Talabostat mesylate
Based on 42 publication(s) in Google Scholar
Talabostat mesylate (Val-boroPro mesylate; PT100 mesylate) is an orally active and nonselective dipeptidyl peptidase IV (DPP-IV) inhibitor (IC50 < 4 nM; Ki = 0.18 nM) and the inhibitor of fibroblast activation protein (FAP) (IC50 = 560 nM), inhibits DPP8/9 (IC50 = 4/11 nM; Ki = 1.5/0.76 nM), quiescent cell proline dipeptidase (QPP) (IC50 = 310 nM), DPP2, and some other DASH family enzymes. Antineoplastic and hematopoiesis- stimulating activities.
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- Purity: 98.35%
- CAS No.: 150080-09-4
- 화학식: C10H23BN2O6S
- 분자량:310.18
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보관:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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용액&용해도
- Protocol
- 순도&문서
- References
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Publications Citing Use of MedChemExpress (MCE) Talabostat mesylate
More- Science. 2020 Dec 4;370(6521):eaay2002. [Abstract]
- Cell. 2024 Feb 29;187(5):1223-1237.e16. [Abstract]
- Cell. 2023 May 11;186(10):2144-2159.e22. [Abstract]
- Cancer Commun (Lond). 2024 May;44(5):554-575. [Abstract]
- Cancer Res. 2026 Jan 2;86(1):58-79. [Abstract]
- Cancer Res. 2016 Jul 15;76(14):4124-35. [Abstract]
- Nat Commun. 2019 May 7;10(1):2091. [Abstract]
- Adv Sci (Weinh). 2025 Jan 17:e2409147. [Abstract]
- Adv Sci (Weinh). 2023 Aug;10(24):e2300881. [Abstract]
- J Adv Res. 2025 Aug:74:225-236. [Abstract]
- J Allergy Clin Immunol. 2021 Jun;147(6):2134-2145.e20. [Abstract]
- J Exp Med. 2025 Nov 3;222(11):e20242403. [Abstract]
- J Exp Med. 2022 Oct 3;219(10):e20212117. [Abstract]
- Int J Biol Sci. 2023 Jan 1;19(2):465-483. [Abstract]
- Proc Natl Acad Sci U S A. 2023 Jan 31;120(5):e2213777120. [Abstract]
- Proc Natl Acad Sci U S A. 2019 Sep 17;116(38):19055-19063. [Abstract]
- Cell Rep. 2021 Oct 26;37(4):109904. [Abstract]
- Anal Chem. 2016 Aug 16;88(16):8309-14. [Abstract]
- Sci Signal. 2023 Jan 17;16(768):eabh1083. [Abstract]
- Neurosci Bull. 2025 Jan;41(1):16-32. [Abstract]
- Biochem Pharmacol. 2026 May:247:117801. [Abstract]
- Cells. 2023 Apr 6;12(7):1100. [Abstract]
- CNS Neurosci Ther. 2023 Mar;29(3):878-892. [Abstract]
- Biomolecules. 2024 Mar 25;14(4):391. [Abstract]
- Int Immunopharmacol. 2023 Jul:120:110291. [Abstract]
- Obesity. 2021 Feb;29(2):327-336. [Abstract]
- J Biol Chem. 2018 Dec 7;293(49):18864-18878. [Abstract]
- Ann Surg Oncol. 2020 Oct;27(11):4337-4347. [Abstract]
- J Immunol. 2020 Sep 15;205(6):1653-1663. [Abstract]
- J Diabetes Investig. 2022 Jan;13(1):22-33. [Abstract]
- Iran J Allergy Asthma Immunol. 2021 Mar 17.
- bioRxiv. 2025 Aug 16.
- NPJ Dement. 2025;1(1):3. [Abstract]
- SSRN. 2025 Jan 28.
- Research Square Preprint. 2024 Apr 18.
- bioRxiv. 2023 Nov 4.
- bioRxiv. 2023 Jun 25.
- bioRxiv. 2023 Mar 19.
- bioRxiv. 2023 Jan 17.
- bioRxiv. January 25, 2022.
- Curr Protoc Immunol. 2020 Dec;131(1):e107. [Abstract]
- SSRN. 2020 Jul.
Customer Validation & Images
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ELISA
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In Vivo Efficacy Study
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ELISA
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WB
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Biological Activity
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DPP-4 |
By cleaving N-terminal Xaa-Pro or Xaa-Ala residues, Talabostat mesylate (Val-boroPro mesylate) inhibits dipeptidyl peptidases, such as FAP, resulting in the stimulation of cytokine and chemokine production and specific T-cell immunity and T-cell dependent activity[3].
Talabostat mesylate (Val-boroPro mesylate) competitively inhibits the dipeptidyl peptidase (DPP) activity of FAP and CD26/DPP-IV, and there is a high-affinity interaction with the catalytic site[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 150080-09-4
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Appearance Solid
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분자량 310.18
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화학식 C10H23BN2O6S
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Color White to off-white
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SMILES
CC(C)[C@H](N)C(N1[C@H](B(O)O)CCC1)=O.CS(=O)(O)=O
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Synonyms
Val-boroPro mesylate; PT100 mesylate
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선적
Room temperature in continental US; may vary elsewhere.
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보관
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (42)
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Journal Impact Factor
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Most Recent
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Science
2020 Dec 4;370(6521):eaay2002. PMID: 33093214 -
Cell
2024 Feb 29;187(5):1223-1237.e16. PMID: 38428396
Talabostat mesylate purchased from MedChemExpress. Usage Cited in: Cell. 2024 Feb 29;187(5):1223-1237.e16. [Abstract]
Activation of CARD8 inflammasome by HIV-1 in THP-1 cells. CARD8-KO THP-1 cells expressing wild-type or mutant CARD8 were exposed to HIV reporter virus NL4-3-ΔEnv-EGFP pseudotyped with the VSVG envelope for six hours before LDH. Talabostat mesylate (VbP, 5 μM) was used as a positive control, as it induces cell death and IL-1β secretion.
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Cell
2023 May 11;186(10):2144-2159.e22. PMID: 37172565
Talabostat mesylate purchased from MedChemExpress. Usage Cited in: Cell. 2023 May 11;186(10):2144-2159.e22. [Abstract]
LDH release and IL-1b secretion by ELISA in cell-free supernatants of N/TERT-1 stably expressing mCitrine (control) or bat/human ASC2-mCitrine, treated with Talabostat mesylate (2-200 μM) for 24 h.
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Cancer Commun (Lond)
2024 May;44(5):554-575. PMID: 38507505
Talabostat mesylate purchased from MedChemExpress. Usage Cited in: Cancer Commun (Lond). 2024 May;44(5):554-575. [Abstract]
Talabostat mesylate (20 µg/mouse; i.g.; once daily for 21 days) effectively inhibited tumor growth in BALB/c mice bearing 4T1 cells.
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Cancer Res
SPP1 Drives Colorectal Cancer Liver Metastasis and Immunotherapy Resistance by Stimulating CXCL12 Production in Cancer-Associated Fibroblasts. [Abstract]2026 Jan 2;86(1):58-79. PMID: 41051794 -
Cancer Res
FAP Promotes Immunosuppression by Cancer-Associated Fibroblasts in the Tumor Microenvironment via STAT3-CCL2 Signaling. [Abstract]2016 Jul 15;76(14):4124-35. PMID: 27216177
Talabostat mesylate purchased from MedChemExpress. Usage Cited in: Cancer Res. 2016 Jul 15;76(14):4124-35. [Abstract]
RAW264.7 cells of the indicated genotypes were treated with 4 µM Talabostat mesylate (Val-boroPro) for the indicated times (6-12 h). Cleaved caspase-3 in the cells was detected by Western blotting. The results indicate that Talabostat mesylate can activate caspase‑3 in Gsdmd‑knockout cells.
Talabostat mesylate purchased from MedChemExpress. Usage Cited in: Cancer Res. 2016 Jul 15;76(14):4124-35. [Abstract]
RAW264.7 cells of the indicated genotypes were treated with 4 µM Talabostat mesylate (Val-boroPro) for the indicated times (6-12 h). Microscopic images of the cells. The results showed that Talabostat mesylate induced apoptotic morphological changes in Gsdmd‑knockout cells.
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Nat Commun
2019 May 7;10(1):2091. PMID: 31064994 -
Adv Sci (Weinh)
Intratumoral Collagen Deposition Supports Angiogenesis Suggesting Anti-angiogenic Therapy in Armored and Cold Tumors. [Abstract]2025 Jan 17:e2409147. PMID: 39823457 -
Adv Sci (Weinh)
ANO1-Mediated Inhibition of Cancer Ferroptosis Confers Immunotherapeutic Resistance through Recruiting Cancer-Associated Fibroblasts. [Abstract]2023 Aug;10(24):e2300881. PMID: 37341301 -
J Adv Res
Hippocampal dipeptidyl peptidase 9 bidirectionally regulates memory associated with synaptic plasticity. [Abstract]2025 Aug:74:225-236. PMID: 39369958 -
J Allergy Clin Immunol
NLRP1 variant M1184V decreases inflammasome activation in the context of DPP9 inhibition and asthma severity. [Abstract]2021 Jun;147(6):2134-2145.e20. PMID: 33378691 -
J Exp Med
Discovery of potent and selective inhibitors of human NLRP3 with a novel mechanism of action. [Abstract]2025 Nov 3;222(11):e20242403. PMID: 40892070 -
J Exp Med
2022 Oct 3;219(10):e20212117. PMID: 36129453 -
Int J Biol Sci
BGN/FAP/STAT3 positive feedback loop mediated mutual interaction between tumor cells and mesothelial cells contributes to peritoneal metastasis of gastric cancer. [Abstract]2023 Jan 1;19(2):465-483. PMID: 36632455 -
Proc Natl Acad Sci U S A
Activation of the NLRP1 inflammasome in human keratinocytes by the dsDNA mimetic poly(dA:dT). [Abstract]2023 Jan 31;120(5):e2213777120. PMID: 36693106 -
Proc Natl Acad Sci U S A
Homozygous NLRP1 gain-of-function mutation in siblings with a syndromic form of recurrent respiratory papillomatosis. [Abstract]2019 Sep 17;116(38):19055-19063. PMID: 31484767 -
Cell Rep
2021 Oct 26;37(4):109904. PMID: 34706239 -
Anal Chem
Ultrasensitive Fluorescent Probes Reveal an Adverse Action of Dipeptide Peptidase IV and Fibroblast Activation Protein during Proliferation of Cancer Cells. [Abstract]2016 Aug 16;88(16):8309-14. PMID: 27444320 -
Sci Signal
Tyrosine kinase inhibitors can activate the NLRP3 inflammasome in myeloid cells through lysosomal damage and cell lysis. [Abstract]2023 Jan 17;16(768):eabh1083. PMID: 36649377 -
Neurosci Bull
Time-Dependent Transcriptional Dynamics of Contextual Fear Memory Retrieval Reveals the Function of Dipeptidyl Peptidase 9 in Reconsolidation. [Abstract]2025 Jan;41(1):16-32. PMID: 39621238 -
Biochem Pharmacol
Targeting the FAPα/Integrin αvβ1 complex attenuates hepatic stellate cell activation and liver fibrosis. [Abstract]2026 May:247:117801. PMID: 41687828 -
Cells
DPP8 Selective Inhibitor Tominostat as a Novel and Broad-Spectrum Anticancer Agent against Hematological Malignancies. [Abstract]2023 Apr 6;12(7):1100. PMID: 37048172 -
CNS Neurosci Ther
Anti-cancer effect of targeting fibroblast activation protein alpha in glioblastoma through remodeling macrophage phenotype and suppressing tumor progression. [Abstract]2023 Mar;29(3):878-892. PMID: 36382346 -
Biomolecules
DPP Inhibition Enhances the Efficacy of PD-1 Blockade by Remodeling the Tumor Microenvironment in Lewis Lung Carcinoma Model. [Abstract]2024 Mar 25;14(4):391. PMID: 38672409 -
Int Immunopharmacol
Cisatracurium besylate rescues Mycobacterium Tuberculosis-infected macrophages from necroptosis and enhances the bactericidal effect of isoniazid. [Abstract]2023 Jul:120:110291. PMID: 37182451 -
Obesity
Talabostat Alleviates Obesity and Associated Metabolic Dysfunction via Suppression of Macrophage-Driven Adipose Inflammation. [Abstract]2021 Feb;29(2):327-336. PMID: 33342076 -
J Biol Chem
Human DPP9 represses NLRP1 inflammasome and protects against autoinflammatory diseases via both peptidase activity and FIIND domain binding. [Abstract]2018 Dec 7;293(49):18864-18878. PMID: 30291141
Talabostat mesylate purchased from MedChemExpress. Usage Cited in: J Biol Chem. 2018 Dec 7;293(49):18864-18878. [Abstract]
Lack of evidence for directly binding to NLRP1 by Talabostat. 293T-ASC-GFPNLRP1 cells are treated with 2 μM Talabostat for 16 hours and lysed by 3 rounds of freezing and thawing. 20 μL (2 μg/uL) clarified lysates are heated at a temperature gradient for 10 minutes, centrifuged at 16,000g for 10mins at room temperature.
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Ann Surg Oncol
Dipeptidyl Peptidase 9 Increases Chemoresistance and is an Indicator of Poor Prognosis in Colorectal Cancer. [Abstract]2020 Oct;27(11):4337-4347. PMID: 32734369 -
J Immunol
RIPK3-MLKL-Mediated Neutrophil Death Requires Concurrent Activation of Fibroblast Activation Protein-α. [Abstract]2020 Sep 15;205(6):1653-1663. PMID: 32796025 -
J Diabetes Investig
VX-765 ameliorates renal injury and fibrosis in diabetes by regulating caspase-1-mediated pyroptosis and inflammation. [Abstract]2022 Jan;13(1):22-33. PMID: 34494385 -
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NPJ Dement
Post-symptomatic NLRP3 inhibition rescues cognitive impairment and mitigates amyloid and tau driven neurodegeneration. [Abstract]2025;1(1):3. PMID: 40343261 -
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Curr Protoc Immunol
2020 Dec;131(1):e107. PMID: 33017103 -
용액&용해도
H2O : 250 mg/mL (805.98 mM; Need ultrasonic)
DMSO : ≥ 40 mg/mL (128.96 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* 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 (8.06 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 (8.06 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: 100 mg/mL (322.39 mM); Clear solution; Need ultrasonic
Add each solvent one by one: Saline
Solubility: 50 mg/mL (161.20 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.
Protocol
Mice: BLM (0.5mg/kg/day) is administered on days -7, -6, -5, -2, -1, 0 in the nostrils of male mice. Talabostat (40 µg/mouse) or vehicle (0.9% NaCl) is dosed per os twice daily from day 1-14. MRI is performed before BLM and at days 0, 7 and 14. After the last MRI acquisition, animals are euthanised and the lungs harvested for histological and quantitative real-time polymerase chain reaction (qRT-PCR) analyses[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
순도&문서
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Data Sheet (282 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Lankas GR, et al. Dipeptidyl peptidase IV inhibition for the treatment of type 2 diabetes: potential importance of selectivity over dipeptidyl peptidases 8 and 9. Diabetes. 2005 Oct;54(10):2988-94. [Content Brief]
[2]. Connolly BA, et al. Dipeptide boronic acid inhibitors of dipeptidyl peptidase IV: determinants of potencyand in vivo efficacy and safety. J Med Chem. 2008 Oct 9;51(19):6005-13. [Content Brief]
[3]. Talabostat
[4]. Adams S, et al. PT-100, a small molecule dipeptidyl peptidase inhibitor, has potent antitumor effects and augments antibody-mediated cytotoxicity via a novel immune mechanism. Cancer Res. 2004 Aug 1;64(15):5471-80. [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 (sealed storage, away from moisture). 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 / H2O | 1 mM | 3.2239 mL | 16.1197 mL | 32.2393 mL | 80.5984 mL |
| 5 mM | 0.6448 mL | 3.2239 mL | 6.4479 mL | 16.1197 mL | |
| 10 mM | 0.3224 mL | 1.6120 mL | 3.2239 mL | 8.0598 mL | |
| 15 mM | 0.2149 mL | 1.0746 mL | 2.1493 mL | 5.3732 mL | |
| 20 mM | 0.1612 mL | 0.8060 mL | 1.6120 mL | 4.0299 mL | |
| 25 mM | 0.1290 mL | 0.6448 mL | 1.2896 mL | 3.2239 mL | |
| 30 mM | 0.1075 mL | 0.5373 mL | 1.0746 mL | 2.6866 mL | |
| 40 mM | 0.0806 mL | 0.4030 mL | 0.8060 mL | 2.0150 mL | |
| 50 mM | 0.0645 mL | 0.3224 mL | 0.6448 mL | 1.6120 mL | |
| 60 mM | 0.0537 mL | 0.2687 mL | 0.5373 mL | 1.3433 mL | |
| 80 mM | 0.0403 mL | 0.2015 mL | 0.4030 mL | 1.0075 mL | |
| 100 mM | 0.0322 mL | 0.1612 mL | 0.3224 mL | 0.8060 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.
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