| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| ln Vitro |
Radioprotectin-1 is a powerful agonist of LPA2 with an EC50 of 5 pM and acts as a complete agonist of the human ortholog of LPA2 [1]. Radioprotectin-1 (0-3 μM; 15 min) substantially decreases apoptosis generated by gamma radiation and the radiomimetic medication doxorubicin in cells expressing LPA2 endogenously or after transfection [1].
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| ln Vivo |
A highly effective and selective agonist of the mouse LPA2 GPCR is radioprotectin-1 [1]. The C57BL/6 Mouse Mortality Rate (GI-ARS) is decreased by subcutaneous injection of radioprotectin-1 (0.1 mg/kg, 0.3 mg/kg; every 12 hours; for 3 days) [1]. In Lgr5+ stem cells, radioprotectin-1 specifically activates the upregulated LPA2 GPCR to produce its effects of radioprotection and radiomitigation [1].
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| Cell Assay |
Cell Viability Assay [1]
Cell Types: MEF cells, IEC-6 cells Tested Concentrations: 0 μM, 0.1 μM, 0.3 μM, 1.0 μM, 3 μM Incubation Duration: 15 minutes Experimental Results: Doxorubicin by gamma radiation and radiomimetic chemotherapy. |
| Animal Protocol |
Animal/Disease Models: 8-10 weeks old C57BL/6 female mice, subjected to total body irradiation (TBI) [1]
Doses: 0.1 mg/kg, 0.3 mg/kg Route of Administration: subcutaneous injection; once every 12 hrs (hrs (hours)); for 3 days Experimental Results: Mortality of C57BL/6 mice was diminished in HE-ARS and GI-ARS models. |
| References |
| Molecular Formula |
C23H19CLN2O6S
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|---|---|
| Molecular Weight |
486.924763917923
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| Exact Mass |
486.065
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| CAS # |
1622006-09-0
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| PubChem CID |
77461257
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| Appearance |
White to light yellow solid powder
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| LogP |
3.7
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
33
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| Complexity |
845
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| Defined Atom Stereocenter Count |
0
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| SMILES |
ClC1C=CC(=C(C(=O)O)C=1)S(NCCCCN1C(C2=CC=CC3=CC=CC(C1=O)=C23)=O)(=O)=O
|
| InChi Key |
OVJUYQCJIFWMBI-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H19ClN2O6S/c24-15-9-10-19(18(13-15)23(29)30)33(31,32)25-11-1-2-12-26-21(27)16-7-3-5-14-6-4-8-17(20(14)16)22(26)28/h3-10,13,25H,1-2,11-12H2,(H,29,30)
|
| Chemical Name |
5-chloro-2-[4-(1,3-dioxobenzo[de]isoquinolin-2-yl)butylsulfamoyl]benzoic acid
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~125 mg/mL (~256.72 mM)
H2O : < 0.1 mg/mL |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.27 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.27 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.27 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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