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GSK163090

GSK163090
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).
Catalog No. TQ0311Cas No. 844903-58-8
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Purity:99.20%
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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).
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.
Pack SizePriceAvailabilityQuantity
1 mg$31In Stock
2 mg$44In Stock
5 mg$73In Stock
10 mg$127In Stock
25 mgInquiryIn Stock
50 mgInquiryIn Stock
1 mL x 10 mM (in DMSO)$79In Stock
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Product Introduction

Bioactivity
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-HT1A:9.4 (pKi), 5-HT1B:8.5 (pKi), 5-HT1D:9.7 (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.
Chemical Properties
Molecular Weight415.53
FormulaC25H29N5O
Cas No.844903-58-8
Storage & Solubility Information
StoragePowder: -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
DMSO
1mg5mg10mg50mg
1 mM2.4066 mL12.0328 mL24.0657 mL120.3283 mL
5 mM0.4813 mL2.4066 mL4.8131 mL24.0657 mL
10 mM0.2407 mL1.2033 mL2.4066 mL12.0328 mL
20 mM0.1203 mL0.6016 mL1.2033 mL6.0164 mL

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Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
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Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSOTargetMol | reagent (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 DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify
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