OSS_128167
Based on 31 publication(s) in Google Scholar
OSS_128167 is a potent selective sirtuin 6 (SIRT6) inhibitor with IC50s of 89 μM, 1578 μM and 751 μM for SIRT6, SIRT1 and SIRT2, respectively. OSS_128167 has anti-HBV activity that inhibits HBV transcription and replication. OSS_128167 has anti-cancer, anti-inflammation and anti-viral effects.
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- 純度: 98.92%
- CAS 番号: 887686-02-4
- 分子式: C19H14N2O6
- 分子量:366.32
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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MedChemExpress（MCE）の使用を引用している文献 OSS_128167
More- Signal Transduct Target Ther. 2025 Dec 8;10(1):398. [Abstract]
- Adv Sci (Weinh). 2025 May 8:e2501552. [Abstract]
- Redox Biol. 2025 Dec:88:103939. [Abstract]
- J Neuroinflammation. 2024 Sep 28;21(1):243. [Abstract]
- Acta Pharmacol Sin. 2020 Dec;41(12):1557-1567. [Abstract]
- Phytomedicine. 2025 Jan 17:138:156395. [Abstract]
- Phytomedicine. 2023 Mar:111:154661. [Abstract]
- Phytomedicine. 2022 Sep:104:154276. [Abstract]
- Free Radic Biol Med. 2025 Nov:239:432-448. [Abstract]
- Free Radic Biol Med. 2025 Apr 15:S0891-5849(25)00231-X. [Abstract]
- Cell Death Discov. 2025 Dec 6. [Abstract]
- Clin Transl Med. 2024 Nov;14(11):e70082. [Abstract]
- Cell Biosci. 2021 Dec 14;11(1):210. [Abstract]
- Biochem Pharmacol. 2025 Oct 29;243(Pt 1):117496. [Abstract]
- J Ethnopharmacol. 2024 Aug 2:335:118646. [Abstract]
- Pharm Biol. 2021 Dec;59(1):11-20. [Abstract]
- Front Pharmacol. 2020 Mar 18;11:264. [Abstract]
- Int Immunopharmacol. 2024 Dec 28:146:113932. [Abstract]
- Mol Neurobiol. 2022 Jan;59(1):429-444. [Abstract]
- FASEB J. 2025 May 15;39(9):e70579. [Abstract]
- J Neuroendocrinol. 2024 Dec;36(12):e13448. [Abstract]
- iScience. 2020 Aug 21;23(8):101431. [Abstract]
- Food Chem Toxicol. 2023 Nov:181:114050. [Abstract]
- Naunyn Schmiedebergs Arch Pharmacol. 2024 Nov;397(11):9111-9121. [Abstract]
- Ren Fail. 2024 Dec;46(2):2410396. [Abstract]
- Theriogenology. 2020 Jan 15;142:158-168. [Abstract]
- J Orthop Res. 2023 Nov;41(11):2405-2417. [Abstract]
- bioRxiv. 2025 January 10.
- bioRxiv. 2024 Jul 31:2024.07.31.606047. [Abstract]
- Research Square Preprint. 2023 Nov 20.
- Research Square Preprint. 2020 Jun.
Customer Validation & Images
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WB
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Cell Imaging/Staining
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Cell Proliferation/Viability Assay
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In Vivo Efficacy Study
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Cell Migration/Invasion Assay
生物活性
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SIRT6 89 μM (IC50) |
SIRT2 751 μM (IC50) |
SIRT1 1578 μM (IC50) |
HBV |
OSS_128167 (Compound 9; 100 μM; 0-24 hours; BxPC3 cells) treatment increases H3K9 acetylation. And also increases GLUT-1 expression in BxPC-3 cells[1].
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OSS_128167 (Compound 9) effectively blunts phorbol myristate acetate (PMA)-induced TNF-α secretion in cultured BxPC-3 cells. OSS_128167 increases glucose uptake in cells[1].
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OSS_128167 (100 μM; 96 hours; HepG2.2.15 and HepG2-NTCP cells) treatment significantly decreaseS HBV core DNA and 3.5-Kb RNA levels. OSS_128167 treatment also inhibits hepatitis B surface antigen (HBsAg) and hepatitis B envelope antigen (HBeAg) secretions, as well as HBsAg expression in cell lysates[2].
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OSS_128167 (200 μM) induces chemosensitization in primary multiple myeloma (MM) cells (NCI-H929), as well as in melphalan-resistant (LR-5) and doxorubicin-resistant (Dox40) MM cell lines[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:BxPC3 cells
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Concentration:100 µM
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Incubation Time:0 hours, 2 hours, 6 hours, 18 hours, 24 hours
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Result:Increased H3K9 acetylation.
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Cell Line:HepG2.2.15 and HepG2-sodium taurocholate cotransporting polypeptide (NTCP) cells
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Concentration:100 µM
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Incubation Time:96 hours
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Result:Significantly decreased HBV core DNA and 3.5-Kb RNA levels.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male HBV transgenic mice (6-8-week-old)[2]
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Dosage:50 mg/kg
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Administration:Intraperitoneal injection; every 4 days; for 12 days
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Result:The level of HBV DNA and 3.5-Kb RNA were markedly suppressed in HBV transgenic mice.
化学情報
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CAS 番号 887686-02-4
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性状 Solid
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分子量 366.32
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分子式 C19H14N2O6
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Color White to light yellow
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SMILES
O=C(C1=CC(NC(C2=CC=CO2)=O)=CC=C1)NC3=CC(C(O)=O)=C(O)C=C3
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months
Publications (31)
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Journal Impact Factor
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Most Recent
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Signal Transduct Target Ther
Lysophosphatidylethanolamine 18:1 drives clear cell renal cell carcinoma by stabilizing SIRT6 to reprogram lipid metabolism. [Abstract]2025 Dec 8;10(1):398. PMID: 41354870
OSS_128167 purchased from MedChemExpress. Usage Cited in: Signal Transduct Target Ther. 2025 Dec 8;10(1):398. [Abstract]
Western blot analysis of SIRT6 and ACAT2 expression in 786-O cells treated with OSS-128167 (OSS, 100 μM, 24 h), LPE18:1 (40 μM, 24 h), or both.
OSS_128167 purchased from MedChemExpress. Usage Cited in: Signal Transduct Target Ther. 2025 Dec 8;10(1):398. [Abstract]
Lipid staining confirmed that OSS-128167 (100 μM) treatment significantly inhibited LPE18:1-induced or SIRT6 overexpression-promoted lipid accumulation.
OSS_128167 purchased from MedChemExpress. Usage Cited in: Signal Transduct Target Ther. 2025 Dec 8;10(1):398. [Abstract]
Colony formation experiments revealed that OSS-128167 (100 μM) reversed the stimulatory effects of LPE18:1 or CAPZA1 overexpression on colony formation.
OSS_128167 purchased from MedChemExpress. Usage Cited in: Signal Transduct Target Ther. 2025 Dec 8;10(1):398. [Abstract]
Tumor growth curves of nude mice that were subcutaneously injected with CAPZA1-depleted or control 786-O cells and treated with OSS-128167 (50 mg/kg) or vehicle every 7 days for 21 days.
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Adv Sci (Weinh)
Fn14 Controls the SIRT2-Mediated Deacetylation of Slug to Inhibit the Metastasis of Epithelial Ovarian Cancer. [Abstract]2025 May 8:e2501552. PMID: 40344622 -
Redox Biol
Melatonin attenuates atherosclerotic plaque vulnerability through SIRT6-dependent regulation of vascular smooth muscle cells senescence. [Abstract]2025 Dec:88:103939. PMID: 41308252 -
J Neuroinflammation
SIRT6 modulates lesion microenvironment in LPC induced demyelination by targeting astrocytic CHI3L1. [Abstract]2024 Sep 28;21(1):243. PMID: 39342313 -
Acta Pharmacol Sin
Downregulation of hippocampal SIRT6 activates AKT/CRMP2 signaling and ameliorates chronic stress-induced depression-like behavior in mice. [Abstract]2020 Dec;41(12):1557-1567. PMID: 32265492 -
Phytomedicine
Qige Decoction attenuated non-alcoholic fatty liver disease through regulating SIRT6-PPARα-mediated fatty acid oxidation. [Abstract]2025 Jan 17:138:156395. PMID: 39855055 -
Phytomedicine
Diosgenin attenuates non-alcoholic fatty liver disease in type 2 diabetes through regulating SIRT6-related fatty acid uptake. [Abstract]2023 Mar:111:154661. PMID: 36682299 -
Phytomedicine
Diosgenin protects against podocyte injury in early phase of diabetic nephropathy through regulating SIRT6. [Abstract]2022 Sep:104:154276. PMID: 35728388 -
Free Radic Biol Med
Hyperactivation of the m6A demethylase FTO to down-regulate SLC7A11/xCT-mediated redox homeostasis and epigenetic remodeling in facial infiltrating lipomatosis. [Abstract]2025 Nov:239:432-448. PMID: 40769313 -
Free Radic Biol Med
Nicotinamide mononucleotide mitigates hyperoxia-aggravated septic lung injury via the GPx4-mediated anti-ferroptosis signaling pathway in alveolar epithelial cells. [Abstract]2025 Apr 15:S0891-5849(25)00231-X. PMID: 40246251 -
Cell Death Discov
2025 Dec 6. PMID: 41353172 -
Clin Transl Med
Targeting endoplasmic reticulum stress-induced lymphatic dysfunction for mitigating bisphosphonate-related osteonecrosis. [Abstract]2024 Nov;14(11):e70082. PMID: 39521624 -
Cell Biosci
SIRT6 inhibition delays peripheral nerve recovery by suppressing migration, phagocytosis and M2-polarization of macrophages. [Abstract]2021 Dec 14;11(1):210. PMID: 34906231
OSS_128167 purchased from MedChemExpress. Usage Cited in: Cell Biosci. 2021 Dec 14;11(1):210. [Abstract]
Transwell assay: the migrated macrophages in the Vehicle group and OSS_128167 (200 μM) treated group.
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Biochem Pharmacol
2025 Oct 29;243(Pt 1):117496. PMID: 41173054 -
J Ethnopharmacol
Specnuezhenide ameliorates hepatic fibrosis via regulating SIRT6-Mediated inflammatory signaling cascades. [Abstract]2024 Aug 2:335:118646. PMID: 39097210 -
Pharm Biol
α-Hederin inhibits the growth of lung cancer A549 cells in vitro and in vivo by decreasing SIRT6 dependent glycolysis. [Abstract]2021 Dec;59(1):11-20. PMID: 33356727 -
Front Pharmacol
Isoorientin Attenuates Cisplatin-Induced Nephrotoxicity Through the Inhibition of Oxidative Stress and Apoptosis via Activating the SIRT1/SIRT6/Nrf-2 Pathway. [Abstract]2020 Mar 18;11:264. PMID: 32256355 -
Int Immunopharmacol
SIRT6 knockdown alleviates keratinocyte hyperproliferation and inflammation in psoriasis via modulating acetylation of FOXO1. [Abstract]2024 Dec 28:146:113932. PMID: 39733643 -
Mol Neurobiol
SIRT6 Negatively Regulates Schwann Cells Dedifferentiation via Targeting c-Jun During Wallerian Degeneration After Peripheral Nerve Injury. [Abstract]2022 Jan;59(1):429-444. PMID: 34708329 -
FASEB J
PRMT1 Upregulates SIRT6 by Enhancing Arginine Methylation of E2F7 to Inhibit Vascular Smooth Muscle Cell Senescence in Aortic Dissection. [Abstract]2025 May 15;39(9):e70579. PMID: 40298071 -
J Neuroendocrinol
The role of NMDA receptors in fish stress response: Assessments based on physiology of the caudal neurosecretory system and defensive behavior. [Abstract]2024 Dec;36(12):e13448. PMID: 39351903 -
iScience
BxPC-3-Derived Small Extracellular Vesicles Induce FOXP3+ Treg through ATM-AMPK-Sirtuins-Mediated FOXOs Nuclear Translocations. [Abstract]2020 Aug 21;23(8):101431. PMID: 32798974 -
Food Chem Toxicol
Oridonin ameliorates doxorubicin induced-cardiotoxicity via the E2F1/Sirt6/PGC1α pathway in mice. [Abstract]2023 Nov:181:114050. PMID: 37734463 -
Naunyn Schmiedebergs Arch Pharmacol
Gastrodin prevents myocardial injury in sleep-deprived mice by suppressing ferroptosis through SIRT6. [Abstract]2024 Nov;397(11):9111-9121. PMID: 38896272 -
Ren Fail
Sirt6 ameliorates high glucose-induced podocyte cytoskeleton remodeling via the PI3K/AKT signaling pathway. [Abstract]2024 Dec;46(2):2410396. PMID: 39378103 -
Theriogenology
Cumulus cell-derived and maternal SIRT6 differentially regulates porcine oocyte meiotic maturation. [Abstract]2020 Jan 15;142:158-168. PMID: 31593883 -
J Orthop Res
Orientin inhibits inflammation in chondrocytes and attenuates osteoarthritis through Nrf2/NF-κB and SIRT6/NF-κB pathway. [Abstract]2023 Nov;41(11):2405-2417. PMID: 37186383 -
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bioRxiv
2024 Jul 31:2024.07.31.606047. PMID: 39211154 -
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溶剤 & 溶解度
DMSO : 100 mg/mL (272.99 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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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: ≥ 2.08 mg/mL (5.68 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
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: 0.5% CMC-Na/saline water
Solubility: 10 mg/mL (27.30 mM); Suspended 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.
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.
純度とドキュメンテーション
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データシート (281 KB)
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SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Portuguese - PT (392 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Parenti MD, et al. Discovery of novel and selective SIRT6 inhibitors. J Med Chem. 2014 Jun 12;57(11):4796-804. [Content Brief]
[2]. Jiang H, et al. SIRT6 Inhibitor, OSS_128167 Restricts Hepatitis B Virus Transcription and Replication Through Targeting Transcription Factor Peroxisome Proliferator-Activated Receptors α. Front Pharmacol. 2019 Oct 25;10:1270. [Content Brief]
[3]. Cea M, et al. Evidence for a role of the histone deacetylase SIRT6 in DNA damage response of multiple myeloma cells. Blood. 2016 Mar 3;127(9):1138-50. [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 | 2.7299 mL | 13.6493 mL | 27.2985 mL | 68.2463 mL |
| 5 mM | 0.5460 mL | 2.7299 mL | 5.4597 mL | 13.6493 mL | |
| 10 mM | 0.2730 mL | 1.3649 mL | 2.7299 mL | 6.8246 mL | |
| 15 mM | 0.1820 mL | 0.9100 mL | 1.8199 mL | 4.5498 mL | |
| 20 mM | 0.1365 mL | 0.6825 mL | 1.3649 mL | 3.4123 mL | |
| 25 mM | 0.1092 mL | 0.5460 mL | 1.0919 mL | 2.7299 mL | |
| 30 mM | 0.0910 mL | 0.4550 mL | 0.9100 mL | 2.2749 mL | |
| 40 mM | 0.0682 mL | 0.3412 mL | 0.6825 mL | 1.7062 mL | |
| 50 mM | 0.0546 mL | 0.2730 mL | 0.5460 mL | 1.3649 mL | |
| 60 mM | 0.0455 mL | 0.2275 mL | 0.4550 mL | 1.1374 mL | |
| 80 mM | 0.0341 mL | 0.1706 mL | 0.3412 mL | 0.8531 mL | |
| 100 mM | 0.0273 mL | 0.1365 mL | 0.2730 mL | 0.6825 mL |
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