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GSK163090
Catalog No. TQ0311Cas No. 844903-58-8
GSK163090 is a specific and orally active 5-HT1A/B/D receptor antagonist (pKis: 9.4/8.5/9.7, and 6.3/6.7 for 5-HT1A/B/D, and dopamine D2/D3).
GSK163090
Catalog No. TQ0311Cas No. 844903-58-8
GSK163090 is a specific and orally active 5-HT1A/B/D receptor antagonist (pKis: 9.4/8.5/9.7, and 6.3/6.7 for 5-HT1A/B/D, and dopamine D2/D3).
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $31 | In Stock | |
| 2 mg | $44 | In Stock | |
| 5 mg | $73 | In Stock | |
| 10 mg | $127 | In Stock | |
| 25 mg | Inquiry | In Stock | |
| 50 mg | Inquiry | In Stock | |
| 1 mL x 10 mM (in DMSO) | $79 | In Stock |
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Purity:99.20%
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All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.Product Introduction
Bioactivity
Chemical Properties
| Description | GSK163090 is a specific and orally active 5-HT1A/B/D receptor antagonist (pKis: 9.4/8.5/9.7, and 6.3/6.7 for 5-HT1A/B/D, and dopamine D2/D3). |
| Targets&IC50 | 5-HT1D:9.7 (pKi), 5-HT1A:9.4 (pKi), 5-HT1B:8.5 (pKi) |
| In vitro | GSK163090 demonstrates clear dose-dependent inhibition of the 8-OH-DPAT-induced hyper locomotor activity (hLMA), with ED50 values ranging from 0.03 to 1 mg/kg. GSK163090 was devoid of agonist activity at R1 receptors, but rather it demonstrated a moderate functional antagonism of the phenylephrine-induced contraction of rabbit aorta (pIC50: 6.9). |
| In vivo | The superior quality of GSK163090 was further highlighted by its commendable in vivo pharmacokinetic profile in rats and its outstanding activity in the 5-HT1A PD model, where 50% efficacy was achieved at a blood concentration of 3 ng/mL. |
| Molecular Weight | 415.53 |
| Formula | C25H29N5O |
| Cas No. | 844903-58-8 |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||
| Solubility Information | DMSO: 14.29 mg/mL (34.39 mM), Sonication is recommended. | |||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||
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(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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