RS-127445 hydrochloride
Based on 3 publication(s) in Google Scholar
RS-127445 hydrochloride is a selective, high affinity, orally bioavailable 5-HT2B receptor antagonist with a pKi of 9.5. RS-127445 hydrochloride shows 1000 fold selectivity for this receptor as compared to numerous other receptor and ion channel binding sites.
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- Reinheit: 99.78%
- CAS. Nr.: 199864-86-3
- Formel: C17H17ClFN3
- Molecular Weight:317.79
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Speicherung:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Chemical Information
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Lösungsmittel & Löslichkeit
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Publications Citing Use of MedChemExpress (MCE) RS-127445 hydrochloride
MoreAlle 5-HT Receptor Isoform-spezifische Produkte anzeigen
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Biologische Aktivität
|
sPLA2 5.5 (pKi) |
5-HT2B Receptor |
5-HT3 Receptor <6 (pKi) |
5-HT5 Receptor <6 (pKi) |
5-HT6 Receptor <6 (pKi) |
5-HT2A Receptor 6.3 (pKi) |
5-HT2C Receptor 6.4 (pKi) |
5-HT2B Receptor 9.5 (pKi) |
RS-127445 is found to has nanomolar affinity for the 5-HT2B receptor (pKi=9.5±0.1) and 1,000 fold selectivity for this receptor as compared to numerous other receptor and ion channel binding sites. RS-127445 potently displaces [3H]-5-HT from human recombinant 5-HT2B receptors expressed in CHO-K1 cells. The affinity (pKi value) of RS-127445 for the 5-HT2B receptor is 9.5±0.1 (n=9). RS-127445 is selective for the 5-HT2B receptor, having approximately 1000 fold lower affinity for the human recombinant 5-HT2A, 5-HT2C, 5-HT5, 5-HT6 and 5-HT7 receptors, a 5-HT1A receptor in rat brain membranes, a 5-HT1B/D receptor in bovine caudate, and a monoamine uptake site in rabbit platelets. RS-127445 potently blocks the 5-HT (10 nM) evoked increases in intracellular calcium concentrations in the HEK-293 cells expressing the 5-HT2B receptor (pIC50 of 10.4±0.1). In cells expressing human recombinant 5-HT2B receptors, RS-127445 potently antagonizes 5-HT-evoked formation of inositol phosphates (pKB=9.5±0.1) and 5-HT-evoked increases in intracellular calcium (pIC10=10.4±0.1). RS-127445 also blocks 5-HT-evoked contraction of rat isolated stomach fundus (pA2B=9.5±1.1) and (±)α-methyl-5-HT-mediated relaxation of the rat jugular vein (pA2=9.9±0.3)[1].
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. Nr. 199864-86-3
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Appearance Solid
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Molecular Weight 317.79
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Formel C17H17ClFN3
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Color White to light yellow
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SMILES
NC1=NC(C(C)C)=CC(C2=C3C=CC=CC3=C(F)C=C2)=N1.[H]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
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (3)
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Journal Impact Factor
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Most Recent
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Adv Sci (Weinh)
Activation of HTR2B Suppresses Osteosarcoma Progression through the STAT1-NLRP3 Inflammasome Pathway and Promotes OASL1+ Macrophage Production to Enhance Antitumor Immunity. [Abstract]2025 Aug;12(29):e15276. PMID: 40387572 -
Mol Neurobiol
Htr2b Promotes M1 Microglia Polarization and Neuroinflammation after Spinal Cord Injury via Inhibition of Neuregulin-1/ErbB Signaling. [Abstract]2024 Mar;61(3):1643-1654. PMID: 37747614 -
Lösungsmittel & Löslichkeit
DMSO : 125 mg/mL (393.34 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). 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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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 (7.87 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 (7.87 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.
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.
Protokoll
HEK-293 cells expressing the human 5-HT2B receptor are incubated with [3H]-myoinositol (1.67 μCi/mL) in 162 cm2 flasks overnight at 37°C in an inositol free Ham's F12 medium containing 10% dialyzed foetal bovine serum. The cells are harvested, washed five times with phosphate buffered saline and resuspended in inositol free Ham's F12 media at density of approximately 3×106 cells/mL. RS-127445 (10 μM) is initially dissolved in 10% (v/v) DMSO with 90% inositol free Ham's F12 medium. Subsequent dilutions are made with inositol free Ham's F12 medium. 5-HT is dissolved in inositol free Ham's F12 medium containing 100 mM LiCl and 1 mM ascorbate. RS-127445, vehicle or other antagonists are pre-incubated with 240 μL of cell suspension at 37°C for 20 min. The reactions are initiated by addition of 5-HT. Sixty minutes later, the reactions are terminated by adding 50 μL of ice-cold 20% perchloric acid, chilled in an ice-water bath for 10 min and then neutralized with 160 μL of 1 N KOH. Each sample is diluted with 2 ml of 50 mM Tris-HCl, pH 7.4 at room temperature. The aqueous portion (2.2 mL) is transferred onto Dowex AG1X8 columns (1 ml, 1 : 1, w/v) which had been washed with 5 ml of distilled water. The columns are then washed with 18 ml of distilled water and the inositol phosphates are eluted with 3 ml of 1 N HCl. The eluted radioactivity is determined by liquid scintillation spectroscopy using a Packard 1900CA analyzer[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Rats[1]
Male Sprague-Dawley rats (200 g) are used. To compare the plasma kinetics of RS-127445 following different routes of administration, 90 rats are distributed into three treatment groups of 30 rats each. A single dose of RS-127445 (5 mg/kg) dissolved (2.5 mg/mL) in ethanol:propylene glycol : water (10 : 50 : 40, v:v:v), is administered to each rat. At 0.08, 0.25, 0.5, 1, 2, 4, 8 and 24 h after dosing, the rats are anaesthetized and blood samples are collected by cardiac puncture.
Mice[2]
Adult male C57BL/6J mice (25-30 g) are used. The effects of RS-127445 (1 nM-10 µM, single concentration per tissue, 15 min contact time) or vehicle (5 or 50 µL DMSO) are expressed as the percentage change in amplitude compared with the mean amplitude of four pre-drug, post-EFS contractile responses. The results are analysed using a two-sample equal variance t-test.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
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Data Sheet (282 KB)
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SDS (479 KB)
- English - EN (479 KB)
- Français - FR (479 KB)
- Deutsch - DE (479 KB)
- Norwegian - NO (479 KB)
- Español - ES (479 KB)
- Swedish - SV (479 KB)
- Italian - IT (479 KB)
- Korean - KR (479 KB)
- Portuguese - PT (479 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Bonhaus DW, et al. RS-127445: a selective, high affinity, orally bioavailable 5-HT2B receptor antagonist. Br J Pharmacol. 1999 Jul;127(5):1075-82. [Content Brief]
[2]. Bassil AK, et al. Inhibition of colonic motility and defecation by RS-127445 suggests an involvement of the 5-HT2B receptor in rodent large bowel physiology. Br J Pharmacol. 2009 Sep;158(1):252-8 [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 | 3.1467 mL | 15.7337 mL | 31.4673 mL | 78.6683 mL |
| 5 mM | 0.6293 mL | 3.1467 mL | 6.2935 mL | 15.7337 mL | |
| 10 mM | 0.3147 mL | 1.5734 mL | 3.1467 mL | 7.8668 mL | |
| 15 mM | 0.2098 mL | 1.0489 mL | 2.0978 mL | 5.2446 mL | |
| 20 mM | 0.1573 mL | 0.7867 mL | 1.5734 mL | 3.9334 mL | |
| 25 mM | 0.1259 mL | 0.6293 mL | 1.2587 mL | 3.1467 mL | |
| 30 mM | 0.1049 mL | 0.5245 mL | 1.0489 mL | 2.6223 mL | |
| 40 mM | 0.0787 mL | 0.3933 mL | 0.7867 mL | 1.9667 mL | |
| 50 mM | 0.0629 mL | 0.3147 mL | 0.6293 mL | 1.5734 mL | |
| 60 mM | 0.0524 mL | 0.2622 mL | 0.5245 mL | 1.3111 mL | |
| 80 mM | 0.0393 mL | 0.1967 mL | 0.3933 mL | 0.9834 mL | |
| 100 mM | 0.0315 mL | 0.1573 mL | 0.3147 mL | 0.7867 mL |
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