Avasimibe
Based on 20 publication(s) in Google Scholar
Avasimibe (CI-1011; PD-148515) is an orally active acyl coenzyme A-cholesterol acyltransferase (ACAT; also called SOAT)) inhibitor with IC50s of 24 and 9.2 µM for ACAT1 and ACAT2, respectively. Avasimibe can be used for the research of prostate cancer.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度 : 99.77%
- CAS 番号: 166518-60-1
- 分子式: C29H43NO4S
- 分子量:501.72
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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
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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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 Avasimibe
More- Nat Commun. 2025 Dec 19. [Abstract]
- Metabolism. 2021 Oct:123:154861. [Abstract]
- Redox Biol. 2023 Jun:62:102678. [Abstract]
- Cell Mol Biol Lett. 2025 Nov 24;30(1):140. [Abstract]
- Cell Death Dis. 2025 Apr 14;16(1):291. [Abstract]
- Cell Death Dis. 2021 Mar 10;12(3):254. [Abstract]
- Phytomedicine. 2025 Nov 25:148:157332. [Abstract]
- Cancer Cell Int. 2021 Aug 30;21(1):461. [Abstract]
- Int J Mol Sci. 2026 Mar 11;27(6):2587. [Abstract]
- Int Immunopharmacol. 2026 Jan 15:169:115973. [Abstract]
- Biomolecules. 2022 Jan 31;12(2):237. [Abstract]
- Biomolecules. 2021 Jun 8;11(6):853. [Abstract]
- Cancer Sci. 2024 Jan;115(1):48-58. [Abstract]
- Aquat Toxicol. 2026 Jun:295:107814. [Abstract]
- Biochem Biophys Res Commun. 2026 Jan 1:794:153070. [Abstract]
- Oncol Lett. 2019 Aug;18(2):1548-1556. [Abstract]
- bioRxiv. 2026 Jun 11:2026.06.10.731372. [Abstract]
- bioRxiv. 2026 Apr 4:2026.04.03.716381. [Abstract]
- bioRxiv. 2025 Jun 15:2025.06.12.659424. [Abstract]
- Biomed Pharmacother. 2020 Oct:130:110508. [Abstract]
Customer Validation & Images
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WB
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IP
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Cell Imaging/Staining
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Cell Proliferation/Viability Assay
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RT-PCR
生物活性
製品説明
IC50 & Target
[1]|
ACAT1 24 μM (IC50) |
ACAT2 9.2 μM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Caco-2 | CC50 |
13.71 μM
Compound: AVASIMIBE
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Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay
Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay
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10.21203/rs.3.rs-23951/v1 |
| Caco-2 | IC50 |
3.93 μM
Compound: AVASIMIBE
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Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging
Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging
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10.21203/rs.3.rs-23951/v1 |
| HepG2 | IC50 |
479 nM
Compound: avasimibe
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Inhibition of ACAT in human HepG2 cells
Inhibition of ACAT in human HepG2 cells
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[PMID: 19167888] |
| THP-1 | IC50 |
1.5 μM
Compound: avasimibe
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Inhibition of ACAT-mediated esterified cholesterol accumulation in human THP1 cells exposed to acetyl-LDL during differentiation assessed as effect on foam cell formation
Inhibition of ACAT-mediated esterified cholesterol accumulation in human THP1 cells exposed to acetyl-LDL during differentiation assessed as effect on foam cell formation
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[PMID: 18620381] |
体外実験
Avasimibe (0-80 μM; for 1-3 days) reduces proliferation in the prostate cancer (PCa) cells[2].
Avasimibe (10 and 20 μM; 48 h) reduces the expression of β-catenin, Vimentin, N-cadherin, Snail and MMP9, which are tightly associated with epithelial-mesenchymal transition (EMT)[2].
Avasimibe (10 and 20 μM) trigger cell cycle arrest via the E2F-1 signalling pathway in prostate cancer. Avasimibe induces G1 phase cell cycle arrest of PCa cells[2].
Avasimibe (10 and 20 μM) inhibits the metastasis of PCa cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
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Cell Line:PCa cells (PC-3 and DU 145)
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Concentration:0, 0.25, 5, 10, 20, 40 and 80 µM
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Incubation Time:1, 2, and 3 days
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Result:Dose dependently inhibited PC-3 and DU 145 cell viability.
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Cell Line:PCa cells (PC-3 and DU 145)
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Concentration:10 and 20 µM
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Incubation Time:48 hours
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Result:Reduced protein levels of EMT-related proteins (β-catenin, Vimentin, N-cadherin, Snail, MMP9 and E-cadherin).
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Cell Line:PCa cells (PC-3 and DU 145)
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Concentration:10 and 20 µM
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Incubation Time:48 hours
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Result:Induced G1 phase cycle arrest and altered the G1 phase-related protein levels in PCa cells.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:SPF male mice (BALB/c-nude, 4 weeks old) bearing PCa cells[2]
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Dosage:30 mg/kg
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Administration:Intraperitoneally injected for 7 weeks
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Result:Reduced tumour volume compared with that of the control group. Inhibited PCa growth and migration in vivo.
化学情報
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CAS 番号 166518-60-1
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性状 Solid
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分子量 501.72
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分子式 C29H43NO4S
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Color White to off-white
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SMILES
O=C(NS(=O)(OC1=C(C(C)C)C=CC=C1C(C)C)=O)CC2=C(C(C)C)C=C(C(C)C)C=C2C(C)C
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別名
CI-1011; PD-148515
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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 (20)
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Journal Impact Factor
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Most Recent
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Nat Commun
IDH2 lactylation promotes angiogenesis in murine diabetic myocardial infarction via blocking Cav1-eNOS interaction. [Abstract]2025 Dec 19. PMID: 41419771
Avasimibe purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Dec 19. [Abstract]
Avasimibe (20 μM; 24 h). Western blot analysis of the expression levels of ACAT1 and IDH2-K272la in CMECs treated with the ACAT1 inhibitor Avasimibe under NOD and HOD stimulation.
Avasimibe purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Dec 19. [Abstract]
Avasimibe (20 μM; 24 h). Coimmunoprecipitation experiment assessing the binding capacity of Cav1 with IDH2 and eNOS in CMECs treated with the ACAT1 inhibitor Avasimibe under NOD and HOD stimulation.
Avasimibe purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Dec 19. [Abstract]
Avasimibe (20 μM; 24 h). Evaluation of tube formation, EdU proliferation, and NO production capabilities of CMECs treated with the ACAT1 inhibitor Avasimibe under HOD stimulation.
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Metabolism
Pharmacological inhibition of acyl-coenzyme A:cholesterol acyltransferase alleviates obesity and insulin resistance in diet-induced obese mice by regulating food intake. [Abstract]2021 Oct:123:154861. PMID: 34371065 -
Redox Biol
Accumulated cholesterol protects tumours from elevated lipid peroxidation in the microenvironment. [Abstract]2023 Jun:62:102678. PMID: 36940607 -
Cell Mol Biol Lett
Abnormal cholesterol-cholesteryl ester metabolism impairs mouse oocyte quality during ovarian aging. [Abstract]2025 Nov 24;30(1):140. PMID: 41286604 -
Cell Death Dis
A targetable antioxidant defense mechanism to EZH2 inhibitors enhances tumor cell vulnerability to ferroptosis. [Abstract]2025 Apr 14;16(1):291. PMID: 40229247 -
Cell Death Dis
CTRP12 ameliorates atherosclerosis by promoting cholesterol efflux and inhibiting inflammatory response via the miR-155-5p/LXRα pathway. [Abstract]2021 Mar 10;12(3):254. PMID: 33692340 -
Phytomedicine
Piperine targets SOAT1 to inhibit the progression of esophageal squamous cell carcinoma via ferroptosis. [Abstract]2025 Nov 25:148:157332. PMID: 41061292 -
Cancer Cell Int
The cholesterol esterification inhibitor avasimibe suppresses tumour proliferation and metastasis via the E2F-1 signalling pathway in prostate cancer. [Abstract]2021 Aug 30;21(1):461. PMID: 34461908 -
Int J Mol Sci
2026 Mar 11;27(6):2587. PMID: 41898448 -
Int Immunopharmacol
ACAT1 inhibitor Avasimibe suppresses osteoclastogenesis and alleviates ovariectomy-induced bone loss via CKB/PI3K-AKT signaling. [Abstract]2026 Jan 15:169:115973. PMID: 41352098 -
Biomolecules
2022 Jan 31;12(2):237. PMID: 35204738 -
Biomolecules
Cholesteryl Ester Promotes Mammary Tumor Growth in MMTV-PyMT Mice and Activates Akt-mTOR Pathway in Tumor Cells. [Abstract]2021 Jun 8;11(6):853. PMID: 34201030 -
Cancer Sci
SCD1 inhibition enhances the effector functions of CD8+ T cells via ACAT1-dependent reduction of esterified cholesterol. [Abstract]2024 Jan;115(1):48-58. PMID: 37879607 -
Aquat Toxicol
Is acyl-CoA cholesterol acyltransferase 2 the enzyme responsible for the esterification of okadaic acid in bivalves?. [Abstract]2026 Jun:295:107814. PMID: 41935504 -
Biochem Biophys Res Commun
7-dehydrocholesterol promotes CCL2-secretion from porcine skeletal muscle satellite cells, enhancing the migration of preadipocytes. [Abstract]2026 Jan 1:794:153070. PMID: 41344212 -
Oncol Lett
Effect of inhibiting ACAT-1 expression on the growth and metastasis of Lewis lung carcinoma. [Abstract]2019 Aug;18(2):1548-1556. PMID: 31423222 -
bioRxiv
2026 Jun 11:2026.06.10.731372. PMID: 42327215 -
bioRxiv
2026 Apr 4:2026.04.03.716381. PMID: 41959418 -
bioRxiv
Inhibition of Acyl-CoA: Cholesterol Acyltransferase 1 Promotes Shedding of Soluble TREM2 and LRP1-Dependent Phagocytosis of Amyloid β Protein in Microglia. [Abstract]2025 Jun 15:2025.06.12.659424. PMID: 40661651 -
Biomed Pharmacother
Avasimibe inhibits the proliferation, migration and invasion of glioma cells by suppressing linc00339. [Abstract]2020 Oct:130:110508. PMID: 32682982
Avasimibe purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2020 Oct:130:110508. [Abstract]
Avasimibe (7.5 μM; 0-72 h). Inhibitory effects of Avasimibe on cell viability of T98 G and LN229 at different times.
Avasimibe purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2020 Oct:130:110508. [Abstract]
qRT-PCR data showing the expression of linc00339 in T98 G or LN229 cells treated with linc00339 plasmid, Avasimibe (7.5 μM for 48 h) alone or in combination with linc00339 plasmids.
Avasimibe purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2020 Oct:130:110508. [Abstract]
Colony formation assays showing the proliferation capacity of T98 G or LN229 cells treated with linc00339 plasmid, Avasimibe (7.5 μM for 48 h) alone or in combination with linc00339 plasmids.
Avasimibe purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2020 Oct:130:110508. [Abstract]
Avasimibe (7.5 μM for 48 h). LN229 cells treated with Avasimibe or combined with linc00339 plasmid were subcutaneously injected into the nude mice. Tumour formation in nude mice.
Avasimibe purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2020 Oct:130:110508. [Abstract]
Transwell assays showing the invasion capacity of T98 G or LN229 cells treated with linc00339 plasmid, Avasimibe (7.5 μM for 48 h) alone or in combination with linc00339 plasmids.
溶剤 & 溶解度
体外:
DMSO : 100 mg/mL (199.31 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)
体内:
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: 7.5 mg/mL (14.95 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 7.5 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 (75.0 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: 7.5 mg/mL (14.95 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 7.5 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 (75.0 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.
In Vivo Dissolution Calculator
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 (289 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Taichi Ohshiro,et al. Pyripyropene A, an acyl-coenzyme A:cholesterol acyltransferase 2-selective inhibitor, attenuates hypercholesterolemia and atherosclerosis in murine models of hyperlipidemia. Arterioscler Thromb Vasc Biol. 2011 May;31(5):1108-15. [Content Brief]
[2]. Kangping Xiong, et al. The cholesterol esterification inhibitor avasimibe suppresses tumour proliferation and metastasis via the E2F-1 signalling pathway in prostate cancer.Cancer Cell Int. 2021 Aug 30;21(1):461. [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 | 1.9931 mL | 9.9657 mL | 19.9314 mL | 49.8286 mL |
| 5 mM | 0.3986 mL | 1.9931 mL | 3.9863 mL | 9.9657 mL | |
| 10 mM | 0.1993 mL | 0.9966 mL | 1.9931 mL | 4.9829 mL | |
| 15 mM | 0.1329 mL | 0.6644 mL | 1.3288 mL | 3.3219 mL | |
| 20 mM | 0.0997 mL | 0.4983 mL | 0.9966 mL | 2.4914 mL | |
| 25 mM | 0.0797 mL | 0.3986 mL | 0.7973 mL | 1.9931 mL | |
| 30 mM | 0.0664 mL | 0.3322 mL | 0.6644 mL | 1.6610 mL | |
| 40 mM | 0.0498 mL | 0.2491 mL | 0.4983 mL | 1.2457 mL | |
| 50 mM | 0.0399 mL | 0.1993 mL | 0.3986 mL | 0.9966 mL | |
| 60 mM | 0.0332 mL | 0.1661 mL | 0.3322 mL | 0.8305 mL | |
| 80 mM | 0.0249 mL | 0.1246 mL | 0.2491 mL | 0.6229 mL | |
| 100 mM | 0.0199 mL | 0.0997 mL | 0.1993 mL | 0.4983 mL |
Avasimibe 関連分類
HY-13215 関連分類
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