1. Cell Cycle/DNA Damage MAPK/ERK Pathway Apoptosis Immunology/Inflammation
  2. PERK JNK TNF Receptor Interleukin Related
  3. Sesamoside

Sesamoside  (Synonyms: セサモシド)

製品番号: HY-N0412 純度: 99.77%
COA 取扱説明書 Technical Support

Sesamoside is an orally active anti-inflammatory, anti-hypoxic and analgesic agent. Sesamoside inhibits the phosphorylation of ERK and JNK, downregulates NLRP3 expression, restricts the nuclear localization of P65, regulates AKR1B1 expression, and reduces the expression of TRPV1 gene in the spinal cord. Sesamoside reduces the production of TNF-α, IL-6, IL-1β, iNOS and NO, restores cellular metabolism and organ function, and alleviates cold and mechanical hyperalgesia. Sesamoside can be used in research related to septic shock, high-altitude pulmonary edema and neuropathic pain.

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Sesamoside

Sesamoside 構造式

CAS 番号 : 117479-87-5

容量 価格(税別) 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 58 在庫あり
Solution
10 mM * 1 mL in DMSO USD 58 在庫あり
Solid
5 mg $53 在庫あり
10 mg $85 在庫あり
25 mg $140 在庫あり
50 mg $196 在庫あり
100 mg $275 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

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製品説明

Sesamoside is an orally active anti-inflammatory, anti-hypoxic and analgesic agent. Sesamoside inhibits the phosphorylation of ERK and JNK, downregulates NLRP3 expression, restricts the nuclear localization of P65, regulates AKR1B1 expression, and reduces the expression of TRPV1 gene in the spinal cord. Sesamoside reduces the production of TNF-α, IL-6, IL-1β, iNOS and NO, restores cellular metabolism and organ function, and alleviates cold and mechanical hyperalgesia. Sesamoside can be used in research related to septic shock, high-altitude pulmonary edema and neuropathic pain[1][2][3][4].

体外実験

Sesamoside (25-500 µM; 12 h) shows no cytotoxicity in mouse Raw264.7 cells even at concentrations up to 200 µM, with an IC50 of 246.4 µM, and only induces significant apoptosis at the concentration of 500 µM[1].
Sesamoside (25-200 µM; 6-24 h) dose-dependently and time-dependently inhibits the LPS (HY-D1056)-induced upregulation of TNF-α, IL-6, IL-1β and iNOS mRNA expression as well as NO production in mouse Raw264.7 cells[1].
Sesamoside (200 µM; 6-24 h) inhibits LPS-induced activation of the NF-κB/MAPK pathway in mouse Raw264.7 cells by reducing the phosphorylation levels of ERK and JNK, and downregulating NLRP3 protein expression in a time-dependent manner[1].
Sesamoside (200 µM; 6-24 h) inhibits LPS-induced nuclear localization of P65 in murine Raw264.7 cells in a time-dependent manner at the concentration of 200 µM[1].
Sesamoside binds tightly to human aldose reductase (AR/AKR1B1) with a binding energy of -5.5 kcal/mol[2].
Pretreatment of human bronchial epithelial BEAS-2B cells with sesamoside (200 μM; 6 h) significantly attenuates hypoxia-induced upregulation of AR, ERK, VEGF-α and TNF-α mRNA expression, elevates hypoxia-downregulated IL-10 mRNA expression, and reduces hypoxia-induced IL-6 secretion, but exerts no significant effect on HIF-1α mRNA expression[2].
Pretreatment of human bronchial epithelial BEAS-2B cells with sesamoside (200 μM; 6 h) reduces hypoxia-induced IL-6 secretion[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cytotoxicity Assay[1]

Cell Line: mouse Raw264.7 macrophage cells
Concentration: 25, 50, 100, 200, 500 µM
Incubation Time: 12 h
Result: Showed almost no cytotoxicity at concentrations up to 200 µM, with an IC50 value of 246.4 µM.
Induced 31.61% apoptosis at 500 µM, while concentrations up to 200 µM caused negligible apoptosis.

Real Time qPCR[1]

Cell Line: mouse Raw264.7 macrophage cells
Concentration: 25, 50, 100, 200 µM (6 h incubation); 200 µM (6, 12, 24 h incubation)
Incubation Time: 6 h (25-200 µM); 6, 12, 24 h (200 µM)
Result: Blocked LPS-induced increases in TNF-α, IL-6, IL-1β, and iNOS mRNA transcription at 25-200 µM for 6 h, with 200 µM showing the strongest effect.
Significantly inhibited mRNA transcription of all four targets and reduced NO production at 200 µM for 6, 12, or 24 h, with the inhibitory effect generally increasing with longer incubation times.

Western Blot Analysis[1]

Cell Line: mouse Raw264.7 macrophage cells
Concentration: 200 µM
Incubation Time: 6, 12, 24 h
Result: Inhibited LPS-induced phosphorylation of ERK and JNK, and downregulated NLRP3 protein expression, with the inhibitory effect increasing in a time-dependent manner over 6-24 h.

Immunofluorescence[1]

Cell Line: mouse Raw264.7 macrophage cells
Concentration: 200 µM
Incubation Time: 6, 12, 24 h
Result: Restricted LPS-induced nuclear translocation of P65 in a time-dependent manner, with the lowest nuclear P65 intensity observed after 24 h of treatment.

Real Time qPCR[2]

Cell Line: human bronchial epithelial BEAS-2B cells
Concentration: 200 μM (pre-treatment); 800 μM (CoCl2, hypoxia induction)
Incubation Time: 6 h (pre-treatment); 6 h (hypoxia induction)
Result: Significantly reduced the hypoxia-induced upregulation of AR, ERK, and VEGF-α mRNA expression compared to the hypoxia-only group.
Significantly reduced the hypoxia-induced upregulation of TNF-α mRNA expression compared to the hypoxia-only group.
Significantly increased the hypoxia-downregulated IL-10 mRNA expression compared to the hypoxia-only group.
Partially reduced the upregulation of IL-6 mRNA expression compared to the hypoxia-only group, but the effect was not statistically significant.
Significantly reduced the hypoxia-induced increase in IL-6 concentration in cell supernatant compared to the hypoxia-only group.
Partially reduced TNF-α secretion compared to the hypoxia-only group, but the effect was not statistically significant.
Had no significant impact on hypoxia-downregulated HIF-1α mRNA expression compared to the hypoxia-only group.

ELISA Assay[2]

Cell Line: human bronchial epithelial BEAS-2B cells
Concentration: 200 μM (pre-treatment); 800 μM (CoCl2, hypoxia induction)
Incubation Time: 6 h (pre-treatment); 6 h (hypoxia induction)
Result: Significantly reduced the hypoxia-induced increase in IL-6 concentration in cell supernatant compared to the hypoxia-only group.
Partially reduced TNF-α secretion compared to the hypoxia-only group, but the effect was not statistically significant.
体内実験

Sesamoside (1-10 mg/kg; i.p.; single dose) dose-dependently reduces LPS-induced inflammatory responses and multi-organ damage in septic shock mice by inhibiting the NF-κB/MAPK signaling pathway[1].
Sesamoside (5-7.5 mg/kg; i.p., p.o.; single dose) alleviates Paclitaxel (HY-B0015)-induced cold and mechanical peripheral neuropathy in mice, with 7.5 mg/kg doses (both intraperitoneal and oral) showing consistent efficacy, and oral 7.5 mg/kg sesamoside reducing spinal TRPV1 gene expression[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Kunming mice (male, 8-10 weeks old, specific pathogen-free, intraperitoneal injection of 10 mg/kg LPS)[1]
Dosage: 1 mg/kg; 5 mg/kg; 10 mg/kg
Administration: i.p.; single dose
Result: Significantly alleviated LPS-induced multi-organ damage to the heart, liver, spleen, lungs, and kidneys, reducing tissue congestion, edema, bleeding foci, and inflammatory cell infiltration in a dose-dependent manner.
Dose-dependently reduced mRNA transcription of pro-inflammatory cytokines TNF-α, IL-6, IL-1β, and iNOS in spleen tissue.
Inhibited LPS-induced phosphorylation of ERK and JNK, decreased protein expression of NLRP3 and P65 in spleen tissue.
Dose-dependently reduced nuclear localization of P65 in multiple organs.
Animal Model: C57BL/6 (male, 6-week-old, peripheral neuropathy induced by paclitaxel)[3]
Dosage: 5 mg/kg; 7.5 mg/kg
Administration: i.p.; single dose; p.o.; single dose
Result: Significantly reduced cold hypersensitivity (decreased response frequency in acetone drop tests) and increased mechanical sensitivity threshold (increased 50% threshold value in von Frey filament tests) at 7.5 mg/kg i.p. compared to paclitaxel + PBS controls.
Showed no significant effect on cold or mechanical hypersensitivity at 5 mg/kg i.p. compared to paclitaxel + PBS controls.
Significantly reduced cold hypersensitivity at 5 mg/kg and 7.5 mg/kg p.o. compared to paclitaxel + PBS controls.
Significantly increased mechanical sensitivity threshold at 7.5 mg/kg p.o. compared to paclitaxel + PBS controls.
Showed no significant effect on mechanical sensitivity threshold at 5 mg/kg p.o. compared to paclitaxel + PBS controls.
Significantly downregulated spinal TRPV1 gene expression at 7.5 mg/kg p.o. compared to paclitaxel + PBS controls.
Showed no significant effect on spinal TRPV1 gene expression at 5 mg/kg p.o. compared to paclitaxel + PBS controls.
分子量

420.37

分子式

C17H24O12

CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

O=C(OC)C1=CO[C@@H](O[C@@]2([H])[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O2)[C@@]3([H])[C@]1(O)[C@H](O)[C@H]4[C@]3(C)O4

Structure Classification
Initial Source
輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶剤 & 溶解度
体外: 

DMSO : 100 mg/mL (237.89 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3789 mL 11.8943 mL 23.7886 mL
5 mM 0.4758 mL 2.3789 mL 4.7577 mL
10 mM 0.2379 mL 1.1894 mL 2.3789 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (5.95 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (5.95 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション

純度: 99.77%

参考文献

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3789 mL 11.8943 mL 23.7886 mL 59.4714 mL
5 mM 0.4758 mL 2.3789 mL 4.7577 mL 11.8943 mL
10 mM 0.2379 mL 1.1894 mL 2.3789 mL 5.9471 mL
15 mM 0.1586 mL 0.7930 mL 1.5859 mL 3.9648 mL
20 mM 0.1189 mL 0.5947 mL 1.1894 mL 2.9736 mL
25 mM 0.0952 mL 0.4758 mL 0.9515 mL 2.3789 mL
30 mM 0.0793 mL 0.3965 mL 0.7930 mL 1.9824 mL
40 mM 0.0595 mL 0.2974 mL 0.5947 mL 1.4868 mL
50 mM 0.0476 mL 0.2379 mL 0.4758 mL 1.1894 mL
60 mM 0.0396 mL 0.1982 mL 0.3965 mL 0.9912 mL
80 mM 0.0297 mL 0.1487 mL 0.2974 mL 0.7434 mL
100 mM 0.0238 mL 0.1189 mL 0.2379 mL 0.5947 mL
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製品名:
Sesamoside
製品番号:
HY-N0412
数量:
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