Ethacrynic acid
Based on 10 publication(s) in Google Scholar
Ethacrynic acid has anti-inflammatory and anticancer activity. Ethacrynic acid is an orally active diuretic. Ethacrynic acid is an inhibitor of glutathione S-transferase (GSTs) and Wnt signaling pathways. Ethacrynic acid is a radiosensitizer. Ethacrynic acid can inhibit airway smooth muscle (ASM) contraction in mice. Ethacrynic acid can increase the outflow of aqueous humor from the eye for the study of glaucoma.
For research use only. We do not sell to patients.
- Purity: 99.90%
- CAS No.: 58-54-8
- Formula: C13H12Cl2O4
- Molecular Weight:303.14
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Storage:
4°C, protect from light
* In solvent : -80°C, 1 year; -20°C, 6 months (protect from light)
Publications Citing Use of MedChemExpress (MCE) Ethacrynic acid
More- Autophagy. 2025 Mar 31. [Abstract]
- Int J Biol Macromol. 2026 Mar:352:151224. [Abstract]
- Free Radic Biol Med. 2024 Jun 19:S0891-5849(24)00531-8. [Abstract]
- J Med Chem. 2026 May 14;69(9):11574-11591. [Abstract]
- EMBO Rep. 2021 Jun 4;22(6):e51649. [Abstract]
- Int J Mol Sci. 2024 Jul 16;25(14):7798. [Abstract]
- Life Sci Alliance. 2021 Jun 18;4(8):e202000906. [Abstract]
- Hear Res. 2025 Aug 15:466:109405. [Abstract]
- J Microbiol Biol Educ. 2025 Sep 25:e0021425. [Abstract]
- Phytomedicine. 2023 Jan:109:154603. [Abstract]
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Bio/Physico-chemical Assay
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Cell Imaging/Staining
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Cell Imaging/Staining
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Bio/Physico-chemical Assay
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WB
All Calcium Channel Isoforms
More
Biological Activity
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L-type calcium channel |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
84 μM
Compound: 1, EA
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Cytotoxicity against human A549 cells
Cytotoxicity against human A549 cells
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[PMID: 22607679] |
| CHO-K1 | EC50 |
56 μM
Compound: 1
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Cytotoxicity against CHO-K1 cells by Alamar blue assay
Cytotoxicity against CHO-K1 cells by Alamar blue assay
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[PMID: 16962325] |
| HCT-116 | IC50 |
30.22 μM
Compound: EA
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Cytotoxic activity against human HCT116 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
Cytotoxic activity against human HCT116 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
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[PMID: 27156773] |
| HCT-116 | IC50 |
75 μM
Compound: 1; EA
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Antiproliferative activity against human HCT116 cells after 24 to 72 hrs by MTS assay
Antiproliferative activity against human HCT116 cells after 24 to 72 hrs by MTS assay
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[PMID: 27448922] |
| HL-60 | GI50 |
44.2 μM
Compound: EA
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Antiproliferative activity against human HL60 cells after 72 hrs
Antiproliferative activity against human HL60 cells after 72 hrs
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[PMID: 17287120] |
| HL-60 | GI50 |
44.2 μM
Compound: EA
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Growth inhibition of human HL60 cells after 72 hrs by trypan blue staining
Growth inhibition of human HL60 cells after 72 hrs by trypan blue staining
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[PMID: 22370342] |
| HL-60 | GI50 |
45 μM
Compound: EA
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Growth inhibition of human HL60 cells by hemocytometry
Growth inhibition of human HL60 cells by hemocytometry
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[PMID: 20055416] |
| HL-60 | IC50 |
3.4 μM
Compound: EA
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Inhibition of GST P1-1 in human HL60 cell lysate
Inhibition of GST P1-1 in human HL60 cell lysate
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[PMID: 20055416] |
| HL-60 | IC50 |
38 μM
Compound: 1; EA
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Cytotoxicity against human HL60 cells assessed as reduction in cell viability after 24 hrs by MTS assay
Cytotoxicity against human HL60 cells assessed as reduction in cell viability after 24 hrs by MTS assay
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[PMID: 27448922] |
| HL-60 | IC50 |
46 μM
Compound: 1; EA
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Antiproliferative activity against human HL60 cells after 24 to 72 hrs by MTS assay
Antiproliferative activity against human HL60 cells after 24 to 72 hrs by MTS assay
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[PMID: 27448922] |
| HT-1080 | IC50 |
54.53 μM
Compound: EA
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Cytotoxic activity against human HT1080 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
Cytotoxic activity against human HT1080 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
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[PMID: 27156773] |
| HT-29 | IC50 |
62.39 μM
Compound: EA
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Cytotoxic activity against human HT-29 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
Cytotoxic activity against human HT-29 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
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[PMID: 27156773] |
| KB | IC50 |
11 μM
Compound: 1; EA
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Antiproliferative activity against human KB cells after 24 to 72 hrs by MTS assay
Antiproliferative activity against human KB cells after 24 to 72 hrs by MTS assay
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[PMID: 27448922] |
| MCF7 | IC50 |
28.92 μM
Compound: EA
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Cytotoxic activity against human MCF7 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
Cytotoxic activity against human MCF7 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
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[PMID: 27156773] |
| MCF7 | IC50 |
41 μM
Compound: 1; EA
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Antiproliferative activity against human MCF7 cells after 24 to 72 hrs by MTS assay
Antiproliferative activity against human MCF7 cells after 24 to 72 hrs by MTS assay
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[PMID: 27448922] |
| MDA-MB-231 | IC50 |
45.24 μM
Compound: EA
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Cytotoxic activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
Cytotoxic activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
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[PMID: 27156773] |
| MDA-MB-468 | IC50 |
81.45 μM
Compound: EA
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Cytotoxic activity against human MDA-MB-468 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
Cytotoxic activity against human MDA-MB-468 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
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[PMID: 27156773] |
| NCI-H1299 | IC50 |
44.29 μM
Compound: EA
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Cytotoxic activity against human H1299 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
Cytotoxic activity against human H1299 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
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[PMID: 27156773] |
| OVCAR-8 | IC50 |
72 μM
Compound: 1; EA
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Antiproliferative activity against human OVCAR8 cells after 24 to 72 hrs by MTS assay
Antiproliferative activity against human OVCAR8 cells after 24 to 72 hrs by MTS assay
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[PMID: 27448922] |
| PC-3 | IC50 |
75 μM
Compound: 1; EA
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Antiproliferative activity against human PC3 cells after 24 to 72 hrs by MTS assay
Antiproliferative activity against human PC3 cells after 24 to 72 hrs by MTS assay
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[PMID: 27448922] |
| SF-188 | IC50 |
31.65 μM
Compound: EA
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Cytotoxic activity against human SF188 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
Cytotoxic activity against human SF188 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
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[PMID: 27156773] |
| SK-BR-3 | IC50 |
34.21 μM
Compound: EA
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Cytotoxic activity against human SKBR3 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
Cytotoxic activity against human SKBR3 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
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[PMID: 27156773] |
| SK-OV-3 | IC50 |
>100 μM
Compound: 1; EA
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Antiproliferative activity against human SKOV3 cells after 24 to 72 hrs by MTS assay
Antiproliferative activity against human SKOV3 cells after 24 to 72 hrs by MTS assay
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[PMID: 27448922] |
| SW480 | IC50 |
32.7 μM
Compound: 1
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Inhibition of Wnt/beta-casein signaling in human SW480 cells by fluorimetry
Inhibition of Wnt/beta-casein signaling in human SW480 cells by fluorimetry
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[PMID: 19121941] |
Ethacrynic acid (50 μM; 24 h) inhibits Wnt/β-catenin signaling in CLL cells[1].
Ethacrynic acid (1-100 μM; 48 h) is cytotoxic in CLL cells with an IC50 of 8.56 μM[1].
Ethacrynic acid (0.01-0.25 mmol/L; 30 min) increases aqueous humor outflow facility acutely in eye and the outflow rate increases from 28% to 105%[2].
Ethacrynic acid (10-100 μM; 30 min) can inhibit the activation of NF-κB pathway in RAW264.7 cells induced by LPS (100 ng/mL) and has anti-inflammatory activity[3].
Ethacrynic acid (20 μM/mL; 2 h) can increase the radiation intensity in MCF-7 cancer cells after radiation exposure[3].
Ethacrynic acid (100 μmol/L; 62.5-250 min) inhibits tracheal ring contraction induced by high -K+ (80 mmol/L) and acetylcholine (ACh, 100 µmol/L) in a dose-dependent manner with EC50 of 40.28 µmol/L and 56.22 µmol/L, respectively[8].
Ethacrynic acid (100 μmol/L; 500-2500 s) decreases the intracellular Ca2+ concentration induced by high -K+ and ACh from 0.40 to 0.16, 0.50 to 0.39, respectively[8].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Chronic lymphocytic leukemia (CLL)
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Concentration:1 μM, 10 μM, 100 μM
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Incubation Time:16 h
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Result:Depressed the expression of LEF-1, Cyclin D1 and Fibronectin in a concentration-dependent manner.( LEF-1, cyclin D1 and fibronectin are established target genes of the Wnt/b-catenin pathway).
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Cell Line:RAW 264.7
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Concentration:10 μM, 20 μM, 50 μM, 100 μM ;Before LPS treatment (100 ng/mL; 1 h)
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Incubation Time:30 min
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Result:Inhibited the expression of iNOS mRNA.
Inhibited degradation of IκBα and IκBβ.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Myeloma Balb/c mice model[5]
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Dosage:450 μg/mouse
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Administration:Oral gavage (p.o.); Once daily for 60 days. After BALB/c mice were injected subcutaneously with 5 × 105 MPC11 myeloma cells.
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Result:Significantly inhibited tumor growth.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 58-54-8
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Appearance Solid
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Molecular Weight 303.14
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Formula C13H12Cl2O4
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Color White to off-white
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SMILES
O=C(O)COC1=CC=C(C(C(CC)=C)=O)C(Cl)=C1Cl
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Synonyms
Etacrynic acid
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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, 1 year; -20°C, 6 months (protect from light)
Publications (10)
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Journal Impact Factor
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Most Recent
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Autophagy
2025 Mar 31. PMID: 40160153
Ethacrynic acid purchased from MedChemExpress. Usage Cited in: Autophagy. 2025 Mar 31. [Abstract]
Mito-ros levels measured with MitoSOX red using a flow cytometer of SH-SY5Y cells pretreated with 10 μM AC220 for 2 h followed by cotreatment with or without 75 μM Ethacrynic acid (EA) for 24 h. n = 5; mean ± S.D.
Ethacrynic acid purchased from MedChemExpress. Usage Cited in: Autophagy. 2025 Mar 31. [Abstract]
Representative microscopy images of SH-SY5Y cells pretreated with 10 μM AC220 for 2 h followed by cotreatment with or without 75 μM Ethacrynic acid (EA) for 24 h. Scale bar: 50 μm.
Ethacrynic acid purchased from MedChemExpress. Usage Cited in: Autophagy. 2025 Mar 31. [Abstract]
PI positive of SH-SY5Y cells pretreated with 10 μM AC220 for 2 h followed by cotreatment with or without 75 μM Ethacrynic acid (EA) for 24 h. Scale bar: 50 μm.
Ethacrynic acid purchased from MedChemExpress. Usage Cited in: Autophagy. 2025 Mar 31. [Abstract]
LDH release assay of SH-SY5Y cells pretreated with 10 μM AC220 for 2 h followed by cotreatment with or without 75 μM Ethacrynic acid (EA) for 24 h. Scale bar: 50 μm.
Ethacrynic acid purchased from MedChemExpress. Usage Cited in: Autophagy. 2025 Mar 31. [Abstract]
Immunoblotting analysis for GSDME cleavage and activation of SH-SY5Y cell lysates pretreated with 10 μM AC220 for 2 h followed by cotreatment with or without 75 μM Ethacrynic acid (EA) treatment for 24 h. TUBB was used as loading control.
Ethacrynic acid purchased from MedChemExpress. Usage Cited in: Autophagy. 2025 Mar 31. [Abstract]
Images of mice administered with AC220 (1.5 mg/kg), Ethacrynic acid (EA, 5 mg/kg, i.p. once daily) or AC220 (1.5 mg/kg) plus EA (5 mg/kg) every day.
Ethacrynic acid purchased from MedChemExpress. Usage Cited in: Autophagy. 2025 Mar 31. [Abstract]
Ethacrynic acid (EA, 5 mg/kg, i.p. once daily). luciferase signal intensities of tumors were quantified using bioluminescence imaging.
Ethacrynic acid purchased from MedChemExpress. Usage Cited in: Autophagy. 2025 Mar 31. [Abstract]
Ethacrynic acid (EA, 5 mg/kg, i.p. once daily). Images of SH-SY5Y orthotopic tumors. Scale bar: 1 cm.
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Int J Biol Macromol
Reticuline isomerase AKR1B1 with aldo-keto reductase activity and detoxification function from the insect Blaps rhynchopetera. [Abstract]2026 Mar:352:151224. PMID: 41791543 -
Free Radic Biol Med
Mifepristone protects acetaminophen induced liver injury through NRF2/GSH/GST mediated ferroptosis suppression. [Abstract]2024 Jun 19:S0891-5849(24)00531-8. PMID: 38906233 -
J Med Chem
Don't Lose Your (War)head: Structure-Activity Relationships of Covalent Warheads as Substrates for GST-Catalyzed Glutathione Conjugation. [Abstract]2026 May 14;69(9):11574-11591. PMID: 42062179 -
EMBO Rep
O-GlcNAcylation of TDP-43 suppresses proteinopathies and promotes TDP-43's mRNA splicing activity. [Abstract]2021 Jun 4;22(6):e51649. PMID: 33855783 -
Int J Mol Sci
In Vivo Chemical Screening in Zebrafish Embryos Identified FDA-Approved Drugs That Induce Differentiation of Acute Myeloid Leukemia Cells. [Abstract]2024 Jul 16;25(14):7798. PMID: 39063039 -
Life Sci Alliance
HCV poly U/UC sequence-induced inflammation leads to metabolic disorders in vulvar lichen sclerosis. [Abstract]2021 Jun 18;4(8):e202000906. PMID: 34145025 -
Hear Res
2025 Aug 15:466:109405. PMID: 40865250 -
J Microbiol Biol Educ
Preliminary assessment of drug repurposing against virus-associated primary effusion lymphoma. [Abstract]2025 Sep 25:e0021425. PMID: 40996285 -
Phytomedicine
Guhong injection mitigates myocardial ischemia/reperfusion injury by activating GST P to inhibit ASK1-JNK/p38 pathway. [Abstract]2023 Jan:109:154603. PMID: 36610111
Solvent & Solubility
DMSO : 100 mg/mL (329.88 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 27.5 mg/mL (90.72 mM; Need ultrasonic)
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, 1 year; -20°C, 6 months (protect from light). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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, 1 year; -20°C, 6 months (protect from light). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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 (8.25 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (8.25 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.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: PBS
Solubility: 1 mg/mL (3.30 mM); Clear solution; Need ultrasonic
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.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Purity & Documentation
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Data Sheet (280 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Portuguese - PT (396 KB)
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Handling Instructions (2659 KB)
References
[1]. Lu D, et al. Ethacrynic acid exhibits selective toxicity to chronic lymphocytic leukemia cells by inhibition of the Wnt/beta-catenin pathway. PLoS One. 2009 Dec 14;4(12):e8294. [Content Brief]
[2]. Liang LL, et al. Ethacrynic acid increases facility of outflow in the human eye in vitro. Arch Ophthalmol. 1992 Jan;110(1):106-9. [Content Brief]
[3]. Han Y,et al. Ethacrynic acid inhibits multiple steps in the NF-kappaB signaling pathway. Shock. 2005 Jan;23(1):45-53. [Content Brief]
[4]. Khil MS, et al. Ethacrynic acid: a novel radiation enhancer in human carcinoma cells. Int J Radiat Oncol Biol Phys. 1996 Jan 15;34(2):375-80. [Content Brief]
[5]. Kim Y, et al. In vivo efficacy of the diuretic agent ethacrynic acid against multiple myeloma. Leuk Res. 2012 May;36(5):598-600. [Content Brief]
[6]. Li XQ, et al. Metabolism of Strained Rings: Glutathione S-transferase-Catalyzed Formation of a Glutathione-Conjugated Spiro-azetidine without Prior Bioactivation. Drug Metab Dispos. 2019 Nov;47(11):1247-1256. [Content Brief]
[7]. Harada T, et al. Ethacrynic acid decreases expression of proinflammatory intestinal wall cytokines and ameliorates gastrointestinal stasis in murine postoperative ileus. Clinics (Sao Paulo). 2018 Oct 18;73:e332. [Content Brief]
[8]. Zhao XX, et al. [Ethacrynic acid inhibits airway smooth muscle contraction in mice]. Sheng Li Xue Bao. 2019 Dec 25;71(6):863-873. Chinese. PMID: 31879742. [Content Brief]
[9]. Byun HJ, Kang KJ, Park MK, Lee HJ, Kang JH, Lee EJ, Kim YR, Kim HJ, Kim YW, Jung KC, Kim SY, Lee CH. Ethacrynic Acid Inhibits Sphingosylphosphorylcholine-Induced Keratin 8 Phosphorylation and Reorganization via Transglutaminase-2 Inhibition. Biomol Ther (Seoul). 2013 Sep 30;21(5):338-42. [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, 1 year; -20°C, 6 months (protect from light). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 3.2988 mL | 16.4940 mL | 32.9881 mL | 82.4701 mL |
| 5 mM | 0.6598 mL | 3.2988 mL | 6.5976 mL | 16.4940 mL | |
| 10 mM | 0.3299 mL | 1.6494 mL | 3.2988 mL | 8.2470 mL | |
| 15 mM | 0.2199 mL | 1.0996 mL | 2.1992 mL | 5.4980 mL | |
| 20 mM | 0.1649 mL | 0.8247 mL | 1.6494 mL | 4.1235 mL | |
| 25 mM | 0.1320 mL | 0.6598 mL | 1.3195 mL | 3.2988 mL | |
| 30 mM | 0.1100 mL | 0.5498 mL | 1.0996 mL | 2.7490 mL | |
| 40 mM | 0.0825 mL | 0.4124 mL | 0.8247 mL | 2.0618 mL | |
| 50 mM | 0.0660 mL | 0.3299 mL | 0.6598 mL | 1.6494 mL | |
| 60 mM | 0.0550 mL | 0.2749 mL | 0.5498 mL | 1.3745 mL | |
| 80 mM | 0.0412 mL | 0.2062 mL | 0.4124 mL | 1.0309 mL | |
| DMSO | 100 mM | 0.0330 mL | 0.1649 mL | 0.3299 mL | 0.8247 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.