SKF-82958 hydrobromide
Based on 4 publication(s) in Google Scholar
SKF-82958 ((±)-SKF 82958) hydrobromide is a dopamine D1 receptor full agonist (K0.5=4 nM), displays selective for D1 over D2 receptors (K0.5=73 nM). SKF-82958 hydrobromide induces dopamine D1 receptor-dependent adenylate cyclase activity in rat striatal membranes (EC50=491 nM).
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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 : 99.53%
- CAS 番号: 74115-01-8
- 分子式: C19H21BrClNO2
- 分子量:410.73
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保管条件:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
MedChemExpress(MCE)の使用を引用している文献 SKF-82958 hydrobromide
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生物活性
製品説明
IC50 & Target
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D1 Receptor |
体内実験
? SKF-82958 hydrobromide (0.5-2.0 mg/kg; i.p) significantly suppresses pilocarpine-induced jaw movements[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Sprague-Dawley rats[3]
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Dosage:0.5-2.0 mg/kg
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Administration:I.p
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Result:Significantly reduced the number of tremulous jaw movements induced by 4.0 mg/kg pilocarpine.
化学情報
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CAS 番号 74115-01-8
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性状 Solid
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分子量 410.73
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分子式 C19H21BrClNO2
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Color White to off-white
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SMILES
OC1=C(O)C=C2C(C3=CC=CC=C3)CN(CC=C)CCC2=C1Cl.[H]Br
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別名
(±)-SKF-82958 hydrobromide; Chloro-APB hydrobromide
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (4)
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Journal Impact Factor
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Most Recent
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Behav Brain Res
Neurobehavioral correlates of dopamine agonist-induced eye-blinking in the marmoset monkey. [Abstract]2026 Feb 28:499:115939. PMID: 41248739 -
Behav Pharmacol
SKF82958, a dopamine D1 receptor agonist, disrupts prepulse inhibition in the medial prefrontal cortex and nucleus accumbens in C57BL/6J mice. [Abstract]2024 Jun 1;35(4):193-200. PMID: 38567425 -
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溶剤 & 溶解度
体外:
DMSO : ≥ 100 mg/mL (243.47 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). 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). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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: ≥ 2.5 mg/mL (6.09 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 (6.09 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.
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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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 (279 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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取扱説明書 (2659 KB)
参考文献
[1]. Mottola DM, et al. Conformational analysis of D1 dopamine receptor agonists: pharmacophore assessment and receptor mapping. J Med Chem. 1996;39(1):285-296. [Content Brief]
[2]. Haile CN, et al. The dopamine D(1) receptor agonist SKF-82958 serves as a discriminative stimulus in the rat. Eur J Pharmacol. 2000;388(2):125-131. [Content Brief]
[3]. Mayorga AJ, et al. Striatal and nigral D1 mechanisms involved in the antiparkinsonian effects of SKF 82958 (APB): studies of tremulous jaw movements in rats. Psychopharmacology (Berl). 1999;143(1):72-81. [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). 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 | 2.4347 mL | 12.1734 mL | 24.3469 mL | 60.8672 mL |
| 5 mM | 0.4869 mL | 2.4347 mL | 4.8694 mL | 12.1734 mL | |
| 10 mM | 0.2435 mL | 1.2173 mL | 2.4347 mL | 6.0867 mL | |
| 15 mM | 0.1623 mL | 0.8116 mL | 1.6231 mL | 4.0578 mL | |
| 20 mM | 0.1217 mL | 0.6087 mL | 1.2173 mL | 3.0434 mL | |
| 25 mM | 0.0974 mL | 0.4869 mL | 0.9739 mL | 2.4347 mL | |
| 30 mM | 0.0812 mL | 0.4058 mL | 0.8116 mL | 2.0289 mL | |
| 40 mM | 0.0609 mL | 0.3043 mL | 0.6087 mL | 1.5217 mL | |
| 50 mM | 0.0487 mL | 0.2435 mL | 0.4869 mL | 1.2173 mL | |
| 60 mM | 0.0406 mL | 0.2029 mL | 0.4058 mL | 1.0145 mL | |
| 80 mM | 0.0304 mL | 0.1522 mL | 0.3043 mL | 0.7608 mL | |
| 100 mM | 0.0243 mL | 0.1217 mL | 0.2435 mL | 0.6087 mL |