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SB-616234-A
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Catalog No. T12847Cas No. 908601-49-0
Alias SB-616234A
SB-616234-A is a selective, orally bioavailable antagonist of the 5-HT1B receptor with anxiolytic and antidepressant properties.
SB-616234-A
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Purity: 99.72%
Catalog No. T12847Alias SB-616234ACas No. 908601-49-0
SB-616234-A is a selective, orally bioavailable antagonist of the 5-HT1B receptor with anxiolytic and antidepressant properties.
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $64 | In Stock | In Stock | |
| 5 mg | $161 | In Stock | In Stock | |
| 10 mg | $232 | In Stock | In Stock | |
| 25 mg | $352 | In Stock | In Stock | |
| 50 mg | $475 | In Stock | In Stock | |
| 1 mL x 10 mM (in DMSO) | $203 | In Stock | In Stock |
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.72%
Appearance:Solid
Color:White
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Product Introduction
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | SB-616234-A is a selective, orally bioavailable antagonist of the 5-HT1B receptor with anxiolytic and antidepressant properties. |
| In vitro | SB-616234A possesses high affinity for human 5-HT1B receptors stably expressed in Chinese hamster ovary (CHO) cells (pKi 8.3 ± 0.2). Similarly, rat and guinea pig striatal 5-HT1B receptors affinity (pKi) of 9.2 ± 0.1. In [35S]-GTPγS binding studies in the human recombinant cell line, SB-616234A acts as a high affinity antagonist with a pA2 value of 8.6 ± 0.2 whilst providing no evidence of agonist activity in this system. In [35S]-GTPγS binding studies in rat striatal membranes, SB-616234A acts as a high affinity antagonist with an apparent pKB of 8.4 ± 0.5, again whilst providing no evidence of agonist activity in this system. SB-616234A (1 μM) potentiates electrically stimulated [3H]-5-HT release from guinea pig and rat cortical slices (S2/S1 ratios of 1.8 and 1.6, respectively)[2]. |
| In vivo | SB-616234A reverses the agonist of 5-HT1/7 receptor, SKF-99101H-induced hypothermia in guinea pigs in a dose related manner with an ED50 of 2.4 mg/kg p.o. SB-616234A produces dose-related anxiolytic effects in both rat and guinea pig maternal separation-induced vocalisation models with an ED50 of 1.0 and 3.3 mg/kg i.p., respectively[1].a dose-dependent inhibition of ex vivo [3H]-GR125743 binding to rat striatal 5-HT1B receptors caused by SB-616234A (0.3-30 mg/kg p.o.) with an ED50 of 2.83 ± 0.39 mg/kg p.o[1]. |
| Synonyms | SB-616234A |
| Molecular Weight | 574.11 |
| Formula | C32H36ClN5O3 |
| Cas No. | 908601-49-0 |
| Smiles | Cl.COc1cc2CCN(C(=O)c3ccc(cc3)-c3ccc(cc3C)-c3noc(C)n3)c2cc1N1C[C@H](C)N[C@H](C)C1 |
| Relative Density. | no data available |
| 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: 5.79 mg/mL (10.09 mM), Sonication is recommended.  | ||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||
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In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Stock Solution Preparation:
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.
Preparation of the In Vivo Formulation:
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.
This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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