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Synonyms:


| Pack Size | Price | USA Stock | Global Stock | Quantity |
|---|---|---|---|---|
| 1 mg | $714 | In Stock | In Stock | |
| 5 mg | $1,430 | In Stock | In Stock | |
| 10 mg | $1,930 | In Stock | In Stock | |
| 25 mg | $2,870 | In Stock | In Stock | |
| 50 mg | $3,870 | In Stock | In Stock | |
| 100 mg | $5,230 | In Stock | In Stock | |
| 1 mL x 10 mM (in DMSO) | $1,690 | In Stock | In Stock |
| Description | 5-HT2 antagonist 1 is a small molecule antagonist functioning as a 5-HT2B receptor antagonist (IC50 = 33.4 nM), with oral bioactivity and weak inhibition of α1 receptors, employed in research on hepatocellular carcinoma and related diseases. |
| In vitro | Methods: In guinea pig mesenteric arteries, 10 μM serotonin-induced contractions were established, and 10 nM, 100 nM, and 1000 nM of 5-HT2 antagonist 1 were administered to observe the inhibitory effects; in guinea pig aorta, 10 μM norepinephrine-induced contractions were established, and 10 nM and 100 nM of 5-HT2 antagonist 1 were administered to observe the inhibitory effects. Results: 5-HT2 antagonist 1 produced inhibitory effects of 45%, 88%, and 93% at concentrations of 10 nM, 100 nM, and 1000 nM, respectively; inhibitions of 1% and 10% were observed at concentrations of 10 nM and 100 nM, respectively. [1] |
| In vivo | Methods: To investigate the effect of 5-HT2 antagonist 1 (compound 15) on visceral hypersensitivity in irritable bowel syndrome (IBS) rats, 5-HT2B antagonist-1 (compound 15) at 30 mg/kg was administered via oral gavage to IBS rats. Results: 5-HT2B antagonist-1 significantly reduced visceral hypersensitivity in IBS rats. [2] |
| Molecular Weight | 400.49 |
| Formula | C22H29FN4O2 |
| Cas No. | 191592-09-3 |
| Smiles | CN1C2=C(C(=O)N(CCCN3CCN(CC3)C4=CC=C(F)C=C4)CCC2O)C=C1 |
| Relative Density. | 1.28 g/cm3 (Predicted) |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 85 mg/mL (212.24 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density. | ||||||||||||||||||||||||||||||||||||
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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