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5mg |
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10mg |
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25mg |
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50mg |
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Protosappanin A is a novel and potent immunosuppressive agent isolated from Caesalpinia sappan L. Protosappanin A inhibits JAK2/STAT3-dependent inflammation pathway through down-regulating the phosphorylation of JAK2/STAT3.
ln Vitro |
In LPS-activated BV2 microglia, protosappanin A (PTA: 12.5, 25, 50 μM, 24 hours) markedly reduced TNF-α and IL-1β production. PTA decreased the mRNA expression of MCP-1, IL-1β, and IL-6 in the BV2 microglial cell line in a dose-dependent manner [1]. In response to LPS treatment, protosappanin A (PTA: 12.5, 25, 50 μM, 24 hours) suppresses the JAK2/STAT3-dependent inflammatory pathway by downregulating JAK2 and STAT3 phosphorylation as well as STAT3 nuclear translocation [1]. Protosappanin A (PTA: 12.5, 25, 50 μM, 24 hours) significantly inhibits the NF-κB-dependent oxidative and nitrative stress-induced increase in LPS by interfering with the interaction between the transmembrane protein CD14 and Toll-like receptor 4. BV2 microglia [2].
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Cell Assay |
Western Blot analysis [1]
Cell Types: mouse BV2 microglial cell line. Tested Concentrations: 12.5, 25, 50 μM. Incubation Duration: 24 hrs (hours). Experimental Results: Inhibited LPS-induced release of NO, TNF-α and IL-1β in BV2 cells. LPS-induced IL-6, IL-1β and MCP-1 gene expression was attenuated in BV2 cells. Inhibits LPS-induced activation of the JAK2/STAT3 pathway in BV2 cells. |
References |
[1]. Wang LC, et al. Protosappanin A exerts anti-neuroinflammatory effect by inhibiting JAK2-STAT3 pathway in lipopolysaccharide-induced BV2 microglia. Chin J Nat Med. 2017 Sep;15(9):674-679.
[2]. Zeng KW, et al. Protosappanin A inhibits oxidative and nitrative stress via interfering the interaction of transmembrane protein CD14 with Toll-like receptor-4 in lipopolysaccharide-induced BV-2 microglia. Int Immunopharmacol, 2012, 14(4): 558- 569. |
Molecular Formula |
C15H12O5
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Molecular Weight |
272.2528
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CAS # |
102036-28-2
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Related CAS # |
102036-28-2;
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
O1C([H])([H])C(C([H])([H])C2=C([H])C(=C(C([H])=C2C2C([H])=C([H])C(=C([H])C1=2)O[H])O[H])O[H])=O
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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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
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 (~459.14 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (7.64 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 (7.64 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 (7.64 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 | 3.6731 mL | 18.3655 mL | 36.7309 mL | |
5 mM | 0.7346 mL | 3.6731 mL | 7.3462 mL | |
10 mM | 0.3673 mL | 1.8365 mL | 3.6731 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.