸;化合物 T22812;化合物GRI977143;2-((3-(1,3-二氧代-1H-苯并[DE]异喹啉-2(3H)-基)丙基)硫基)苯甲酸;GRI 977143,LPA2受体非脂质激动剂 |
| 英文名称 | 2-[3-(1,3-Dioxo-1H,3H-benzo[de]isoquinolin-2-yl)-propylsulfanyl]-benzoic acid |
| 英文同义词 | 2-((3-(1,3-Dioxo-(1H)benzo[de]isoquinolin-2(3H)-yl)propyl)thio)benzoic Acid;2-[[3-(1,3-Dioxo-1H-benz[de]isoquinolin-2(3H)-yl)propyl]thio]-benzoic acid;GRI977143;2-[3-(1,3-Dioxo-1H,3H-benzo[de]isoquinolin-2-yl)-propylsulfanyl]-benzoic acid;GRI977143; GRI-977143;Benzoic acid, 2-[[3-(1,3-dioxo-1H-benz[de]isoquinolin-2(3H)-yl)propyl]thio]-;2-((3-(1,3-Dioxo-1H-benzo[de]isoquinolin-2(3H)-yl)propyl)thio)benzoic acid , GRI977143 |
| CAS号 | 325850-81-5 |
| 分子式 | C22H17NO4S |
| 分子量 | 391.44 |
| EINECS号 | 803-533-4 |
| 相关类别 | |
| Mol文件 | 325850-81-5.mol |
| 结构式 |  |
GRI977143; GRI-977143 性质
| 储存条件 | 2-8°C |
|---|---|
| 溶解度 | DMSO：可溶10mg/mL，澄清 |
| 形态 | 粉末 |
| 颜色 | 白色至浅棕色 |
GRI977143 是特异性的 LPA2 受体的激动剂，其EC50 值为3.3 μM。
|
LPA 2 Receptor 3.3 μM (EC 50 ) |
GRI977143 (10 μM, 24-72 h) is effective in reducing activation of caspases 3, 7, 8, and 9 and inhibits poly(ADP-ribose)polymerase 1 cleavage and DNA fragmentation in different extrinsic and intrinsic models of apoptosis.
GRI977143 is an effective stimulator of extracellular signal-regulated kinase 1/2 activation and promotes the assembly of a macromolecular signaling complex consisting of LPA2, Na+-H+ exchange regulatory factor 2, and thyroid receptor interacting protein 6.
Cell Proliferation Assay
| Cell Line: | Vector- and LPA2-transduced MEF cells (2 × 10 4 ) [1] . |
| Concentration: | 10 μM. |
| Incubation Time: | 24-72 h. |
| Result: | Did not cause a significant increase in vector cell proliferation except at 72 h (p < 0.05). |
Apoptosis Analysis.
| Cell Line: | Doxorubicin-induced apoptotic signaling in vector-transduced or LPA2-transduced MEF. |
| Concentration: | 10 μM. |
| Incubation Time: | 24 h. |
| Result: |
Reduced caspase 3 and 7 activation on LPA2-transduced MEF cells by 51 ± 3% and was approximately as potent as 3 μM LPA or OTP.
Protected against doxorubicin-induced apoptosis by inhibiting caspase 3, 7, 8, and 9 and reducing DNA fragmentation. |
安全信息
| 危险品标志 | Xn,N |
|---|---|
| 危险类别码 | 22-43-50/53 |
| 安全说明 | 36/37-60-61 |
| 危险品运输编号 | UN 3077 9 / PGIII |
| WGK Germany | 3 |