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1622006-09-0

中文名稱 RADIOPROTECTIN-1
英文名稱 Radioprotectin-1
CAS 1622006-09-0
分子式 C23H19ClN2O6S
分子量 486.92
MOL 文件 1622006-09-0.mol
更新日期 2023/03/20 15:41:25
1622006-09-0 結(jié)構(gòu)式 1622006-09-0 結(jié)構(gòu)式

基本信息

中文別名
化合物 T12684
化合物RADIOPROTECTIN-1
英文別名
Radioprotectin-1
Benzoic acid, 5-chloro-2-[[[4-(1,3-dioxo-1H-benz[de]isoquinolin-2(3H)-yl)butyl]amino]sulfonyl]-

物理化學(xué)性質(zhì)

沸點720.6±70.0 °C(Predicted)
密度1.490±0.06 g/cm3(Predicted)
儲存條件-20°C儲存
溶解度DMSO : 125 mg/mL (256.72 mM);Water : < 0.1 mg/mL (insoluble)
酸度系數(shù)(pKa)2.69±0.36(Predicted)
形態(tài)Solid
顏色White to light yellow

常見問題列表

生物活性
Radioprotectin-1 是一種高效特異性的溶血磷脂酸受體 2 (LPA2) 激動劑,EC50 值為 25 nM (鼠源 LPA2 亞型) 。
靶點

EC50: 25 nM (murine LPA 2 subtype)

體外研究

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.
體內(nèi)研究

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.
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