Gomisin M2
Based on 1 Customer Validation
Gomisin M2 ((+)-Gomisin M2) is a lignan isolated from the fruits of Schisandra chinensis with oral availability. Gomisin M2 inhibits STAT1 phosphorylation as well as NF-κB p65 phosphorylation and nuclear translocation. Gomisin M2 reduces inflammatory cell infiltration, cytokine and chemokine expression, and serum IgE and IgG2a levels. Gomisin M2 inhibits MAPK phosphorylation, IκBα degradation, and NF-κB nuclear translocation in keratinocytes. Gomisin M2 induces apoptosis, mitochondrial membrane potential disruption, and cytochrome c release, and inhibits DNA synthesis and mammosphere formation through downregulation of Wnt/β-catenin. Gomisin M2 can be used for research on atopic dermatitis, psoriasis, breast cancer, liver injury, and multidrug-resistant mammary adenocarcinoma.
For research use only. We do not sell to patients.
- Purity : 99.75%
- CAS No.: 82425-45-4
- Formula: C22H26O6
- Molecular Weight:386.44
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Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
All DNA/RNA Synthesis Isoforms
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Biological Activity
Description
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STAT1 |
NF-κB |
p65 |
IκBα |
p38 MAPK |
Wnt |
β-catenin |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MDA-MB-231 | IC50 |
60 μM
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Inhibition of proliferation of human MDA-MB-231 cells assessed by Alamar blue cell viability assay after 48 hrs of treatment.
Inhibition of proliferation of human MDA-MB-231 cells assessed by Alamar blue cell viability assay after 48 hrs of treatment.
|
31612865 |
| HCC1806 | IC50 |
57 μM
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Inhibition of proliferation of human HCC1806 cells assessed by Alamar blue cell viability assay after 48 hrs of treatment.
Inhibition of proliferation of human HCC1806 cells assessed by Alamar blue cell viability assay after 48 hrs of treatment.
|
31612865 |
| MCF-10A | IC50 |
80 μM
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Viability of immortalized normal human breast epithelial MCF10A cells assessed by Alamar blue cell viability assay after 48 hrs of treatment, where the IC50 was reported as greater than 80 μM.
Viability of immortalized normal human breast epithelial MCF10A cells assessed by Alamar blue cell viability assay after 48 hrs of treatment, where the IC50 was reported as greater than 80 μM.
|
31612865 |
In Vitro
Gomisin M2 (GM2) (0.1-10 μM; 1 h) inhibits the expression of inflammatory cytokines and chemokines in TNF-α/IFN-γ-stimulated HaCaT cells through the suppression of STAT1 phosphorylation and the nuclear translocation of NF-κB[1].
Gomisin M2 (GM2) (0.1-10 µM; 1 h) reduces the secretion of CCL17 and IL-6 in TNF-α- and IFN-γ-stimulated HaCaT keratinocytes[2].
Gomisin M2 (0.1-10 µM; 1 h) decreases inflammatory gene expression in TNF-α- and IFN-γ-stimulated HaCaT keratinocytes[2].
Gomisin M2 (10 µM; 1 h) inhibits STAT1 phosphorylation and NF-κB translocation in TNF-α- and IFN-γ-activated HaCaT keratinocytes[2].
Gomisin M2 (0.1-10 μM) possesses anti-inflammatory effects on TNF-α and IFN-γ stimulated HaCaT keratinocytes by alleviating PS-associated cytokines and inhibiting mitogen-activated protein kinase phosphorylation[3].
Gomisin M2 (48 h) inhibits MDA-MB-231 and HCC1806 cell viability with IC50 values of 60 and 57 μM respectively, and shows low cytotoxic activity against MCF10A non-cancer cells in vitro[4].
Gomisin M2 (100 μM; 9 days) decreases the size of 3D spheroids formed by MDA-MB-231 and HCC1806 cells over 9 days in culture[4].
Gomisin M2 (5-40 μM; 48 h) dose-dependently increases cytosolic cytochrome c release in MDA-MB-231 and HCC1806 cells after 48 h of treatment[4].
Gomisin M2 (20-80 μM; 48 h) inhibits DNA synthesis and cell proliferation in MDA-MB-231 and HCC1806 cells[4].
Gomisin M2 (5-40 μM; 1-3 days) downregulates the Wnt/β-catenin self-renewal pathway in MDA-MB-231 and HCC1806 cells by decreasing CyclinD1, β-catenin, and p-GSK3β, and increasing p-β-catenin and GSK3-β in a dose- and time-dependent manner[4].
Gomisin M2 (40 μM; 48 h) induces mitochondrial-initiated apoptotic events in MDA-MB-231 and HCC1806 tumor spheres, characterized by increased cell permeability and cytochrome c release, decreased mitochondrial membrane potential, and reduced nuclear intensity[4].
Gomisin M2 (20-80 μM; 48 h) induces apoptosis in MDA-MB-231 and HCC1806 cells in a dose-dependent manner[4].
Gomisin M2 (10-60 μM; 48 h) induces cleavage of caspase-3 and PARP in MDA-MB-231 and HCC1806 cells in a dose-dependent manner[4].
Gomisin M2 (compound 5) (10 µM; 1 h) exhibits moderate hepatoprotective activity against APAP-induced damage in HepG2 cells, resulting in a 43.5% survival rate at 10 µM[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HaCaT cells
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Concentration:0.1 μM; 1 μM; 10 μM
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Incubation Time:1 h (GM2 pretreatment); 6 h (TNF-α/IFN-γ stimulation)
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Result:Decreased the expression of inflammatory cytokines IL-1β and IL-6 and chemokines CXCL8 and CCL22 compared to TNF-α/IFN-γ-stimulated HaCaT cells.
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Cell Line:HaCaT
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Concentration:0.1 μM; 1 μM; 10 μM
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Incubation Time:1 h (GM2); 15 h (TNF-α and IFN-γ)
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Result:Significantly reduced the secretion of CCL17 and IL-6 in a dose-dependent manner compared with the TNF-α- and IFN-γ-stimulated group.
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Cell Line:HaCaT
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Concentration:0.1 μM; 1 μM; 10 μM
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Incubation Time:1 h (GM2); 6 h (TNF-α and IFN-γ)
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Result:Significantly reduced the expression of cytokines and chemokines, including CCL17, IL-8, IL-6 and IL-1β, in a dose-dependent manner compared with the TNF-α- and IFN-γ-stimulated group.
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Cell Line:HaCaT
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Concentration:10 µM
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Incubation Time:1 h (GM2); 15 min (TNF-α and IFN-γ)
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Result:Significantly inhibited the phosphorylation of STAT1, the translocation of NF-κB and the degradation of IκBα compared with the TNF-α- and IFN-γ-stimulated group.
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Cell Line:MDA-MB-231, HCC1806
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Concentration:100 μM
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Incubation Time:9 days
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Result:Significantly decreased the cross-sectional spheroid area over 9 days in culture.
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Cell Line:MDA-MB-231, HCC1806
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Concentration:40 μM
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Incubation Time:48 h
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Result:Increased fluorescence intensity of cell permeability and cytochrome c, and significantly decreased mitochondrial membrane potential (MMP).
Decreased total nuclear intensity of blue fluorescence.
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Cell Line:MDA-MB-231, HCC1806
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Concentration:5-40 μM (MDA-MB-231); 7.5-60 μM (HCC1806)
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Incubation Time:48 h
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Result:Significantly increased the expression of cytochrome c.
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Cell Line:MDA-MB-231, HCC1806
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Concentration:20 μM; 40 μM; 80 μM
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Incubation Time:48 h
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Result:Significantly increased the number of apoptotic cells in a dose-dependent manner.
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Cell Line:MDA-MB-231, HCC1806
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Concentration:20 μM; 40 μM; 80 μM
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Incubation Time:48 h
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Result:Inhibited DNA synthesis and cell proliferation in MDA-MB-231 and HCC1806 cells.
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Cell Line:MDA-MB-231, HCC1806
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Concentration:5 μM; 10 μM; 20 μM; 40 μM
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Incubation Time:1-3 days
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Result:Significantly downregulated CyclinD1, β-catenin, and p-GSK3β, and upregulated p-β-catenin and GSK3-β in a dose- and time-dependent manner.
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Cell Line:HepG2
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Concentration:10 µM
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Incubation Time:1 h
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Result:Exhibited moderate hepatoprotective activity against APAP-induced damage, resulting in a survival rate of 43.5%.
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Cell Line:MCF-7/ADR
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Concentration:25, 20 μM (Gomisin M2); 1.25, 2.5, 5, 10, 20 μM (Adriamycin)
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Incubation Time:1 h (Gomisin M2 pre-incubation)
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Result:Reduced the IC50 of adriamycin to 3.0 μM at 25 μM, corresponding to a reversal fold of 23.6.
Reduced the IC50 of adriamycin to 4.3 μM at 20 μM, corresponding to a reversal fold of 16.5.
In Vivo
Gomisin M2 (0.1-10 mg/kg; p.o.; daily; 7 consecutive days) dose-dependently alleviates IMQ-induced psoriasis-like skin inflammation by reducing skin thickness, PASI scores, TEWL, inflammatory gene expression, serum inflammatory proteins, and Th1/Th17 cell populations[2].
Gomisin M2 (0.1-10 mg/kg; p.o.) possesses anti-inflammatory effects on psoriasis-like skin inflammation, reducing symptoms and Th1/Th17-related cytokine production in a dose-dependent manner[3].
Gomisin M2 (10 μM; water exposure; single treatment) effectively suppresses the growth and proliferation of CSC-enriched breast cancer cells in a zebrafish xenograft model, demonstrating in vivo anti-BCSC activity at a concentration two-fold lower than that required to suppress tumor sphere formation in vitro[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c mice[1]
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Dosage:0.1 mg/kg; 1 mg/kg; 10 mg/kg
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Administration:p.o.; five consecutive days per week; two weeks
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Result:Decreased ear thickness in a dose-dependent manner.
Decreased epidermal and dermal thickness of the ears.
Reduced infiltration of tissue eosinophils and mast cells.
Suppressed expressions of CD4 and CD44 in AD-like skin at 10 mg/kg.
Decreased expression of IL-1β, IL-4, IL-5, IL-6, IL-12a, and TSLP in ear tissue.
Reduced IFN-γ, IL-4, and IL-17A in draining lymph nodes.
Inhibited phosphorylation of STAT1 and NF-κB p65 in ear tissues.
Reduced serum levels of DFE-specific IgE, total IgE, and IgG2a.
Reduced protein levels of IL-4, IL-6, and TSLP in ear tissue.
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Animal Model:C57BL/6J (female, 8 weeks old, 18-20 g)[2]
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Dosage:0.1 mg/kg; 1 mg/kg; 10 mg/kg
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Administration:p.o.; daily; 7 consecutive days
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Result:Dose-dependently alleviated psoriasis characteristics including epidermis, dermis and skin thickness, epidermal hyperplasia, dry skin, and immune cell infiltration.
Decreased IMQ-induced TEWL and dose-dependently alleviated PASI score.
Decreased IMQ-induced infiltration of MPO-related cells, mast cells, and CD4+ cells into the skin.
Alleviated gene expression levels of CXCL1, IL-1β, IFN-γ, IL-17A, IL-23, and TNF-α in back skin.
Dose-dependently reduced serum levels of MPO, TNF-α, and IgG2a.
Significantly decreased spleen weights and significantly decreased CD4+ IFN-γ+ IL-17A+ cell populations in the spleen.
Did not induce pathological increases in skin thickness, PASI score, or TEWL in normal mice without IMQ induction.
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Animal Model:C57BL/6J (female)[3]
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Dosage:0.1 mg/kg; 1 mg/kg; 10 mg/kg
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Administration:p.o.
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Result:Reduced symptoms of psoriasis-like skin inflammation based on Psoriasis Area and Severity Index and histological observation.
Reduced serum levels of TNF-α, IgG2a, and myeloperoxidase.
Decreased MPO-associated cell infiltration in skin tissue in a dose-dependent manner.
Decreased production of Th1 and Th17-related cytokines such as TNF-α, IFN-γ, IL-8, IL-1β and IL-17A in the back skin.
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Animal Model:wild-type AB strain (embryos at 2 days post-fertilization)[4]
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Dosage:10 μM
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Administration:water exposure; single treatment
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Result:Reduced the growth and proliferation of CSC-enriched MDA-MB-231 or HCC1806 cells.
Decreased fluorescence intensity gradually over 48 h compared with the control group.
Increased the percentages of embryos without proliferation at 48 h compared with the DMSO group.
Chemical Information
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CAS No. 82425-45-4
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Appearance Solid
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Molecular Weight 386.44
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Formula C22H26O6
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Color White to yellow
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SMILES
OC1=C(OCO2)C2=CC3=C1C4=C(OC)C(OC)=C(OC)C=C4C[C@H](C)[C@H](C)C3
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Synonyms
(+)-Gomisin M2
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Structure Classification
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Initial Source
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (258.77 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.47 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 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)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Purity & Documentation
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Data Sheet (320 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
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 | 2.5877 mL | 12.9386 mL | 25.8772 mL | 64.6931 mL |
| 5 mM | 0.5175 mL | 2.5877 mL | 5.1754 mL | 12.9386 mL | |
| 10 mM | 0.2588 mL | 1.2939 mL | 2.5877 mL | 6.4693 mL | |
| 15 mM | 0.1725 mL | 0.8626 mL | 1.7251 mL | 4.3129 mL | |
| 20 mM | 0.1294 mL | 0.6469 mL | 1.2939 mL | 3.2347 mL | |
| 25 mM | 0.1035 mL | 0.5175 mL | 1.0351 mL | 2.5877 mL | |
| 30 mM | 0.0863 mL | 0.4313 mL | 0.8626 mL | 2.1564 mL | |
| 40 mM | 0.0647 mL | 0.3235 mL | 0.6469 mL | 1.6173 mL | |
| 50 mM | 0.0518 mL | 0.2588 mL | 0.5175 mL | 1.2939 mL | |
| 60 mM | 0.0431 mL | 0.2156 mL | 0.4313 mL | 1.0782 mL | |
| 80 mM | 0.0323 mL | 0.1617 mL | 0.3235 mL | 0.8087 mL | |
| 100 mM | 0.0259 mL | 0.1294 mL | 0.2588 mL | 0.6469 mL |