GSK1016790A
Based on 38 publication(s) in Google Scholar
GSK1016790A is a potent and selective transient receptor potential vanilloid 4 (TRPV4) channel agonist. GSK1016790A can elicit Ca2+ influx and elevate intracellular Ca2+ in HEK cells.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity: 99.93%
- CAS No.: 942206-85-1
- 화학식: C28H32Cl2N4O6S2
- 분자량:655.61
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) GSK1016790A
More- Signal Transduct Target Ther. 2025 Nov 28;10(1):388. [Abstract]
- Nat Immunol. 2026 May;27(5):949-960. [Abstract]
- Adv Mater. 2025 May 9:e2417734. [Abstract]
- Nat Commun. 2025 Sep 29;16(1):8541. [Abstract]
- Adv Sci (Weinh). 2024 Apr 24:e2401583. [Abstract]
- Chem Eng J. 2025 Nov 19.
- Cell Discov. 2024 Nov 12;10(1):114. [Abstract]
- Cell Death Dis. 2023 Jun 28;14(6):379. [Abstract]
- Acta Pharmacol Sin. 2023 Apr;44(4):811-821. [Abstract]
- Br J Pharmacol. 2025 Nov 2. [Abstract]
- Br J Pharmacol. 2022 May;179(10):2297-2312. [Abstract]
- Antioxidants (Basel). 2022 Nov 23;11(12):2315. [Abstract]
- J Agric Food Chem. 2025 Jul 23;73(29):18153-18164. [Abstract]
- JCI Insight. 2026 Jan 23;11(2):e182439. [Abstract]
- Transl Res. 2024 Apr:266:16-31. [Abstract]
- Acta Physiol. 2023 Apr;237(4):e13926. [Abstract]
- Acs Biomater Sci Eng. 2019 Dec 9;5(12):6520-6529. [Abstract]
- J Ethnopharmacol. 2022 May 23:290:115105. [Abstract]
- Front Pharmacol. 2021 Jul 14:12:684538. [Abstract]
- Exp Neurol. 2023 Jun:364:114392. [Abstract]
- J Cell Physiol. 2023 Nov;238(11):2692-2709. [Abstract]
- Cell Calcium. 2022 Jun;104:102590. [Abstract]
- Sci Rep. 2025 Nov 24;15(1):41644. [Abstract]
- J Biol Chem. 2022 May;298(5):101847. [Abstract]
- Cell Signal. 2024 Feb:114:110973. [Abstract]
- Exp Cell Res. 2025 Apr 1;447(1):114515. [Abstract]
- Mol Hum Reprod. 2022 Feb 4;28(2):gaac001. [Abstract]
- Am J Physiol Lung Cell Mol Physiol. 2020 Apr 1;318(4):L723-L741. [Abstract]
- J Cancer. 2025 Jan 13;16(4):1324-1334. [Abstract]
- J Leukoc Biol. 2023 Sep 1;114(3):266-279. [Abstract]
- Pain Res Manag. 2025 Aug 6:2025:3697374. [Abstract]
- Ultrasound Med Biol. 2025 Mar;51(3):494-507. [Abstract]
- J Cardiovasc Transl Res. 2023 Apr;16(2):414-426. [Abstract]
- Biomed Res Int. 2022 Jan 4:2022:2777882. [Abstract]
- SSRN. 2025 Dec 12.
- SSRN. 2025 Oct 29.
- bioRxiv. 2024 November 26.
- SSRN. 2024 Jan 22.
Customer Validation & Images
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Others
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Cell Migration/Invasion Assay
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WB
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Flow Cytometry
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WB
All Calcium Channel Isoforms
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Biological Activity
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TRPV4 |
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Cell Line
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Type | Value | Description | References |
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| HEK293 | EC50 |
49 nM
Compound: 1; GSK1016790A
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Agonist activity at recombinant human TRPV4 expressed in HEK293 cells assessed as increase in intracellular calcium level after 30 mins by Fura-2 AM/Pluronic F-127 probe based fluorescence assay
Agonist activity at recombinant human TRPV4 expressed in HEK293 cells assessed as increase in intracellular calcium level after 30 mins by Fura-2 AM/Pluronic F-127 probe based fluorescence assay
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[PMID: 30629441] |
GSK1016790A (0.1-1000 nM) elicits Ca2+ influx in mouse and human TRPV4-expressing human embryonic kidney (HEK) cells (EC50 values of 18 and 2.1 nM, respectively) and it evokes a dose-dependent activation of TRPV4 whole-cell currents at concentrations above 1 nM. GSK1016790A (100 nM) treatment elicits a rapid elevation of intracellular Ca2+ in a subset of neurons[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
GSK1016790A (0.1-1000 nM; pretreatment 10 min) significantly inhibits the electrical field stimulation (EFS)-induced twitch contractions in isolated mouse colon strips in a concentration-dependent manner[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:S100β-GFP and TRPV4 knockout (TRPV4-/-) mice[2]
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Dosage:0.001, 0.01, 0.1 mg/kg
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Administration:IP; single dose
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Result:Produced a dose-dependent inhibitory effect on whole gut transit time in mice.
Produced a dose-dependent and time-dependent inhibitory effect on colonic expulsion.
Chemical Information
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CAS No. 942206-85-1
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Appearance Solid
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분자량 655.61
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화학식 C28H32Cl2N4O6S2
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Color White to off-white
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SMILES
O=C(C1=CC2=CC=CC=C2S1)N[C@H](C(N3CCN(C([C@@H](NS(=O)(C4=CC=C(Cl)C=C4Cl)=O)CO)=O)CC3)=O)CC(C)C
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (38)
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Journal Impact Factor
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Most Recent
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Signal Transduct Target Ther
Pulsed electromagnetic fields inhibit atherosclerosis by regulating pyroptosis through membrane tension-mediated mechanosensitive channels. [Abstract]2025 Nov 28;10(1):388. PMID: 41309549
GSK1016790A purchased from MedChemExpress. Usage Cited in: Signal Transduct Target Ther. 2025 Nov 28;10(1):388. [Abstract]
HC067047 (100 nM, transient administration) blocked both GSK1016790A (80 nM,transient administration) -evoked inward and outward transmembrane currents in HUVEC cells.
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Nat Immunol
Lipid asymmetry disruption by XKR8 orchestrates neutrophil extracellular trap formation and inhibits fungal infection. [Abstract]2026 May;27(5):949-960. PMID: 41781710 -
Adv Mater
A Highly Adaptable Hydrogen Bond Re-Orientation (HyBRO) Strategy for Multiscale Vasculature Fabrication. [Abstract]2025 May 9:e2417734. PMID: 40344457 -
Nat Commun
Biomimetic organo-hydrogels reveal the adipose tissue local mechanical anisotropy regulates ovarian cancer invasion. [Abstract]2025 Sep 29;16(1):8541. PMID: 41022685 -
Adv Sci (Weinh)
2024 Apr 24:e2401583. PMID: 38659239 -
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Cell Discov
Cancer cells sense solid stress to enhance metastasis by CKAP4 phase separation-mediated microtubule branching. [Abstract]2024 Nov 12;10(1):114. PMID: 39528501 -
Cell Death Dis
Inhibition of TRPV4 remodels single cell polarity and suppresses the metastasis of hepatocellular carcinoma. [Abstract]2023 Jun 28;14(6):379. PMID: 37369706
GSK1016790A purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2023 Jun 28;14(6):379. [Abstract]
MHCC-97H and HCC-LM3 cells were treated with 4 μM GSK1016790A or 8 μM HC067047 for 24 h. Transwell migration assay without Matrigel matrix was detected and the number of transmigrated cells were quantified. Scale bar: 200 μm.
GSK1016790A purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2023 Jun 28;14(6):379. [Abstract]
GSK1016790A (2-8 μM, 24 h). The expression of cytoskeleton-related proteins was measured by western blot.
GSK1016790A purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2023 Jun 28;14(6):379. [Abstract]
The MHCC-97H cells were stimulated with 16 μM GSK1016790A for a brief period of time, and the calcium ion fluorescence intensity was acquired by flow cytometry analysis.
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Acta Pharmacol Sin
TRPV4 channel is involved in HSV-2 infection in human vaginal epithelial cells through triggering Ca2+ oscillation. [Abstract]2023 Apr;44(4):811-821. PMID: 36151392 -
Br J Pharmacol
ATP release and metabolism by human and guinea pig airways and P2X receptor-dependent effects on bronchopulmonary vagal afferent nerve subtypes. [Abstract]2025 Nov 2. PMID: 41178173 -
Br J Pharmacol
2022 May;179(10):2297-2312. PMID: 34822720 -
Antioxidants (Basel)
Blocking TRPV4 Ameliorates Osteoarthritis by Inhibiting M1 Macrophage Polarization via the ROS/NLRP3 Signaling Pathway. [Abstract]2022 Nov 23;11(12):2315. PMID: 36552524 -
J Agric Food Chem
2025 Jul 23;73(29):18153-18164. PMID: 40662381 -
JCI Insight
2026 Jan 23;11(2):e182439. PMID: 41574606 -
Transl Res
TRPV4 in adipose tissue ameliorates diet-induced obesity by promoting white adipocyte browning. [Abstract]2024 Apr:266:16-31. PMID: 37926276 -
Acta Physiol
2023 Apr;237(4):e13926. PMID: 36606511 -
Acs Biomater Sci Eng
Cation Channel Transient Receptor Potential Vanilloid 4 Mediates Topography-Induced Osteoblastic Differentiation of Bone Marrow Stem Cells. [Abstract]2019 Dec 9;5(12):6520-6529. PMID: 33417804
GSK1016790A purchased from MedChemExpress. Usage Cited in: Acs Biomater Sci Eng. 2019 Dec 9;5(12):6520-6529. [Abstract]
Protein levels of NFATc1 in nuclei of BMSCs cultured on various surfaces with or without GSK101 and RN-1734.
GSK1016790A purchased from MedChemExpress. Usage Cited in: Acs Biomater Sci Eng. 2019 Dec 9;5(12):6520-6529. [Abstract]
Effects of TRPV4 on NFATc1 nuclear localization in BMSCs on MNTs. Micrographs stained for NFATc1 of BMSCs cultured for 7d on (A) PT, (B) PT with TRPV4 agonist (GSK101) , (C) TNT-30, (D)TNT-100, (E) TNT-100 with TRPV4 antagonist (RN-1734). Red fluorescence: NFATc1; Blue fluorescence: nucleus.
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J Ethnopharmacol
Magnolol and honokiol target TRPC4 to regulate extracellular calcium influx and relax intestinal smooth muscle. [Abstract]2022 May 23:290:115105. PMID: 35157953 -
Front Pharmacol
Role of Serosal TRPV4-Constituted SOCE Mechanism in Secretagogues-Stimulated Intestinal Epithelial Anion Secretion. [Abstract]2021 Jul 14:12:684538. PMID: 34335254 -
Exp Neurol
Activation of TRPV4 induces intraneuronal tau hyperphosphorylation via cholesterol accumulation. [Abstract]2023 Jun:364:114392. PMID: 36990137 -
J Cell Physiol
Simulated microgravity-induced oxidative stress and loss of osteogenic potential of osteoblasts can be prevented by protection of primary cilia. [Abstract]2023 Nov;238(11):2692-2709. PMID: 37796139 -
Cell Calcium
Blockage of transient receptor potential vanilloid 4 prevents postoperative atrial fibrillation by inhibiting NLRP3-inflammasome in sterile pericarditis mice. [Abstract]2022 Jun;104:102590. PMID: 35439615 -
Sci Rep
The TRPV4-YAP axis mediates cytoskeletal and extracellular matrix remodeling in trabecular meshwork cells as a novel glaucoma mechanism. [Abstract]2025 Nov 24;15(1):41644. PMID: 41286165 -
J Biol Chem
Capsaicin inhibits intestinal Cl- secretion and promotes Na+ absorption by blocking TRPV4 channels in healthy and colitic mice. [Abstract]2022 May;298(5):101847. PMID: 35314195 -
Cell Signal
TRPV4 blockade alleviates endoplasmic reticulum stress mediated apoptosis in hypoxia-induced cardiomyocyte injury. [Abstract]2024 Feb:114:110973. PMID: 37981067 -
Exp Cell Res
Investigating the effects of TRPV4 and Cav1.2 channels in 3D culture for promoting the differentiation of BMSCs at various stages. [Abstract]2025 Apr 1;447(1):114515. PMID: 40073957 -
Mol Hum Reprod
Activation of TRPV4 stimulates transepithelial K+ secretion in rat epididymal epithelium. [Abstract]2022 Feb 4;28(2):gaac001. PMID: 35040999 -
Am J Physiol Lung Cell Mol Physiol
Adipose-derived exosomes protect the pulmonary endothelial barrier in ventilator-induced lung injury by inhibiting the TRPV4/Ca2+ signaling pathway. [Abstract]2020 Apr 1;318(4):L723-L741. PMID: 32073873 -
J Cancer
Matrix stiffness regulates NPC invasiveness by modulating a mechanoresponsive TRPV4-Nox4-IL-8 signaling axis. [Abstract]2025 Jan 13;16(4):1324-1334. PMID: 39895789 -
J Leukoc Biol
Transient receptor potential vanilloid 4 (TRPV4) in neutrophils enhances myocardial ischemia/reperfusion injury. [Abstract]2023 Sep 1;114(3):266-279. PMID: 37232941 -
Pain Res Manag
Tuina Alleviates Neuropathic Pain in CCI Rats by Regulating the TRPV4-CaMKII Signaling Pathway in Dorsal Root Ganglion. [Abstract]2025 Aug 6:2025:3697374. PMID: 40809812 -
Ultrasound Med Biol
2025 Mar;51(3):494-507. PMID: 39632209 -
J Cardiovasc Transl Res
Roles of TRPV4 in Regulating Circulating Angiogenic Cells to Promote Coronary Microvascular Regeneration. [Abstract]2023 Apr;16(2):414-426. PMID: 36103035 -
Biomed Res Int
Role of TRPV4 in the Diagnosis and Treatment of Helicobacter pylori Infection in Children with Duodenal Ulcers. [Abstract]2022 Jan 4:2022:2777882. PMID: 35028313 -
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용액&용해도
Methanol : 50 mg/mL (76.26 mM; Need ultrasonic)
DMSO : ≥ 33 mg/mL (50.33 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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 (3.81 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 (3.81 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.
순도&문서
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Data Sheet (276 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)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Kevin S Thorneloe, et al. N-((1S)-1-{[4-((2S)-2-{[(2,4-dichlorophenyl)sulfonyl]amino}-3-hydroxypropanoyl)-1-piperazinyl]carbonyl}-3-methylbutyl)-1-benzothiophene-2-carboxamide (GSK1016790A), a novel and potent transient receptor potential vanilloid 4 channel agonist induces urinary bladder contraction and hyperactivity: Part I. J Pharmacol Exp Ther. 2008 Aug;326(2):432-42. [Content Brief]
[2]. J Fichna, et al. Transient receptor potential vanilloid 4 inhibits mouse colonic motility by activating NO-dependent enteric neurotransmission. J Mol Med (Berl). 2015 Dec;93(12):1297-309. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO / Methanol | 1 mM | 1.5253 mL | 7.6265 mL | 15.2530 mL | 38.1324 mL |
| 5 mM | 0.3051 mL | 1.5253 mL | 3.0506 mL | 7.6265 mL | |
| 10 mM | 0.1525 mL | 0.7626 mL | 1.5253 mL | 3.8132 mL | |
| 15 mM | 0.1017 mL | 0.5084 mL | 1.0169 mL | 2.5422 mL | |
| 20 mM | 0.0763 mL | 0.3813 mL | 0.7626 mL | 1.9066 mL | |
| 25 mM | 0.0610 mL | 0.3051 mL | 0.6101 mL | 1.5253 mL | |
| 30 mM | 0.0508 mL | 0.2542 mL | 0.5084 mL | 1.2711 mL | |
| 40 mM | 0.0381 mL | 0.1907 mL | 0.3813 mL | 0.9533 mL | |
| 50 mM | 0.0305 mL | 0.1525 mL | 0.3051 mL | 0.7626 mL | |
| Methanol | 60 mM | 0.0254 mL | 0.1271 mL | 0.2542 mL | 0.6355 mL |
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