Efaproxiral
Based on 1 publication(s) in Google Scholar
Efaproxiral (RSR13) is a haemoglobin (Hb) synthetic allosteric modifier. Efaproxiral decreases Hb-oxygen (O2) binding affinity and enhances oxygenation of hypoxic tumours during radiation therapy .
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- 純度: 99.94%
- CAS 番号: 131179-95-8
- 分子式: C20H23NO4
- 分子量:341.40
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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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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MedChemExpress（MCE）の使用を引用している文献 Efaproxiral
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生物活性
haemoglobin (Hb)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| INS1(832/13) | EC50 |
6 nM
Compound: 37
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Induction of glucose-stimulated insulin secretion in rat INS-1 832/13 cells incubated for 5 mins by ELISA assay
Induction of glucose-stimulated insulin secretion in rat INS-1 832/13 cells incubated for 5 mins by ELISA assay
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[PMID: 33771587] |
Efaproxiral binds to only one pair of symmetry-related sites in the Hb central water cavity[2].
Efaproxiral readily crosses the red cell membrane in the presence of serum albumin solutions[2].
Efaproxiral is not inhibited from entering erythrocytes in the presence of an anion-channel blocking agent (DIDS)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Efaproxiral reduces hemoglobin-oxygen binding affinity, which facilitates oxygen release from hemoglobin into surrounding tissues and potentially increases the pO(2) of the tumors[4]
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female C3H/HEJ mice (18–20 g), with radiation-induced fibrosarcoma tumor (RIF-1) cells xenograft[3]
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Dosage:150 mg/kg
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Administration:Intraperitoneal injection; prior to X Irradiation (4 Gy/day), for 5 days
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Result:Significantly increased tumor oxygenation by 8.4 to 43.4 mmHg within 5 days, with maximum increases at 22–31 minutes after treatment.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 131179-95-8
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性状 Solid
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分子量 341.40
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分子式 C20H23NO4
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Color White to off-white
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SMILES
CC(C)(OC1=CC=C(CC(NC2=CC(C)=CC(C)=C2)=O)C=C1)C(O)=O
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別名
RSR13
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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 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
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J Enzyme Inhib Med Chem
Pharmacophore-guided repurposing of fibrates and retinoids as GPR40 allosteric ligands with activity on insulin release. [Abstract]2021 Dec;36(1):377-383. PMID: 33525941
溶剤 & 溶解度
DMSO : ≥ 150 mg/mL (439.37 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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 (6.09 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (6.09 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 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: 50% PEG300 50% Saline
Solubility: 27.5 mg/mL (80.55 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.
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 (273 KB)
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- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Stea B, et al. Efaproxiral red blood cell concentration predicts efficacy in patients with brain metastases. Br J Cancer. 2006 Jun 19;94(12):1777-1784. [Content Brief]
[2]. Abraham DJ, et al. Allosteric modifiers of hemoglobin: 2-[4-[[(3,5-disubstituted anilino)carbonyl]methyl]phenoxy]-2-methylpropionic acid derivatives that lower the oxygen affinity of hemoglobin in red cell suspensions, in whole blood, and in vivo in rats. Biochemistry. 1992 Sep 29;31(38):9141-9. [Content Brief]
[3]. Hou H, et al. The effects of Efaproxyn (efaproxiral) on subcutaneous RIF-1 tumor oxygenation and enhancement of radiotherapy-mediated inhibition of tumor growth in mice. Radiat Res. 2007 Aug;168(2):218-25. [Content Brief]
[4]. Hou H, et al. Increased oxygenation of intracranial tumors by efaproxyn (efaproxiral), an allosteric hemoglobin modifier: In vivo EPR oximetry study. Int J Radiat Oncol Biol Phys. 2005 Apr 1;61(5):1503-9. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.9291 mL | 14.6456 mL | 29.2912 mL | 73.2279 mL |
| 5 mM | 0.5858 mL | 2.9291 mL | 5.8582 mL | 14.6456 mL | |
| 10 mM | 0.2929 mL | 1.4646 mL | 2.9291 mL | 7.3228 mL | |
| 15 mM | 0.1953 mL | 0.9764 mL | 1.9527 mL | 4.8819 mL | |
| 20 mM | 0.1465 mL | 0.7323 mL | 1.4646 mL | 3.6614 mL | |
| 25 mM | 0.1172 mL | 0.5858 mL | 1.1716 mL | 2.9291 mL | |
| 30 mM | 0.0976 mL | 0.4882 mL | 0.9764 mL | 2.4409 mL | |
| 40 mM | 0.0732 mL | 0.3661 mL | 0.7323 mL | 1.8307 mL | |
| 50 mM | 0.0586 mL | 0.2929 mL | 0.5858 mL | 1.4646 mL | |
| 60 mM | 0.0488 mL | 0.2441 mL | 0.4882 mL | 1.2205 mL | |
| 80 mM | 0.0366 mL | 0.1831 mL | 0.3661 mL | 0.9153 mL | |
| 100 mM | 0.0293 mL | 0.1465 mL | 0.2929 mL | 0.7323 mL |
Efaproxiral 関連分類
HY-13619 関連分類
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