4-Hydroxylonchocarpin
Based on 2 publication(s) in Google Scholar
4-Hydroxylonchocarpin is a chalcone compound. 4-Hydroxylonchocarpin enhances the phosphorylation of p38 MAPK, JNK and ERK. 4-Hydroxylonchocarpin induces reactive oxygen species (ROS) and apoptosis in liver cancer cells. 4-Hydroxylonchocarpin has various pharmacological activities, including antibacterial, anticancer, anti-retroviral, anti-tuberculosis, anti-malarial and anti-inflammatory activities.
For research use only. We do not sell to patients.
- Purity : 98.95%
- CAS No.: 56083-03-5
- Formula: C20H18O4
- Molecular Weight:322.36
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Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications Citing Use of MedChemExpress (MCE) 4-Hydroxylonchocarpin
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Biological Activity
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEp-2 | CC50 |
2 μM
Compound: 19
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Cytotoxicity against human HEp-2 cells measured after 3 days by CellTiter 96 aqueous one solution assay (Rvb >100 microM)
Cytotoxicity against human HEp-2 cells measured after 3 days by CellTiter 96 aqueous one solution assay (Rvb >100 microM)
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[PMID: 38579352] |
| HEp-2 | IC50 |
>0.8 μM
Compound: 19
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Antiviral activity against Human respiratory syncytial virus infected in human HEp-2 cells assessed as plaque reduction preincubated with cells 15 mins followed by viral infection for 2.5 hrs and measured after 3 days by crystal violet staining based micr
Antiviral activity against Human respiratory syncytial virus infected in human HEp-2 cells assessed as plaque reduction preincubated with cells 15 mins followed by viral infection for 2.5 hrs and measured after 3 days by crystal violet staining based micr
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[PMID: 38579352] |
| J774.A1 | IC50 |
>20 μM
Compound: 3
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Antiamastigote activity against promastigote stage of Leishmania donovani MHOM/IN/80/Dd8 expressing luciferase firefly reporter gene infected in mouse J774A1 cells after 72 hrs by luminescence assay
Antiamastigote activity against promastigote stage of Leishmania donovani MHOM/IN/80/Dd8 expressing luciferase firefly reporter gene infected in mouse J774A1 cells after 72 hrs by luminescence assay
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[PMID: 24858541] |
| MCF7 | IC50 |
27 μM
Compound: 7
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Cytotoxicity against human MCF7 cells after 72 hrs
Cytotoxicity against human MCF7 cells after 72 hrs
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[PMID: 10075742] |
| MCF7 | IC50 |
4.7 μM
Compound: 7
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Inhibition of phorbol ester-induced ornithine decarboxylase in human MCF7 cells after 6 hrs
Inhibition of phorbol ester-induced ornithine decarboxylase in human MCF7 cells after 6 hrs
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[PMID: 10075742] |
| RAW264.7 | IC50 |
10.2 μM
Compound: Table 4, R8C1
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Inhibition of LPS-induced nitric oxide production in mouse RAW264.7 cells
Inhibition of LPS-induced nitric oxide production in mouse RAW264.7 cells
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[PMID: 32208222] |
| THP-1 | CC50 |
76.25 μM
Compound: 2
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Cytotoxicity against human THP1 cells assessed as cell viability after 72 hrs by MTT assay
Cytotoxicity against human THP1 cells assessed as cell viability after 72 hrs by MTT assay
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[PMID: 26906638] |
| THP-1 | IC50 |
23.02 μM
Compound: 2
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Antileishmanial activity against intracellular amastigote stage of Leishmania amazonensis infected in human THP1 cells after 3 hrs by microplate based assay
Antileishmanial activity against intracellular amastigote stage of Leishmania amazonensis infected in human THP1 cells after 3 hrs by microplate based assay
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[PMID: 26906638] |
In Vitro
4-Hydroxylonchocarpin (7.5-30 μM) reduces the oxidation activity of L-DOPA in B16F10 cells in a dose-dependent manner[1].
4-Hydroxylonchocarpin (15 μM, pretreated for 30 min-3 h) reduces α-MSH and IBMX-induced tyrosinase activity in B16F10 cells[1].
4-hydroxylonchocarpin causes hepatocyte injury and apoptosis by inducing oxidative stress and mitochondrial dysfunction in HepG2 cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:B16F10, SKMEL and MNT-1
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Concentration:15 μM
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Incubation Time:pretreated 30 min, 1 or 3 h
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Result:The expression of tyrosinase induced by IBMX or α-MSH was significantly reduced.
MITF expression at the protein level was reduced.
Reversed the decrease in AKT and GSK3β phosphorylation due to IMBX and α-MSH treatment.
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Cell Line:B16F10, SKMEL and MNT-1
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Concentration:15 μM
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Incubation Time:pretreated 1 or 3 h
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Result:Expression of Tyrp1 and Dct/Tyrp2 was downregulated even in the presence of IBMX.
MITF expression at the mRNA level was reduced.
Inhibited the promoter activity of tyrosinase and MITF.
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Cell Line:HepG2
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Concentration:16, 32, 48, 64, 80, 96, 112, and 128 μM
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Incubation Time:24 h
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Result:16 and 32 μM had little effect on cell viability, while cell viability decreased at higher drug concentrations.
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Cell Line:HepG2
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Concentration:9, 45, and 90 μM
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Incubation Time:24 h
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Result:9 μM reduced HepG2 cells apoptosis, while 45 μM and 90 μM significantly increased apoptosis.
Chemical Information
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CAS No. 56083-03-5
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Appearance Solid
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Molecular Weight 322.36
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Formula C20H18O4
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Color Yellow to orange
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SMILES
O=C(C1=CC=C2C(C=CC(C)(C)O2)=C1O)/C=C/C3=CC=C(O)C=C3
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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)
Publications (2)
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Journal Impact Factor
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Most Recent
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Pharmacol Res
2026 Mar:225:108112. PMID: 41620153 -
Toxicol Lett
4-hydroxylonchocarpin and corylifol A: The potential hepatotoxic components of Psoralea corylifolia L. [Abstract]2023 Aug 15:385:31-41. PMID: 37598872
Solvent & Solubility
In Vitro:
DMSO : 50 mg/mL (155.11 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 (7.76 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (7.76 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
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.
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.
Protocols
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Kinase activity and phosphorylation assays
Kinase activity assays measure the ability of kinases to transfer phosphate groups from ATP to specific substrates, while phosphorylation assays detect the presence and levels of phosphorylated proteins. Common methods include radiolabeled ATP incorporation (e. g. ,), ADP release detection via bioluminescence (e. g. ,[3]), enzyme-linked immunosorbent assays (ELISA) for phospho-specific epitopes (e. g. ,[6]), and microtiter-based formats for high-throughput screening (e. g. ,[8]). The ADP-Glo assay quantifies kinase activity by measuring ADP produced during phosphorylation using a luciferase-based system. Radiometric assays involve autoradiography or scintillation counting after incorporation of 32P-labeled ATP into substrate proteins. ELISA-based approaches rely on phospho-specific antibodies to detect activated kinases in cell lysates or purified samples.
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Western Blot
Western blotting (WB) is a commonly used experimental method in molecular biology, biochemistry, and immunogenetics for identifying and quantifying target proteins. It combines gel electrophoresis with immunoassay, enabling researchers to analyze protein expression, post-translational modifications, and molecular weight.
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Research Protocol for Infectious Diseases
Infectious-disease experiments test how pathogens interact with host barriers, innate immune receptors, inflammatory signaling, pathogen replication, and tissue injury; pattern-recognition receptors such as TLRs, RIG-I-like receptors, NOD-like receptors, and inflammasomes detect microbial molecules and activate NF-κB, interferon, and cytokine responses. The central hypothesis is that infection severity reflects the balance between pathogen burden and host response: protective inflammation restricts pathogen growth, whereas excessive or mislocalized inflammation contributes to tissue damage and disease phenotype. Unresolved questions include which host pathways are protective versus pathogenic, why some infection models fail to translate to human disease, and which combined readouts best predict clinically relevant infection outcomes.
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Apoptosis
Apoptosis, also called programmed cell death, is generally characterized by distinct morphological characteristics.
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TUNEL staining for apoptotic DNA fragmentation
TUNEL staining detects DNA strand breaks by using terminal deoxynucleotidyl transferase to add labeled nucleotides to exposed 3′-OH DNA termini, generating either microscopic staining in fixed cells or tissue sections, or fluorescence/cytometric signal in cell suspensions. TUNEL positivity reflects DNA fragmentation but should not be interpreted alone as definitive apoptosis, because TUNEL can also label necrotic, autolytic, mechanically damaged, or DNA-repair-associated DNA breaks.
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Annexin V plus membrane-impermeant dye apoptosis staining
Annexin V-based apoptosis assays rely on the detection of phosphatidylserine (PS) externalization from the inner leaflet of the plasma membrane to the outer leaflet, an early biochemical hallmark of apoptosis. Fluorescently labeled Annexin V binds PS in a calcium-dependent manner, enabling identification of early apoptotic cells by flow cytometry or fluorescence microscopy. When combined with a membrane-impermeant DNA-binding dye (e. g. , propidium iodide), this approach allows discrimination between viable (Annexin V−/dye−), early apoptotic (Annexin V+/dye−), and late apoptotic or necrotic (Annexin V+/dye+) cell populations by assessing membrane integrity and PS exposure.
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ROS/oxidative-stress fluorescent staining
ROS/oxidative-stress fluorescent staining uses cell-permeant fluorogenic probes that become fluorescent after oxidation inside cells or tissues; commonly used examples include DCFH-DA/DCFDA for broad cellular oxidant detection, DHE for superoxide-related signal detection, MitoSOX for mitochondrial superoxide-related signal detection, and CellROX probes for oxidative-stress-associated fluorescence readouts. The assay detects probe oxidation rather than a single ROS species unless the probe and analysis method have been chemically validated for that species. DCFH-DA enters cells, is deacetylated by intracellular esterases to DCFH, and produces fluorescent DCF after oxidation, so the readout is used as an operational measure of total cellular oxidative stress rather than a species-specific ROS measurement. DHE and MitoSOX can report superoxide-related oxidation, but red fluorescence alone can include non-specific ethidium-like oxidation products; HPLC or optimized spectral approaches are
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Apoptosis Solutions
Apoptosis is a regulated, generally non-lytic cell-death pathway that removes unwanted, damaged, infected, or abnormal cells through coordinated morphological changes, caspase activation, DNA fragmentation, and membrane remodeling. The intrinsic apoptosis pathway is controlled mainly by mitochondrial outer membrane permeabilization, BCL-2 family proteins, cytochrome c release, apoptosome formation, caspase-9 activation, and downstream executioner caspase-3/7 activation. The extrinsic apoptosis pathway is initiated by death receptors such as Fas, TNFR, and TRAIL receptors, which recruit adaptor proteins and activate caspase-8 before engaging executioner caspases or mitochondrial amplification through BID cleavage. Apoptosis is linked to many phenotypes, including cancer cell killing, tissue homeostasis, immune regulation, neurodegeneration, infection response, and treatment-induced cytotoxicity; unresolved questions include how apoptosis interacts with necroptosis, pyroptosis, ferroptos
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Protocol for Kinase activity and phosphorylation assays
Kinase activity assays measure transfer of phosphate from ATP to a protein or peptide substrate, generating phosphorylated substrate, ADP, or incorporated radiolabeled phosphate as the readout; phosphorylation assays measure site-specific phosphorylation in cells or tissues as a proxy for kinase-pathway activation, inhibition, or substrate regulation. Phosphorylation can be detected by phospho-specific Western blot, immunoprecipitation kinase assay, phospho-immunofluorescence, phospho-flow cytometry, luminescent ADP detection, radiolabeled ATP incorporation, or reporter-based pathway assays, and these readouts can be applied to cancer cells, primary neurons, mouse tumors, organoids, inflammatory macrophages, ferroptosis studies, and mitophagy studies when the kinase target is biologically relevant.
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Liver Cancer Modeling
Liver cancer can be classified into primary liver cancer and secondary liver cancer. Secondary liver cancer is the metastatic liver cancer. Primary liver cancer includes hepatocellular carcinoma (HCC), intrahepatic cholangiocarcinoma (ICC) and fibrolamellar HCC, of which HCC is the most common form, accounting for approximately 90% of primary liver cancers[1]. HCC mouse models include chemical agent-induced models, transplanted tumor models, and genetic engineered models.
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Research Protocol for Inflammation-related Diseases
The NLRP3 inflammasome is a cytosolic innate immune signaling platform that integrates priming signals and danger-signal activation to promote caspase-1 activation, maturation of IL-1β and IL-18, and gasdermin D-mediated pyroptotic cell death. The core experimental logic is to determine whether inflammatory disease phenotypes are driven by increased NLRP3 expression, ASC-containing inflammasome assembly, caspase-1 cleavage, GSDMD cleavage, and extracellular release of IL-1β/IL-18 rather than by nonspecific cell injury alone. The pathway is strongly linked to inflammation-related disease phenotypes because monosodium urate crystals activate NALP3/NLRP3 inflammasome signaling in gout-like crystal inflammation, cholesterol crystals activate NLRP3 inflammasomes in atherogenesis models, and DSS-induced intestinal inflammation has been reported to involve NLRP3 inflammasome activity. However, experimental colitis studies also show context-dependent protective effects of NLRP3 inflammasome co
Purity & Documentation
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Data Sheet (276 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
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- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Handling Instructions (2659 KB)
References
[1]. Lim J, et al. Antimelanogenic effect of 4-hydroxylonchocarpin through the inhibition of tyrosinase-related proteins and MAPK phosphatase. Exp Dermatol. 2016 Jul;25(7):574-6. [Content Brief]
[2]. Ouyang L, et al. 4-hydroxylonchocarpin and corylifol A: The potential hepatotoxic components of Psoralea corylifolia L. Toxicol Lett. 2023 Aug 15;385:31-41. [Content Brief]
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 | 3.1021 mL | 15.5106 mL | 31.0212 mL | 77.5530 mL |
| 5 mM | 0.6204 mL | 3.1021 mL | 6.2042 mL | 15.5106 mL | |
| 10 mM | 0.3102 mL | 1.5511 mL | 3.1021 mL | 7.7553 mL | |
| 15 mM | 0.2068 mL | 1.0340 mL | 2.0681 mL | 5.1702 mL | |
| 20 mM | 0.1551 mL | 0.7755 mL | 1.5511 mL | 3.8777 mL | |
| 25 mM | 0.1241 mL | 0.6204 mL | 1.2408 mL | 3.1021 mL | |
| 30 mM | 0.1034 mL | 0.5170 mL | 1.0340 mL | 2.5851 mL | |
| 40 mM | 0.0776 mL | 0.3878 mL | 0.7755 mL | 1.9388 mL | |
| 50 mM | 0.0620 mL | 0.3102 mL | 0.6204 mL | 1.5511 mL | |
| 60 mM | 0.0517 mL | 0.2585 mL | 0.5170 mL | 1.2926 mL | |
| 80 mM | 0.0388 mL | 0.1939 mL | 0.3878 mL | 0.9694 mL | |
| 100 mM | 0.0310 mL | 0.1551 mL | 0.3102 mL | 0.7755 mL |