| Size | Price | Stock | Qty |
|---|---|---|---|
| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
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| Targets |
NF-κB
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|---|---|
| ln Vitro |
Barlerin (8-O-Acetyl shanzhiside methyl ester) treatment inhibits TNF-induced nuclear transcription factor B (NF-κB) activation and reduces high-mobility group box-1 (HMGB-1) expression in SH-SY5Y cells. [1]. By preventing High-mobility group box 1 (HMGB1) expression, treatment of H9c2 cells with barlerin (8-O-Acetyl shanzhiside methyl ester) 9 μM prevents TNF-α-induced NF-κB phosphorylation[2].
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| ln Vivo |
Barlerin (8-O-Acetyl shanzhiside methyl ester) 40 mg/kg exhibits a notable neuroprotective effect even when administered 4 hours after I/R. In ischaemic brain tissue, barlerin 40 mg/kg inhibits NF-κB activation, reduces HMGB-1 expression, attenuates histopathological damage, and reduces brain swelling[1]. The angiogenesis in the ischaemic brain is markedly accelerated by barlerin (8-O-Acetyl shanzhiside methyl ester), which also enhances functional recovery after stroke. Additionally, compared to vehicle treatment, barlerin significantly boosts vascularization. It raises the levels of Ang1, Tie2, and Akt VEGF as well as their expression[3]. Activated partial thromboplastin, prothrombin, and thrombin times in mice are unaffected by barlerin (8-O-Acetyl shanzhiside methyl ester), but capillary blood clotting time and blood loss volume are significantly shortened. In hyperfibrinolysis mice, it significantly extends the time it takes for euglobulin clots to dissolve[4].
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| Cell Assay |
Cells are pretreated with Barlerin (8-O-Acetyl shanzhiside methyl ester) in a range of concentrations (1, 3, 9 and 27 27μM) for 24 hours prior to hypoxia. MTT assays are used to assess cell viability[2].
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| Animal Protocol |
Rats: In saline, Barlerin (8-O-Acetyl shanzhiside methyl ester) is made. Adult male rats are given an hour of middle cerebral artery occlusion (MCAO) and reperfusion. They are then given different doses of ND01 (5 and 10 mg/kg) intravenously every day for 14 days, starting 24 hours after the I/R (ischaemia and reperfusion). In addition to measuring cerebral Evans blue extravasation, neurological functional tests are carried out[3].
Mouse: In saline, Barlerin (8-O-Acetyl shanzhiside methyl ester) is made. The five groups (saline group, Hemocoagulase, 0.34 KU/kg, intravenous, ASM-L, 100 mg/kg, ASM-M, 250 mg/kg, and ASM-H, 500 mg/kg) of male Balb/C mice (20 to 25g) are assigned at random. Five minutes before sodium pentobarbital (200 mg/kg, i.p.) is used to anesthetize the patient, the drugs and the vehicle are injected through the vena cauda. After the injection, blood is drawn from the heart 20 minutes later. Prothrombin time, thrombin time, fibrinogen, and activated partial thromboplastin time are measured[4]. |
| References |
|
| Molecular Formula |
C₁₉H₂₈O₁₂
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|---|---|
| Molecular Weight |
448.42
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| Exact Mass |
448.15807632
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| CAS # |
57420-46-9
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| Related CAS # |
57420-46-9
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| Appearance |
Solid
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| SMILES |
CC(=O)O[C@]1(C[C@H]([C@H]2[C@@H]1[C@@H](OC=C2C(=O)OC)O[C@H]3[C@@H]([C@H]([C@@H]([C@H](O3)CO)O)O)O)O)C
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| InChi Key |
ARFRZOLTIRQFCI-NGQYDJQZSA-N
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| InChi Code |
InChI=1S/C19H28O12/c1-7(21)31-19(2)4-9(22)11-8(16(26)27-3)6-28-17(12(11)19)30-18-15(25)14(24)13(23)10(5-20)29-18/h6,9-15,17-18,20,22-25H,4-5H2,1-3H3/t9-,10-,11+,12-,13-,14+,15-,17+,18+,19+/m1/s1
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| Chemical Name |
methyl (1S,4aS,5R,7S,7aS)-7-acetyloxy-5-hydroxy-7-methyl-1-[(2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-4a,5,6,7a-tetrahydro-1H-cyclopenta[c]pyran-4-carboxylate
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| Synonyms |
8-O-Acetyl shanzhiside methyl ester; Barlerin
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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: ~100 mg/mL (~223.0 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.58 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 25.0 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: ≥ 2.5 mg/mL (5.58 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 25.0 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: ≥ 2.5 mg/mL (5.58 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 | 2.2301 mL | 11.1503 mL | 22.3005 mL | |
| 5 mM | 0.4460 mL | 2.2301 mL | 4.4601 mL | |
| 10 mM | 0.2230 mL | 1.1150 mL | 2.2301 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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