Prazobind
Based on 1 Customer Validation
Prazobind (SZL 49), a prazosin analog, is an irreversible α1-adrenoceptor antagonist. Prazobind competes for alpha 1-adrenoceptor binding sites with a similar potency (IC50 of 1 nM) in tissues enriched in both the alpha 1A (hippocampus) and alpha 1B (liver) subtypes. Prazobind partially inhibits the contractions of circular muscles, longitudinal muscles and smooth muscles of the spleen. Prazobind can be used for the study of blood pressure.
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- Pureté: 96.20%
- CAS No.: 107021-36-3
- Formule: C23H27N5O3
- Masse moléculaire:421.49
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Stockage:
-20°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
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Alpha-1A adrenergic receptor 1 nM (IC50) |
Alpha-1B adrenergic receptor 1 nM (IC50) |
Prazobind (10-100 nM, 15-30 min) produces a significantly greater inhibitory effect on the circular muscle of the human vas deferens than on the longitudinal muscle[3].
Prazobind (0.1-1 nM, 45 min) clearly inhibits the contraction of the mouse spleen, but this effect was incomplete[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 107021-36-3
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Appearance Solid
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Masse moléculaire 421.49
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Formule C23H27N5O3
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Color White to off-white
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SMILES
NC1=NC(N(CC2)CCN2C(C3=CC4CCC3C=C4)=O)=NC(C=C5OC)=C1C=C5OC
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Synonyms
SZL 49
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
-20°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Solvant et solubilité
DMSO : 50 mg/mL (118.63 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 (sealed storage, away from moisture and light). 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 (sealed storage, away from moisture and light). 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: ≥ 1.25 mg/mL (2.97 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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: ≥ 1.25 mg/mL (2.97 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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.
Pureté et documentation
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Fiche technique (274 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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Instruction de manipulation (2659 KB)
Références
[1]. Mante S, et al. The alkylating prazosin analog SZL 49 inactivates both alpha 1A- and alpha 1B-adrenoceptors. Eur J Pharmacol. 1991;208(2):113-117. [Content Brief]
[2]. Tabrizchi R, et al. The effects of losartan and captopril on vasopressor actions of cirazoline in the absence and presence of SZL-49 and nifedipine. J Cardiovasc Pharmacol. 1995 Jul;26(1):137-44. [Content Brief]
[3]. Amobi NI, et al. Discrimination by SZL49 between contractions evoked by noradrenaline in longitudinal and circular muscle of human vas deferens. Br J Pharmacol. 2002 May;136(1):127-35. [Content Brief]
[4]. Eltze M. Functional evidence for an alpha 1B-adrenoceptor mediating contraction of the mouse spleen. Eur J Pharmacol. 1996 Sep 12;311(2-3):187-98. [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 (sealed storage, away from moisture and light). 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 | 2.3725 mL | 11.8627 mL | 23.7254 mL | 59.3134 mL |
| 5 mM | 0.4745 mL | 2.3725 mL | 4.7451 mL | 11.8627 mL | |
| 10 mM | 0.2373 mL | 1.1863 mL | 2.3725 mL | 5.9313 mL | |
| 15 mM | 0.1582 mL | 0.7908 mL | 1.5817 mL | 3.9542 mL | |
| 20 mM | 0.1186 mL | 0.5931 mL | 1.1863 mL | 2.9657 mL | |
| 25 mM | 0.0949 mL | 0.4745 mL | 0.9490 mL | 2.3725 mL | |
| 30 mM | 0.0791 mL | 0.3954 mL | 0.7908 mL | 1.9771 mL | |
| 40 mM | 0.0593 mL | 0.2966 mL | 0.5931 mL | 1.4828 mL | |
| 50 mM | 0.0475 mL | 0.2373 mL | 0.4745 mL | 1.1863 mL | |
| 60 mM | 0.0395 mL | 0.1977 mL | 0.3954 mL | 0.9886 mL | |
| 80 mM | 0.0297 mL | 0.1483 mL | 0.2966 mL | 0.7414 mL | |
| 100 mM | 0.0237 mL | 0.1186 mL | 0.2373 mL | 0.5931 mL |
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