Bazedoxifene
Based on 17 publication(s) in Google Scholar
Bazedoxifene (TSE-424) is an oral, BBB-penetrant nonsteroidal selective estrogen receptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene can be used for the research of osteoporosis. Bazedoxifene also acts as an inhibitor of IL-6/GP130 protein-protein interactions and can be used for the research of pancreatic cancer.
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- Pureza: 99.06%
- No. CAS: 198481-32-2
- Fòrmula: C30H34N2O3
- Peso molecular:470.60
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Bazedoxifene
More- Nat Commun. 2026 Apr 1;17(1):4716. [Abstract]
- Free Radic Biol Med. 2023 Aug 20:205:163-174. [Abstract]
- J Med Chem. 2020 Oct 8;63(19):11085-11099. [Abstract]
- Glia. 2023 Feb;71(2):284-304. [Abstract]
- Eur J Pharmacol. 2023 May 15:947:175681. [Abstract]
- Cell Rep Methods. 2023 Oct 23;3(10):100599. [Abstract]
- iScience. 2026 Feb 6;29(3):114931. [Abstract]
- Gynecol Oncol. 2019 Jul;154(1):199-206. [Abstract]
- Sci Rep. 2026 Mar 17. [Abstract]
- mSphere. 2020 Apr 8;5(2):e00124-20. [Abstract]
- Arch Biochem Biophys. 2025 Jun:768:110366. [Abstract]
- Breast Cancer Res Treat. 2020 Jan;179(1):67-77. [Abstract]
- J Cell Biochem. 2023 Sep;124(9):1404-1422. [Abstract]
- University of Colorado Denver. 2024.
- biorxiv. 2024 May 21.
- Research Square Preprint. 2022 Jul.
- Res Sq. 2020 Dec 31:rs.3.rs-100914. [Abstract]
Actividad biológica
IC50: 26 nM (ERα), 99 nM (ERβ)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
38.48 μM
Compound: Baz
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Cytotoxicity against human HEK293 cells incubated for 48 hrs by MTT assay
Cytotoxicity against human HEK293 cells incubated for 48 hrs by MTT assay
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[PMID: 38665833] |
| HeLa | IC50 |
3.43 μM
Compound: Bazedoxifene
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Inhibition of Ebolavirus glycoprotein/matrix protein VP40 entry in human HeLa cells after 4.5 hrs beta-lactamase reporter assay
Inhibition of Ebolavirus glycoprotein/matrix protein VP40 entry in human HeLa cells after 4.5 hrs beta-lactamase reporter assay
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[PMID: 29624387] |
| MCF7 | IC50 |
0.4 nM
Compound: 3
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Antiproliferative activity against human breast cancer MCF7 cell line in presence of 0.003 nM estradiol
Antiproliferative activity against human breast cancer MCF7 cell line in presence of 0.003 nM estradiol
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[PMID: 16203138] |
| MCF7 | IC50 |
3.7 nM
Compound: 7 ; TSE-424
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In vitro antagonist effect on estrogen receptor alpha transcriptional activation in MCF-7 cells against 10 pM 17-beta-estradiol
In vitro antagonist effect on estrogen receptor alpha transcriptional activation in MCF-7 cells against 10 pM 17-beta-estradiol
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[PMID: 11356100] |
| MCF7 | IC50 |
7.31 μM
Compound: Baz
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Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
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[PMID: 38665833] |
| MDA-MB-231 | IC50 |
6.73 μM
Compound: Baz
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Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
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[PMID: 38665833] |
| MDA-MB-231 | IC50 |
7.45 μM
Compound: 60; TSE-424
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Anticancer activity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay
Anticancer activity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay
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[PMID: 33650861] |
| MDA-MB-468 | IC50 |
3.14 μM
Compound: 60; TSE-424
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Anticancer activity against human MDA-MB-468 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay
Anticancer activity against human MDA-MB-468 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay
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[PMID: 33650861] |
| MH60 | IC50 |
3.8 μM
Compound: 2
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Cytotoxicity in mouse MH60 cells assessed as inhibition of recombinant human IL-6-induced growth incubated for 72 hrs by tetrazolium method
Cytotoxicity in mouse MH60 cells assessed as inhibition of recombinant human IL-6-induced growth incubated for 72 hrs by tetrazolium method
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[PMID: 36971365] |
| MIA PaCa-2 | IC50 |
9.7 μM
Compound: Bazedoxifene
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Cytotoxicity against human MIAPaCa2 cells assessed as cell viability
Cytotoxicity against human MIAPaCa2 cells assessed as cell viability
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[PMID: 24456369] |
| SUM-159-PT | IC50 |
24.9 μM
Compound: Bazedoxifene
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Cytotoxicity against ER-negative human SUM159 cells assessed as cell viability after 72 hrs by MTT assay in presence of IL-6
Cytotoxicity against ER-negative human SUM159 cells assessed as cell viability after 72 hrs by MTT assay in presence of IL-6
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[PMID: 24456369] |
| T47D | IC50 |
14.23 μM
Compound: Baz
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Antiproliferative activity against human T47D cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
Antiproliferative activity against human T47D cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
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[PMID: 38665833] |
| T47D | IC50 |
16.43 μM
Compound: Bazedoxifene
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Antiproliferative activity against human T47D cells after 48 hrs by MTT assay
Antiproliferative activity against human T47D cells after 48 hrs by MTT assay
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[PMID: 29198894] |
| Vero | CC50 |
14.97 μM
Compound: Bazedoxifene
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Cell viability measured by CellTiter-Glo assay in Vero cells at MOI 0.05 after 72hr
Cell viability measured by CellTiter-Glo assay in Vero cells at MOI 0.05 after 72hr
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10.1101/2020.03.20.999730 |
| Vero | IC50 |
3.44 μM
Compound: Bazedoxifene
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Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr
Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr
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10.1101/2020.03.20.999730 |
Bazedoxifene is a small molecular GP130 inhibitor, which binds to GP130 D1 domain[1].
Bazedoxifene inhibits STAT3 phosphorylation induced by Il-6 and IL-11 in GP130/STAT3 pathway signaling[1].
Bazedoxifene (10 μM-20 μM; 2 hours) inhibits STAT3 Phosphorylation Induced by cytokines in human pancreatic cancer cells[2].
Bazedoxifene (5-20 μM; overnight) induces apoptosis in human pancreatic cancer cells[2].
Bazedoxifene inhibits STAT3 nuclear translocation induced by IL-6[2].
Bazedoxifene blocks the cells migration in pancreatic cancer cells by inhibition of GP130[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:AsPC-1 cells
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Concentration:10 μM, 20 μM
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Incubation Time:2 hours
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Result:Inhibited IL-6, IL-11 or OSM (50 ng/mL) induced STAT3 phosphorylation.
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Cell Line:Capan-1 cells, BxPC-3 cells, HPAF-II cells, HPAC cells
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Concentration:10 μM, 20 μM (Capan-1); 5 μM, 10 μM (BxPC-3); 10 μM, 20 μM (HPAF-II); 10 μM, 15 μM (HPAC)
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Incubation Time:Overnight
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Result:Induced apoptosis.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:6-week-old female athymic nude mice[2]
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Dosage:5 mg/kg
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Administration:Oral gavage, daily, for 18 days
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Result:Suppressed pancreatic cancer xenograft tumor growth and induced apoptosis in tumor cells.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 198481-32-2
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Appearance Solid
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Peso molecular 470.60
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Fòrmula C30H34N2O3
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Color White to yellow
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SMILES
CC1=C(C2=CC=C(O)C=C2)N(CC3=CC=C(OCCN4CCCCCC4)C=C3)C5=CC=C(O)C=C51
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Synonyms
TSE-424
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (17)
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Journal Impact Factor
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Most Recent
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Nat Commun
2026 Apr 1;17(1):4716. PMID: 41922346 -
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 -
J Med Chem
Screening and Reverse-Engineering of Estrogen Receptor Ligands as Potent Pan-Filovirus Inhibitors. [Abstract]2020 Oct 8;63(19):11085-11099. PMID: 32886512 -
Glia
Remyelination in neuromyelitis optica spectrum disorder is promoted by edaravone through mTORC1 signaling activation. [Abstract]2023 Feb;71(2):284-304. PMID: 36089914 -
Eur J Pharmacol
Bazedoxifene attenuates intestinal injury in sepsis by suppressing the NF-κB/NLRP3 signaling pathways. [Abstract]2023 May 15:947:175681. PMID: 36965746 -
Cell Rep Methods
RECOVER identifies synergistic drug combinations in vitro through sequential model optimization. [Abstract]2023 Oct 23;3(10):100599. PMID: 37797618 -
iScience
Bazedoxifene rescues hepatocytes from chemically induced oxidative ferroptotic injury in vivo and in vitro by inhibiting protein disulfide isomerase. [Abstract]2026 Feb 6;29(3):114931. PMID: 41782827 -
Gynecol Oncol
Constitutively active ESR1 mutations in gynecologic malignancies and clinical response to estrogen-receptor directed therapies. [Abstract]2019 Jul;154(1):199-206. PMID: 30987772 -
Sci Rep
Novel soluble bazedoxifene formulation gains antiproliferative and migrastatic effect in squamous cell carcinoma cells. [Abstract]2026 Mar 17. PMID: 41844825 -
mSphere
Bazedoxifene Suppresses Intracellular Mycobacterium tuberculosis Growth by Enhancing Autophagy. [Abstract]2020 Apr 8;5(2):e00124-20. PMID: 32269154 -
Arch Biochem Biophys
Role of protein disulfide isomerase in mediating sulfasalazine-induced ferroptosis in HT22 cells: The PDI-NOS-NO-ROS/lipid-ROS cascade. [Abstract]2025 Jun:768:110366. PMID: 40023379 -
Breast Cancer Res Treat
Pharmacokinetic and pharmacodynamic analysis of fulvestrant in preclinical models of breast cancer to assess the importance of its estrogen receptor-α degrader activity in antitumor efficacy. [Abstract]2020 Jan;179(1):67-77. PMID: 31562570 -
J Cell Biochem
Novel chemical scaffold as potential drug against Leishmania donovani: Integrated computational and experimental approaches. [Abstract]2023 Sep;124(9):1404-1422. PMID: 37566640 -
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Res Sq
Sex differences in viral entry protein expression, host responses to SARS-CoV-2, and in vitro responses to sex steroid hormone treatment in COVID-19. [Abstract]2020 Dec 31:rs.3.rs-100914. PMID: 33173861
Solvente y solubilidad
DMSO : 100 mg/mL (212.49 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 (5.31 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 (5.31 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.
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.
Pureza y Documentación
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Ficha de datos (280 KB)
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SDS (419 KB)
- English - EN (419 KB)
- Français - FR (419 KB)
- Deutsch - DE (419 KB)
- Norwegian - NO (419 KB)
- Español - ES (419 KB)
- Swedish - SV (419 KB)
- Italian - IT (419 KB)
- Portuguese - PT (419 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Barry S Komm, et al. Bazedoxifene acetate: a selective estrogen receptor modulator with improved selectivity. Endocrinology. 2005 Sep;146(9):3999-4008. [Content Brief]
[2]. Xiaojuan Wu, et al. Bazedoxifene as a Novel GP130 Inhibitor for Pancreatic Cancer Therapy. Mol Cancer Ther. 2016 Nov; 15(11): 2609–2619. [Content Brief]
[3]. R.A. Hill, et al. Bazedoxifene – a promising brain active SERM that crosses the blood brain barrier and enhances spatial memor. Psychoneuroendocrinology. Volume 121, November 2020, 104830 [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. 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 | 1 mM | 2.1249 mL | 10.6247 mL | 21.2495 mL | 53.1237 mL |
| 5 mM | 0.4250 mL | 2.1249 mL | 4.2499 mL | 10.6247 mL | |
| 10 mM | 0.2125 mL | 1.0625 mL | 2.1249 mL | 5.3124 mL | |
| 15 mM | 0.1417 mL | 0.7083 mL | 1.4166 mL | 3.5416 mL | |
| 20 mM | 0.1062 mL | 0.5312 mL | 1.0625 mL | 2.6562 mL | |
| 25 mM | 0.0850 mL | 0.4250 mL | 0.8500 mL | 2.1249 mL | |
| 30 mM | 0.0708 mL | 0.3542 mL | 0.7083 mL | 1.7708 mL | |
| 40 mM | 0.0531 mL | 0.2656 mL | 0.5312 mL | 1.3281 mL | |
| 50 mM | 0.0425 mL | 0.2125 mL | 0.4250 mL | 1.0625 mL | |
| 60 mM | 0.0354 mL | 0.1771 mL | 0.3542 mL | 0.8854 mL | |
| 80 mM | 0.0266 mL | 0.1328 mL | 0.2656 mL | 0.6640 mL | |
| 100 mM | 0.0212 mL | 0.1062 mL | 0.2125 mL | 0.5312 mL |
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