Proxyfan
Based on 1 Customer Validation
Proxyfan is a potent histamine H3 receptor antagonist with Ki values of 2.9 nM and 2.7 nM for rat and human H3 receptor, respectively. Proxyfan is over 1000-fold more potent at H3 receptors than other histamine receptors.
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- Purity: 99.33%
- CAS No.: 177708-09-7
- 화학식: C13H16N2O
- 분자량:216.28
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보관:Pure form -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
All Histamine Receptor Isoforms
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Biological Activity
제품 설명
IC50 & Target
[1]|
Rat H3LR 2.9 nM (Ki) |
Human H3LR 2.7 nM (Ki) |
Chemical Information
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CAS No. 177708-09-7
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Appearance Liquid
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분자량 216.28
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화학식 C13H16N2O
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Color Colorless to light yellow
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SMILES
C1(CCCOCC2=CC=CC=C2)=CNC=N1
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Pure form -20°C 3 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
In Vitro:
DMSO : 200 mg/mL (924.73 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)
In Vivo:
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: ≥ 5 mg/mL (23.12 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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: ≥ 5 mg/mL (23.12 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
순도&문서
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Data Sheet (269 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. X Ligneau, et al. Distinct pharmacology of rat and human histamine H(3) receptors: role of two amino acids in the third transmembrane domain. Br J Pharmacol. 2000 Dec;131(7):1247-50. [Content Brief]
[2]. R H Clapp, et al. Proxyfan acts as a neutral antagonist of histamine H3 receptors in the feeding-related hypothalamic ventromedial nucleus. Br J Pharmacol. 2012 Nov;167(5):1099-110. [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 |
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| DMSO | 1 mM | 4.6236 mL | 23.1182 mL | 46.2364 mL | 115.5909 mL |
| 5 mM | 0.9247 mL | 4.6236 mL | 9.2473 mL | 23.1182 mL | |
| 10 mM | 0.4624 mL | 2.3118 mL | 4.6236 mL | 11.5591 mL | |
| 15 mM | 0.3082 mL | 1.5412 mL | 3.0824 mL | 7.7061 mL | |
| 20 mM | 0.2312 mL | 1.1559 mL | 2.3118 mL | 5.7795 mL | |
| 25 mM | 0.1849 mL | 0.9247 mL | 1.8495 mL | 4.6236 mL | |
| 30 mM | 0.1541 mL | 0.7706 mL | 1.5412 mL | 3.8530 mL | |
| 40 mM | 0.1156 mL | 0.5780 mL | 1.1559 mL | 2.8898 mL | |
| 50 mM | 0.0925 mL | 0.4624 mL | 0.9247 mL | 2.3118 mL | |
| 60 mM | 0.0771 mL | 0.3853 mL | 0.7706 mL | 1.9265 mL | |
| 80 mM | 0.0578 mL | 0.2890 mL | 0.5780 mL | 1.4449 mL | |
| 100 mM | 0.0462 mL | 0.2312 mL | 0.4624 mL | 1.1559 mL |
Proxyfan Related Classifications
HY-107557 Related Classifications
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