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Synonyms: R 5188


| Pack Size | Price | USA Stock | Global Stock | Quantity |
|---|---|---|---|---|
| 5 mg | $80 | In Stock | In Stock | |
| 10 mg | $128 | In Stock | In Stock | |
| 25 mg | $263 | In Stock | In Stock | |
| 50 mg | $422 | - | In Stock | |
| 100 mg | $613 | - | In Stock |
| Description | Spiroxatrine (R 5188) is a selective and potent 5-HT1α and α2-adrenergic dual antagonist with sedative activity, and inhibitory effects on 5-HT1α, 5-HT1β, 5-HT2, and dopamine receptors. Spiroxatrine may be used in the study of disorders related to the cardiovascular system. |
| Targets & IC50 | 5-HT1B/D receptor:224000 nM (Ki), 5-HT2 receptor:118.5 nM (Ki), 5-HT1A receptor:3.94 nM (Ki) |
| In vitro | Sproxatrine (0.01-0.1 μM, 15 mins) enhances contraction in the vas deferens tissue of α2A/D-adrenergic receptor knockout mice[2]. |
| In vivo | Sproxatrine (1-25 μg, intraperitoneal injection, 5 days) increases withdrawal latency to thermal and mechanical stimuli in the hind paw of nerve-injured rats and carrageenan-induced inflammatory rats[3]. Sproxatrine (4 mg/kg/day, intraperitoneal injection, 5 minutes) enhances the effect of Fluoxetine in reducing selectively bred alcohol-preferring (P) rat's voluntary oral ethanol intake[3]. |
| Synonyms | R 5188 |
| Molecular Weight | 379.45 |
| Formula | C22H25N3O3 |
| Cas No. | 1054-88-2 |
| Smiles | O=C1C2(N(CN1)C3=CC=CC=C3)CCN(CC4OC=5C(OC4)=CC=CC5)CC2 |
| Relative Density. | 1.32 g/cm3 (Predicted) |
| Storage | Store at low temperature,Keep away from direct sunlight Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO: < 1 mg/mL (insoluble or slightly soluble) |
| In Vivo Formulation | 10% DMSO+90% Saline: < 1.36 mg/mL (3.58 mM), Lower concentrations may be soluble, but exact solubility limit is unknown. 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 1.36 mg/mL (3.58 mM), Suspension. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. |
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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