Radioprotectin-1
目录号 : GC34752
Radioprotectin-1是一种高效特异性的LPA2激动剂，EC50值为25nM(鼠源LPA2亚型)。
Cas No.:1622006-09-0
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Radioprotectin-1 is a potent and specific nonlipid agonist of LPA2, with an EC50 value of 25 nM for murine LPA2 subtype[1]. EC50: 25 nM (murine LPA2 subtype)[1]
Radioprotectin-1 is a potent agonist of LPA2 with an EC50 of 5 pM and functions as a full agonist at the human ortholog of LPA2[1].Radioprotectin-1 (0-3 μM; 15 minutes) effectively reduces apoptosis induced by γ-irradiation and the radiomimetic drug Adriamycin in cells that expressed LPA2 either endogenously or after transfection[1]. Cell Viability Assay[1] Cell Line: MEF cells , IEC-6 cells
Radioprotectin-1 is a high-potency specific agonist of the murine LPA2 GPCR [1].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) [1].Radioprotectin-1 exerts its radioprotective and radiomitigative action through specific activation of the upregulated LPA2 GPCR in Lgr5+stem cells[1]. Animal Model: 8-10 weeks old C57BL/6 female mice bearing total body irradiation (TBI) [1]
[1]. Kuo B, et al. The LPA2 receptor agonist Radioprotectin-1 spares Lgr5-positive intestinal stem cells from radiation injury in murine enteroids. Cell Signal. 2018 Nov;51:23-33.
| Cas No. | 1622006-09-0 | SDF | |
| Canonical SMILES | O=C(O)C1=CC(Cl)=CC=C1S(=O)(NCCCCN(C(C2=CC=CC3=CC=CC4=C23)=O)C4=O)=O | ||
| 分子式 | C23H19ClN2O6S | 分子量 | 486.92 |
| 溶解度 | DMSO : 125 mg/mL (256.72 mM);Water : < 0.1 mg/mL (insoluble) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.0537 mL | 10.2686 mL | 20.5373 mL |
| 5 mM | 0.4107 mL | 2.0537 mL | 4.1075 mL |
| 10 mM | 0.2054 mL | 1.0269 mL | 2.0537 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
The LPA2 receptor agonist Radioprotectin-1 spares Lgr5-positive intestinal stem cells from radiation injury in murine enteroids
Cell Signal 2018 Nov;51:23-33.PMID:30063964DOI:PMC6163127
Rapidly proliferating cells are highly sensitive to ionizing radiation and can undergo apoptosis if the oxidative and genotoxic injury exceed the defensive and regenerative capacity of the cell. Our earlier work has established the antiapoptotic action of the growth factor-like lipid mediator lysophosphatidic acid (LPA). Activation of the LPA2 GPCR has been hypothesized to elicit antiapoptotic and regenerative actions of LPA. Based on this hypothesis we developed a novel nonlipid agonist of LPA2, which we designated Radioprotectin-1 (RP-1). We tested RP-1 at the six murine LPA GPCR subtypes using the transforming growth factor alpha shedding assay and found that it had a 25 nM EC50 that is similar to that of LPA18:1 at 32 nM. RP-1 effectively reduced apoptosis induced by γ-irradiation and the radiomimetic drug Adriamycin only in cells that expressed LPA2 either endogenously or after transfection. RP-1 reduced γ-H2AX levels in irradiated mouse embryonic fibroblasts transduced with the human LPA2 GPCR but was ineffective in vector transduced MEF control cells and significantly increased clonogenic survival after γ-irradiation. γ-Irradiation induced the expression of lpar2 transcripts that was further enhanced by RP-1 exposure within 30 min after irradiation. RP-1 decreased the mortality of C57BL/6 mice in models of the hematopoietic and gastrointestinal acute radiation syndromes. Using Lgr5-EGFP-CreER;Tdtomatoflox transgenic mice, we found that RP-1 increased the survival and growth of intestinal enteroids via the enhanced survival of Lgr5+ intestinal stem cells. Taken together, our results suggest that the LPA2-specific agonist RP-1 exerts its radioprotective and radiomitigative action through specific activation of the upregulated LPA2 GPCR in Lgr5+ stem cells.