1622006-09-0
基本信息
化合物RADIOPROTECTIN-1
Benzoic acid, 5-chloro-2-[[[4-(1,3-dioxo-1H-benz[de]isoquinolin-2(3H)-yl)butyl]amino]sulfonyl]-
物理化学性质
| 沸点 | 720.6±70.0 °C(Predicted) |
| 密度 | 1.490±0.06 g/cm3(Predicted) |
| 储存条件 | -20°C储存 |
| 溶解度 | DMSO : 125 mg/mL (256.72 mM);Water : < 0.1 mg/mL (insoluble) |
| 酸度系数(pKa) | 2.69±0.36(Predicted) |
| 形态 | Solid |
| 颜色 | White to light yellow |
安全数据
| 危险性符号(GHS) |  GHS07 |
| 警示词 | 警告 |
| 危险性描述 | H302-H319-H315-H335 |
| 防范说明 | P264-P280-P302+P352-P321-P332+P313-P362-P264-P270-P301+P312-P330-P501-P264-P280-P305+P351+P338-P337+P313P |
常见问题列表
EC50: 25 nM (murine LPA 2 subtype)
Radioprotectin-1 is a potent agonist of LPA
2
with an EC
50
of 5 pM and functions as a full agonist at the human ortholog of LPA
2
.
Radioprotectin-1 (0-3 μM; 15 minutes) effectively reduces apoptosis induced by γ-irradiation and the radiomimetic drug Adriamycin in cells that expressed LPA
2
either endogenously or after transfection.
Cell Viability Assay
| Cell Line: | MEF cells , IEC-6 cells |
| Concentration: | 0 μM, 0.1 μM, 0.3 μM, 1.0 μM,3 μM |
| Incubation Time: | 15 minutes |
| Result: | Protected cells from apoptosis by γ-irradiation- and the radiomimetic chemotherapeutic Adiamycin. |
Radioprotectin-1 is a high-potency specific agonist of the murine LPA
2
GPCR .
Radioprotectin-1 (0.1 mg/kg, 0.3 mg/kg; s.c.; every 12 hours; for 3 days) decreases the mortality of C57BL/6 mice in models of the hematopoietic acute radiation syndromes (HE-ARS) and gastrointestinal acute radiation syndromes (GI-ARS) .
Radioprotectin-1 exerts its radioprotective and radiomitigative action through specific activation of the upregulated LPA
2
GPCR in Lgr5
+
stem cells.
| Animal Model: | 8-10 weeks old C57BL/6 female mice bearing total body irradiation (TBI) |
| Dosage: | 0.1 mg/kg, 0.3 mg/kg |
| Administration: | Subcutaneous injection; every 12 hours; for 3 days |
| Result: | Decreased mortality of C57BL/6 mice in models of the HE-ARS and the GI-ARS. |