PT-2385
Based on 53 publication(s) in Google Scholar
PT-2385 is a selective HIF-2α inhibitor with a Ki of less than 50 nM.
For research use only. We do not sell to patients.
- Purity: 99.95%
- CAS No.: 1672665-49-4
- Formula: C17H12F3NO4S
- Molecular Weight:383.34
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Epigenetics Compound Library
HY-L005
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Immunology/Inflammation Compound Library
HY-L007
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HY-L012
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HY-L025
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HY-L026
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HY-L035
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HY-L039
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HY-L045
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HY-L052
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HY-L063
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HY-L064
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HY-L074
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HY-L135
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HY-L158
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HY-L205
Publications Citing Use of MedChemExpress (MCE) PT-2385
More- Nat Med. 2017 Nov;23(11):1298-1308. [Abstract]
- Cell Metab. 2020 Jan 7;31(1):115-130.e6. [Abstract]
- Cell Host Microbe. 2024 May 13:S1931-3128(24)00137-9. [Abstract]
- Nat Commun. 2026 Feb 12;17(1):1214. [Abstract]
- Nat Commun. 2025 Jul 8;16(1):6302. [Abstract]
- Nat Commun. 2024 Aug 29;15(1):7483. [Abstract]
- Nat Commun. 2020 Oct 6;11(1):5005. [Abstract]
- Adv Sci (Weinh). 2025 Jun 23:e05070. [Abstract]
- J Clin Invest. 2020 May 1;130(5):2237-2251. [Abstract]
- J Clin Invest. 2019 Jan 2;129(1):336-348. [Abstract]
- Biomaterials. 2022 May;284:121512. [Abstract]
- Sci Adv. 2022 Mar 4;8(9):eabm1896. [Abstract]
- J Hazard Mater. 2024 Jan 5:461:132570. [Abstract]
- Cell Death Dis. 2017 Oct 12;8(10):e3095. [Abstract]
- Proc Natl Acad Sci U S A. 2024 Jul 30;121(31):e2321929121. [Abstract]
- Proc Natl Acad Sci U S A. 2021 Oct 5;118(40):e2109186118. [Abstract]
- Br J Pharmacol. 2022 Mar;179(5):1065-1081. [Abstract]
- Neoplasia. 2020 Dec;22(12):689-701. [Abstract]
- Biomed Pharmacother. 2022 Jun:150:112955. [Abstract]
- Arterioscler Thromb Vasc Biol. 2025 Nov;45(11):1983-1996. [Abstract]
- Cell Mol Gastroenterol Hepatol. 2022;13(4):1057-1072. [Abstract]
- Cell Rep. 2025 Jan 8;44(1):115169. [Abstract]
- Cell Rep. 2024 Jul 23;43(7):114471. [Abstract]
- Mol Metab. 2024 Jun:84:101944. [Abstract]
- Antioxidants (Basel). 2023 Feb 24;12(3):566. [Abstract]
- Biochem Pharmacol. 2024 Aug 9:116478. [Abstract]
- J Enzyme Inhib Med Chem. 2026 Dec;41(1):2606435. [Abstract]
- Int J Pharm. 2024 Sep 23:124752. [Abstract]
- Cancer Immunol Immunother. 2025 Jul 30;74(9):278. [Abstract]
- Cancer Immunol Immunother. 2019 May;68(5):731-741. [Abstract]
- Int J Mol Sci. 2025 Mar 29;26(7):3182. [Abstract]
- Drug Metab Dispos. 2018 Apr;46(4):336-345. [Abstract]
- Sci Rep. 2025 Jun 5;15(1):19818. [Abstract]
- Biomedicines. 2023 Nov 7;11(11):2992. [Abstract]
- Cell Signal. 2022 Oct:98:110407. [Abstract]
- Membranes. 2021 Aug 17;11(8):636. [Abstract]
- Front Oncol. 2022 Sep 23;12:998295. [Abstract]
- Environ Toxicol. 2024 Apr;39(4):2363-2373. [Abstract]
- Mol Pharmacol. 2022 Sep 27;102(6):MOLPHARM-AR-2022-000525. [Abstract]
- Life Sci Alliance. 2023 Feb 1;6(4):e202201756. [Abstract]
- Mol Cell Biol. 2024 Dec 2:1-14. [Abstract]
- Drug Test Anal. 2022 Oct;14(10):1703-1723. [Abstract]
- PLoS One. 2018 Dec 19;13(12):e0208579. [Abstract]
- Biochem Biophys Res Commun. 2019 Jan 22;508(4):1233-1239. [Abstract]
- bioRxiv. 2026 Jun 10:2026.06.09.731212. [Abstract]
- University of California, Irvine. 2024.
- bioRxiv. 2024 August 27.
- bioRxiv. 2024 May 5:2024.05.04.592520. [Abstract]
- UNIVERSITY OF THESSALY. 2023 Sep.
- bioRxiv. 2023 Sep 17.
- Research Square Preprint. 2022 Jul.
- Research Square Print. 2022 Jun.
- University of Michigan. 2020 Feb.
Customer Validation & Images
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Cell Imaging/Staining
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Biological Activity
Kd: <50 nM (HIF-2α)[1]
PT-2385 (PT2385) inhibits expression of HIF-2α regulated genes in a dose dependent manner in vivo. Tumor is regressed with PT-2385 (3 and 10 mg/kg, p.o., b.i.d. dose) in 786-O xenograft. PT-2385 (1,3 and 10 mg/kg) also inhibits tumor-derived VEGFA protein levels. PT-2385 (10 mg/kg) treatment reduces proliferation (Ki67) and angiogenesis (CD-31)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:SCID/beige mice with the 786-O and A498 RCC cell lines[3]
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Dosage:30 or 100 mg/kg
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Administration:Oral gavage; twice daily
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Result:Resulted in a rapid, dose-dependent tumor regression.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1672665-49-4
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Appearance Solid
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Molecular Weight 383.34
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Formula C17H12F3NO4S
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Color White to off-white
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SMILES
N#CC1=CC(F)=CC(OC2=CC=C(S(=O)(C)=O)C3=C2CC(F)(F)[C@H]3O)=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months
Publications (53)
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Journal Impact Factor
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Most Recent
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Nat Med
Activation of intestinal hypoxia-inducible factor 2α during obesity contributes to hepatic steatosis. [Abstract]2017 Nov;23(11):1298-1308. PMID: 29035368
PT-2385 purchased from MedChemExpress. Usage Cited in: Nat Med. 2017 Nov;23(11):1298-1308. [Abstract]
Western blot analysis of NEU3 protein expression in the small intestine.
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Cell Metab
2020 Jan 7;31(1):115-130.e6. PMID: 31708445 -
Cell Host Microbe
Candida albicans accelerates atherosclerosis by activating intestinal hypoxia-inducible factor2α signaling. [Abstract]2024 May 13:S1931-3128(24)00137-9. PMID: 38754418 -
Nat Commun
Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]2026 Feb 12;17(1):1214. PMID: 41680175 -
Nat Commun
2025 Jul 8;16(1):6302. PMID: 40628749 -
Nat Commun
Adipocyte deletion of the oxygen-sensor PHD2 sustains elevated energy expenditure at thermoneutrality. [Abstract]2024 Aug 29;15(1):7483. PMID: 39209825 -
Nat Commun
2020 Oct 6;11(1):5005. PMID: 33024109
PT-2385 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2020 Oct 6;11(1):5005. [Abstract]
WT naïve CD4+ T cells are activated by CD3/CD28 (2/1 μg/mL) in the presence of HIF-2α inhibitor PT2385 for 2 days, or activating WT iTreg cells are treated with 10 μM PT2385, and HIF-1α levels determined. Treatment of activating WT CD4+ T cells with PT2385 leads to dose-dependent upregulation of HIF-1α. PT2385 also increases the level of HIF-1α induction in activated WT iTreg cells.
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Adv Sci (Weinh)
Lysosome-Featured Cell Aggregate-Released Extracellular Vesicles Regulate Iron Homeostasis and Alleviate Post-Irradiation Endothelial Ferroptosis for Mandibular Regeneration. [Abstract]2025 Jun 23:e05070. PMID: 40546115
PT-2385 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Jun 23:e05070. [Abstract]
Bright-field images for the process of cell aggregation. The results showed that Ferrozine (6.5 mM) slowed the CA formation. Scale bars, 150 µm.
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J Clin Invest
Marked and rapid effects of pharmacological HIF-2α antagonism on hypoxic ventilatory control. [Abstract]2020 May 1;130(5):2237-2251. PMID: 31999648 -
J Clin Invest
Hepatic hepcidin/intestinal HIF-2α axis maintains iron absorption during iron deficiency and overload. [Abstract]2019 Jan 2;129(1):336-348. PMID: 30352047 -
Biomaterials
HIF-2α-targeted interventional chemoembolization multifunctional microspheres for effective elimination of hepatocellular carcinoma. [Abstract]2022 May;284:121512. PMID: 35405577 -
Sci Adv
PAI-1 is a vascular cell-specific HIF-2-dependent angiogenic factor that promotes retinal neovascularization in diabetic patients. [Abstract]2022 Mar 4;8(9):eabm1896. PMID: 35235351 -
J Hazard Mater
In vitro and in vivo investigations on arsenic-induced cartilage degeneration in osteoarthritis. [Abstract]2024 Jan 5:461:132570. PMID: 37742380 -
Cell Death Dis
Increasing AR by HIF-2α inhibitor (PT-2385) overcomes the side-effects of sorafenib by suppressing hepatocellular carcinoma invasion via alteration of pSTAT3, pAKT and pERK signals. [Abstract]2017 Oct 12;8(10):e3095. PMID: 29022906
PT-2385 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2017 Oct 12;8(10):e3095. [Abstract]
Western blot assays show PT-2385 can suppress HIF-2α level and partly reverse the decrease of AR and the increase of downstream signals (pSTAT3, pAKT and pERK) by Bay 43-9006 treatment.
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Proc Natl Acad Sci U S A
Iron regulatory protein 2 contributes to antimicrobial immunity by preserving lysosomal function in macrophages. [Abstract]2024 Jul 30;121(31):e2321929121. PMID: 39047035 -
Proc Natl Acad Sci U S A
Essential role of systemic iron mobilization and redistribution for adaptive thermogenesis through HIF2-α/hepcidin axis. [Abstract]2021 Oct 5;118(40):e2109186118. PMID: 34593646 -
Br J Pharmacol
Established pulmonary hypertension in rats was reversed by a combination of a HIF-2α antagonist and a p53 agonist. [Abstract]2022 Mar;179(5):1065-1081. PMID: 34599843 -
Neoplasia
2020 Dec;22(12):689-701. PMID: 33142235 -
Biomed Pharmacother
Berberine reduces hepatic ceramide levels to improve insulin resistance in HFD-fed mice by inhibiting HIF-2α. [Abstract]2022 Jun:150:112955. PMID: 35429745 -
Arterioscler Thromb Vasc Biol
2025 Nov;45(11):1983-1996. PMID: 41036559 -
Cell Mol Gastroenterol Hepatol
2022;13(4):1057-1072. PMID: 34902628 -
Cell Rep
Conserved patterns of transcriptional dysregulation, heterogeneity, and cell states in clear cell kidney cancer. [Abstract]2025 Jan 8;44(1):115169. PMID: 39792555 -
Cell Rep
2024 Jul 23;43(7):114471. PMID: 38996069 -
Mol Metab
Microbial metabolite deoxycholic acid-mediated ferroptosis exacerbates high-fat diet-induced colonic inflammation. [Abstract]2024 Jun:84:101944. PMID: 38642891 -
Antioxidants (Basel)
2023 Feb 24;12(3):566. PMID: 36978814 -
Biochem Pharmacol
The 'ABC' of split-nanoluciferase HIF heterodimerization bioassays: Applications, Benefits & Considerations. [Abstract]2024 Aug 9:116478. PMID: 39128589 -
J Enzyme Inhib Med Chem
2026 Dec;41(1):2606435. PMID: 41493169 -
Int J Pharm
A pH-responsive novel delivery system utilizing carbon quantum dots loaded with PT2385 for targeted inhibition of HIF-2α in the treatment of osteoarthritis. [Abstract]2024 Sep 23:124752. PMID: 39321898 -
Cancer Immunol Immunother
VHL restoration in clear cell renal cell carcinoma improves NK cell infiltration and function. [Abstract]2025 Jul 30;74(9):278. PMID: 40736709 -
Cancer Immunol Immunother
Tumor infiltrating mast cells determine oncogenic HIF-2α-conferred immune evasion in clear cell renal cell carcinoma. [Abstract]2019 May;68(5):731-741. PMID: 30758643 -
Int J Mol Sci
Role of Hypoxia-Inducible Factors in Respiratory Syncytial Virus Infection-Associated Lung Disease. [Abstract]2025 Mar 29;26(7):3182. PMID: 40244000 -
Drug Metab Dispos
Metabolic Profiling of the Novel Hypoxia-Inducible Factor 2 α Inhibitor PT2385 In Vivo and In Vitro. [Abstract]2018 Apr;46(4):336-345. PMID: 29363499 -
Sci Rep
Characterisation of an autochthonous mouse ccRCC model of immune checkpoint inhibitor therapy resistance. [Abstract]2025 Jun 5;15(1):19818. PMID: 40473819 -
Biomedicines
High-Altitude Hypoxia Induces Excessive Erythrocytosis in Mice via Upregulation of the Intestinal HIF2a/Iron-Metabolism Pathway. [Abstract]2023 Nov 7;11(11):2992. PMID: 38001992 -
Cell Signal
EP300 promotes renal tubular epithelial cell fibrosis by increasing HIF2α expression in diabetic nephropathy. [Abstract]2022 Oct:98:110407. PMID: 35839978 -
Membranes
Effective Perturbations of the Amplitude, Gating, and Hysteresis of IK(DR) Caused by PT-2385, an HIF-2α Inhibitor. [Abstract]2021 Aug 17;11(8):636. PMID: 34436399 -
Front Oncol
HIF-2α regulates proliferation, invasion, and metastasis of hepatocellular carcinoma cells via VEGF/Notch1 signaling axis after insufficient radiofrequency ablation. [Abstract]2022 Sep 23;12:998295. PMID: 36212390 -
Environ Toxicol
2024 Apr;39(4):2363-2373. PMID: 38156404 -
Mol Pharmacol
Structural basis for the allosteric inhibition of hypoxia-inducible factor (HIF)-2 by belzutifan. [Abstract]2022 Sep 27;102(6):MOLPHARM-AR-2022-000525. PMID: 36167425 -
Life Sci Alliance
Multi-level interaction between HIF and AHR transcriptional pathways in kidney carcinoma. [Abstract]2023 Feb 1;6(4):e202201756. PMID: 36725335 -
Mol Cell Biol
Erythropoietin Production in Embryonic Neural Cells is Controlled by Hypoxia Signaling and Histone Deacetylases with an Undifferentiated Cellular State. [Abstract]2024 Dec 2:1-14. PMID: 39620278 -
Drug Test Anal
Metabolic study of hypoxia-inducible factor stabilizers BAY 87-2243, MK-8617, and PT-2385 in equine liver microsomes for doping control. [Abstract]2022 Oct;14(10):1703-1723. PMID: 35853151 -
PLoS One
2018 Dec 19;13(12):e0208579. PMID: 30566445 -
Biochem Biophys Res Commun
EPAS1/HIF2α correlates with features of low-risk neuroblastoma and with adrenal chromaffin cell differentiation during sympathoadrenal development. [Abstract]2019 Jan 22;508(4):1233-1239. PMID: 30563765
PT-2385 purchased from MedChemExpress. Usage Cited in: Biochem Biophys Res Commun. 2019 Jan 22;508(4):1233-1239. [Abstract]
Western blot with HIF2a-specific antibody on lysates from LAN-1 cells treated grown in normoxia (21% O2) or in hypoxia (1% O2), with the indicated concentration of PT2385.
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bioRxiv
Epigenetic de-repression of basal cell metaplasia in aging AT2 cells is a risk factor for idiopathic pulmonary fibrosis (IPF). [Abstract]2026 Jun 10:2026.06.09.731212. PMID: 42327275 -
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bioRxiv
HIF2α-dependent inhibition of mitochondrial clustering of glutaminase suppresses clear cell renal cell carcinoma. [Abstract]2024 May 5:2024.05.04.592520. PMID: 38746132 -
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Solvent & Solubility
DMSO : ≥ 50 mg/mL (130.43 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, 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.
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 (6.52 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 (6.52 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.
Purity & Documentation
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Data Sheet (279 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
[2]. Xie C, et al. Activation of intestinal hypoxia-inducible factor 2α during obesity contributes to hepatic steatosis. Nat Med. 2017 Nov;23(11):1298-1308. [Content Brief]
[3]. Wallace EM, et al. A Small-Molecule Antagonist of HIF2α Is Efficacious in Preclinical Models of Renal Cell Carcinoma. Cancer Res. 2016 Sep 15;76(18):5491-500. [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 | 2.6087 mL | 13.0433 mL | 26.0865 mL | 65.2163 mL |
| 5 mM | 0.5217 mL | 2.6087 mL | 5.2173 mL | 13.0433 mL | |
| 10 mM | 0.2609 mL | 1.3043 mL | 2.6087 mL | 6.5216 mL | |
| 15 mM | 0.1739 mL | 0.8696 mL | 1.7391 mL | 4.3478 mL | |
| 20 mM | 0.1304 mL | 0.6522 mL | 1.3043 mL | 3.2608 mL | |
| 25 mM | 0.1043 mL | 0.5217 mL | 1.0435 mL | 2.6087 mL | |
| 30 mM | 0.0870 mL | 0.4348 mL | 0.8696 mL | 2.1739 mL | |
| 40 mM | 0.0652 mL | 0.3261 mL | 0.6522 mL | 1.6304 mL | |
| 50 mM | 0.0522 mL | 0.2609 mL | 0.5217 mL | 1.3043 mL | |
| 60 mM | 0.0435 mL | 0.2174 mL | 0.4348 mL | 1.0869 mL | |
| 80 mM | 0.0326 mL | 0.1630 mL | 0.3261 mL | 0.8152 mL | |
| 100 mM | 0.0261 mL | 0.1304 mL | 0.2609 mL | 0.6522 mL |
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