SB-203186 hydrochloride
Based on 1 Customer Validation
SB-203186 hydrochloride is a potent, selective and competitive 5-HT4 antagonist. SB-203186 hydrochloride antagonizes the 5-HT4 receptor-mediated relaxations of the carbachol-contracted rat isolated oesophagus against 5-HT with pKB values of 10.9 (rat oesophagus), 9.5 (guinea-pig ileum), and 9.0 (human colon) respectively.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 99.94%
- CAS. Nr.: 207572-69-8
- Formel: C16H21ClN2O2
- Molecular Weight:308.80
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Speicherung:
4°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)
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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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Biologische Aktivität
Beschreibung
IC50 & Target
pKB: 10.9 (5-HT4 in rat oesophagus), 9.5 (5-HT4 in guinea-pig ileum), and 9.0 (5-HT4 in human colon)[3].
In Vitro
Pretreatment with SB-203186 (10 μM) enhances the 5-HT-induced contractions of the antral strips[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
SB-203186 (0.1-3mg/kg, i.v.) surmountably antagonised 5-HT-evoked tachycardia in anaesthetized Yucatan minipigs or new-born Camborough piglets with similar potency[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 207572-69-8
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Appearance Solid
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Molecular Weight 308.80
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Formel C16H21ClN2O2
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Color White to off-white
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SMILES
O=C(C1=CNC2=C1C=CC=C2)OCCN3CCCCC3.Cl
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°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)
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 100 mg/mL (323.83 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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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: ≥ 2.5 mg/mL (8.10 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 (8.10 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 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.
Reinheit & Dokumentation
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Data Sheet (277 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)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. S G Parker, et al. Blockade of human and porcine myocardial 5-HT4 receptors by SB 203186. Naunyn Schmiedebergs Arch Pharmacol. 1995 Dec;353(1):28-35. [Content Brief]
[2]. Tohru Komada, et al. Pharmacological characterization of 5-Hydroxytryptamine-receptor subtypes in circular muscle from the rat stomach. Biol Pharm Bull. 2007 Mar;30(3):508-13. [Content Brief]
[3]. P G McLean, et al. 5-HT4 receptor antagonist affinities of SB207710, SB205008, and SB203186 in the human colon, rat oesophagus, and guinea-pig ileum peristaltic reflex. Naunyn Schmiedebergs Arch Pharmacol. 1995 Aug;352(2):132-40. [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 | 3.2383 mL | 16.1917 mL | 32.3834 mL | 80.9586 mL |
| 5 mM | 0.6477 mL | 3.2383 mL | 6.4767 mL | 16.1917 mL | |
| 10 mM | 0.3238 mL | 1.6192 mL | 3.2383 mL | 8.0959 mL | |
| 15 mM | 0.2159 mL | 1.0794 mL | 2.1589 mL | 5.3972 mL | |
| 20 mM | 0.1619 mL | 0.8096 mL | 1.6192 mL | 4.0479 mL | |
| 25 mM | 0.1295 mL | 0.6477 mL | 1.2953 mL | 3.2383 mL | |
| 30 mM | 0.1079 mL | 0.5397 mL | 1.0794 mL | 2.6986 mL | |
| 40 mM | 0.0810 mL | 0.4048 mL | 0.8096 mL | 2.0240 mL | |
| 50 mM | 0.0648 mL | 0.3238 mL | 0.6477 mL | 1.6192 mL | |
| 60 mM | 0.0540 mL | 0.2699 mL | 0.5397 mL | 1.3493 mL | |
| 80 mM | 0.0405 mL | 0.2024 mL | 0.4048 mL | 1.0120 mL | |
| 100 mM | 0.0324 mL | 0.1619 mL | 0.3238 mL | 0.8096 mL |
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