Carvedilol
Based on 14 publication(s) in Google Scholar
Carvedilol (BM 14190) is a non-selective β/α-1 blocker. Carvedilol inhibits lipid peroxidation in a dose-dependent manner with an IC50 of 5 μM. Carvedilol is a multiple action antihypertensive agent with potential use in angina and congestive heart failure. Carvedilol is an autophagy inducer that inhibits the NLRP3 inflammasome.
For research use only. We do not sell to patients.
- Purity: 99.98%
- CAS No.: 72956-09-3
- Formula: C24H26N2O4
- Molecular Weight:406.47
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
Publications Citing Use of MedChemExpress (MCE) Carvedilol
More- Redox Biol. 2024 Dec 21:79:103481. [Abstract]
- Free Radic Biol Med. 2023 Aug 20:205:163-174. [Abstract]
- Cell Rep. 2026 Jun 18;45(7):117570.
- Cell Rep. 2025 Apr 16;44(5):115572. [Abstract]
- Cell Rep. 2023 Mar 20;42(3):112275. [Abstract]
- J Pathol. 2023 Jun;260(2):203-221. [Abstract]
- Cells. 2022 Aug 24;11(17):2633. [Abstract]
- ACS Omega. 2022 Aug 8;7(32):27950-27958. [Abstract]
- Biochim Biophys Acta Mol Basis Dis. 2025 Jun;1871(5):167754. [Abstract]
- J Nat Prod. 2026 Feb 27;89(2):645-655. [Abstract]
- J Diabetes Res. 2024 Nov 23:2024:9378405. [Abstract]
- Cardiooncology. 2025 Nov 13;11(1):106. [Abstract]
- Comput Biol Chem. 2025 Aug:117:108419. [Abstract]
- J Pharm Biomed Anal. 2021 Feb 20:195:113870. [Abstract]
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Cell Imaging/Staining
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RT-PCR
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ELISA
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WB
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IF
All Adrenergic Receptor Isoforms
More
Biological Activity
β/α-1 adrenergic receptor[1]
IC50: 5 μM (lipid peroxidation)[2]
Autophagy[3]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A-375 | IC50 |
13.01 μM
Compound: Carvedilol
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Antiproliferative activity against human A375 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay
Antiproliferative activity against human A375 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay
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[PMID: 32216987] |
| HEK293 | IC50 |
1.6 μM
Compound: 38
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Inhibition of of human TREK1 expressed in HEK293 cells assessed as reduction in channel currents
Inhibition of of human TREK1 expressed in HEK293 cells assessed as reduction in channel currents
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[PMID: 26588045] |
| HEK293 | IC50 |
12 μM
Compound: Carvedilol
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Inhibition of human recombinant UGT1A1 expressed in HEK293 cells assessed as reduction in estradiol 3-glucuronidation by LC-MS/MS method
Inhibition of human recombinant UGT1A1 expressed in HEK293 cells assessed as reduction in estradiol 3-glucuronidation by LC-MS/MS method
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[PMID: 21030469] |
| HEK293 | IC50 |
15.9 μM
Compound: 1
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Inhibition of RyR2 R4496C mutant (unknown origin)-mediated store-overload induced calcium release expressed in HEK293 cells after 8 to 10 mins by fura-2/AM dye-based fluorescence assay
Inhibition of RyR2 R4496C mutant (unknown origin)-mediated store-overload induced calcium release expressed in HEK293 cells after 8 to 10 mins by fura-2/AM dye-based fluorescence assay
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[PMID: 24124794] |
| HEK293 | IC50 |
27 μM
Compound: Carvedilol
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Inhibition of human recombinant UGT1A1 expressed in HEK293 cells assessed as reduction in bilirubin glucuronidation by LC-MS/MS method
Inhibition of human recombinant UGT1A1 expressed in HEK293 cells assessed as reduction in bilirubin glucuronidation by LC-MS/MS method
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[PMID: 21030469] |
| HEK293 | IC50 |
3.4 μM
Compound: Carvedilol
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Inhibition of human OCT1 expressed in HEK293 cells assessed as decrease in uptake of ASP+ after 2 mins by fluorescence assay
Inhibition of human OCT1 expressed in HEK293 cells assessed as decrease in uptake of ASP+ after 2 mins by fluorescence assay
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[PMID: 28230985] |
| HEK293 | IC50 |
7.5 μM
Compound: carvedilol
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Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay
Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay
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[PMID: 23241029] |
| HEK293 | IC50 |
7.6 μM
Compound: 38
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Inhibition of of TREK2 (unknown origin) expressed in HEK293 cells assessed as reduction in channel currents
Inhibition of of TREK2 (unknown origin) expressed in HEK293 cells assessed as reduction in channel currents
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[PMID: 26588045] |
| HEK293 | IC50 |
92.4 μM
Compound: carvedilol
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Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay
Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay
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[PMID: 23241029] |
| L02 | IC50 |
85 μM
Compound: SYSU-20532S
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Cytotoxicity against human LO2 cells assessed as reduction in cell viability after 48 hrs by CCK8 assay
Cytotoxicity against human LO2 cells assessed as reduction in cell viability after 48 hrs by CCK8 assay
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10.1039/C3MD00397C |
| NIH-3T3-G185 | IC50 |
4.6 μM
Compound: Carvedilol
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TP_TRANSPORTER: inhibition of Daunorubicin efflux in NIH-3T3-G185 cells
TP_TRANSPORTER: inhibition of Daunorubicin efflux in NIH-3T3-G185 cells
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[PMID: 11716514] |
| NIH-3T3-G185 | IC50 |
6 μM
Compound: Carvedilol
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TP_TRANSPORTER: inhibition of LDS-751 efflux in NIH-3T3-G185 cells
TP_TRANSPORTER: inhibition of LDS-751 efflux in NIH-3T3-G185 cells
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[PMID: 11716514] |
| NIH-3T3-G185 | IC50 |
6.6 μM
Compound: Carvedilol
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TP_TRANSPORTER: inhibition of Rhodamine 123 efflux in NIH-3T3-G185 cells
TP_TRANSPORTER: inhibition of Rhodamine 123 efflux in NIH-3T3-G185 cells
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[PMID: 11716514] |
| SK-MEL-28 | IC50 |
15.55 μM
Compound: Carvedilol
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Antiproliferative activity against human SK-MEL-28 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay
Antiproliferative activity against human SK-MEL-28 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay
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[PMID: 32216987] |
| SK-MEL-5 | IC50 |
13.73 μM
Compound: Carvedilol
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Antiproliferative activity against human SK-MEL-5 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay
Antiproliferative activity against human SK-MEL-5 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay
|
[PMID: 32216987] |
Superoxide generation by activated human neutrophils in vitro is inhibited by Carvedilol with an IC50 of 28 μM. Carvedilol is shown to scavenge oxygen free radicals in a cell-free system with an IC50 of 25 μM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 72956-09-3
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Appearance Solid
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Molecular Weight 406.47
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Formula C24H26N2O4
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Color White to off-white
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SMILES
OC(CNCCOC1=CC=CC=C1OC)COC2=CC=CC(N3)=C2C4=C3C=CC=C4
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Synonyms
BM 14190
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months
Publications (14)
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Journal Impact Factor
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Most Recent
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Redox Biol
2024 Dec 21:79:103481. PMID: 39721495
Carvedilol purchased from MedChemExpress. Usage Cited in: Redox Biol. 2024 Dec 21:79:103481. [Abstract]
U937 macrophages cultured with or without 5 % CSE were treated with 5 μM, 10 μM, or 20 μM Carvedilol (Carv) for 3 days. LLM formation was determined using ORO staining.
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Free Radic Biol Med
IL-6/gp130/STAT3 signaling contributed to the activation of the PERK arm of the unfolded protein response in response to chronic β-adrenergic stimulation. [Abstract]2023 Aug 20:205:163-174. PMID: 37307935 -
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Cell Rep
2025 Apr 16;44(5):115572. PMID: 40249703
Carvedilol purchased from MedChemExpress. Usage Cited in: Cell Rep. 2025 Apr 16;44(5):115572. [Abstract]
Real-time qPCR measurement of Ifnb1 and Cxcl10 transcripts in mouse peritoneal macrophages treated with cGAMP (1 μg/mL) and Digitonin (10 μg/mL) for indicated times in the presence of DMSO or Carvedilol (10 μM).
Carvedilol purchased from MedChemExpress. Usage Cited in: Cell Rep. 2025 Apr 16;44(5):115572. [Abstract]
ELISA of IFN-β and CXCL10 production in mouse peritoneal macrophages treated with cGAMP or ISD for 12 h in the presence of DMSO or Carvedilol (10 μM).
Carvedilol purchased from MedChemExpress. Usage Cited in: Cell Rep. 2025 Apr 16;44(5):115572. [Abstract]
Immunoblotting of the indicated signaling molecules in mouse peritoneal macrophages treated with cGAMP or ISD in the presence of DMSO or Carvedilol (10 μM) for indicated times.
Carvedilol purchased from MedChemExpress. Usage Cited in: Cell Rep. 2025 Apr 16;44(5):115572. [Abstract]
Carvedilol (10 μM) enhanced HA-STING but not HA-STINGT263A localizing to ERGIC by Immunofluorescence assay.
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Cell Rep
Pharmacological boosting of cGAS activation sensitizes chemotherapy by enhancing antitumor immunity. [Abstract]2023 Mar 20;42(3):112275. PMID: 36943864 -
J Pathol
Novel prognostication biomarker adipophilin reveals a metabolic shift in uveal melanoma and new therapeutic opportunities. [Abstract]2023 Jun;260(2):203-221. PMID: 36825655 -
Cells
Redistribution of the SWI/SNF Complex Dictates Coordinated Transcriptional Control over Epithelial-Mesenchymal Transition of Normal Breast Cells through TGF-β Signaling. [Abstract]2022 Aug 24;11(17):2633. PMID: 36078038 -
ACS Omega
Computational and Experimental Approaches Identify Beta-Blockers as Potential SARS-CoV-2 Spike Inhibitors. [Abstract]2022 Aug 8;7(32):27950-27958. PMID: 35983371 -
Biochim Biophys Acta Mol Basis Dis
Both carvedilol and cimetidine alleviate cisplatin-induced nephrotoxicity via downregulating OCT2. [Abstract]2025 Jun;1871(5):167754. PMID: 40044066 -
J Nat Prod
Spirocyclic Adduct Formation of Tryptanthrin with Indole Monoamines under Biomimetic Acidic Conditions. [Abstract]2026 Feb 27;89(2):645-655. PMID: 41680098 -
J Diabetes Res
2024 Nov 23:2024:9378405. PMID: 39619569 -
Cardiooncology
Breast cancer progression in the presence of treated and untreated left ventricular dysfunction. [Abstract]2025 Nov 13;11(1):106. PMID: 41233850 -
Comput Biol Chem
Targeting quorum sensing in Pseudomonas aeruginosa with high-affinity inhibitors: A high-throughput screening and in-silico analysis. [Abstract]2025 Aug:117:108419. PMID: 40088808 -
J Pharm Biomed Anal
Screening method of mildronate and over 300 doping agents by reversed-phase liquid chromatography-high resolution mass spectrometry. [Abstract]2021 Feb 20:195:113870. PMID: 33453569
Solvent & Solubility
DMSO : 100 mg/mL (246.02 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
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. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
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 (6.15 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 (6.15 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
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.
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.
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 (277 KB)
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SDS (458 KB)
- English - EN (458 KB)
- Français - FR (458 KB)
- Deutsch - DE (458 KB)
- Norwegian - NO (458 KB)
- Español - ES (458 KB)
- Swedish - SV (458 KB)
- Italian - IT (458 KB)
- Korean - KR (458 KB)
- Portuguese - PT (458 KB)
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Handling Instructions (2659 KB)
References
[1]. Eggertsen R, et al. Acute haemodynamic effects of carvedilol (BM 14190), a new combined beta-adrenoceptor blocker and precapillary vasodilating agent, in hypertensive patients. Eur J Clin Pharmacol. 1984;27(1):19-22. [Content Brief]
[2]. Feuerstein GZ, et al. Myocardial protection by the novel vasodilating beta-blocker, carvedilol: potential relevance of anti-oxidant activity. J Hypertens Suppl. 1993 Jun;11(4):S41-8. [Content Brief]
[3]. Wong WT, et al. Repositioning of the β-Blocker Carvedilol as a Novel Autophagy Inducer That Inhibits the NLRP3 Inflammasome. Front Immunol. 2018 Aug 22;9:1920. [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. 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4602 mL | 12.3010 mL | 24.6021 mL | 61.5052 mL |
| 5 mM | 0.4920 mL | 2.4602 mL | 4.9204 mL | 12.3010 mL | |
| 10 mM | 0.2460 mL | 1.2301 mL | 2.4602 mL | 6.1505 mL | |
| 15 mM | 0.1640 mL | 0.8201 mL | 1.6401 mL | 4.1003 mL | |
| 20 mM | 0.1230 mL | 0.6151 mL | 1.2301 mL | 3.0753 mL | |
| 25 mM | 0.0984 mL | 0.4920 mL | 0.9841 mL | 2.4602 mL | |
| 30 mM | 0.0820 mL | 0.4100 mL | 0.8201 mL | 2.0502 mL | |
| 40 mM | 0.0615 mL | 0.3075 mL | 0.6151 mL | 1.5376 mL | |
| 50 mM | 0.0492 mL | 0.2460 mL | 0.4920 mL | 1.2301 mL | |
| 60 mM | 0.0410 mL | 0.2050 mL | 0.4100 mL | 1.0251 mL | |
| 80 mM | 0.0308 mL | 0.1538 mL | 0.3075 mL | 0.7688 mL | |
| 100 mM | 0.0246 mL | 0.1230 mL | 0.2460 mL | 0.6151 mL |