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GSK163090
CAS No. 844903-58-8
GSK163090( —— )
Catalog No. M24834 CAS 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).
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 1 mL x 10 mM in DMSO | 75 | In Stock |
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| 2MG | 42 | In Stock |
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| 5MG | 69 | In Stock |
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| 10MG | 121 | In Stock |
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| 100MG | Get Quote | In Stock |
|
| 200MG | Get Quote | In Stock |
|
| 500MG | Get Quote | In Stock |
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| 1G | Get Quote | In Stock |
|
Biological Information
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Product NameGSK163090
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NoteResearch use only, not for human use.
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Brief DescriptionGSK163090 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).
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DescriptionGSK163090 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).(In Vitro):GSK163090 (compound 36) is devoid of agonist activity at R1 receptors, but rather it demonstrates a moderate functional antagonismof the phenylephrineinduced contraction of rabbit aorta (pIC50=6.9).At 1 μM concentration, the ratio of the apparent permeabilities measured from basolateral-to-apical (BA) to apical-to-basolateral (AB) indicated that GSK163090 is a moderate P-glycoprotein (P-gp) substrate (BA/AB = 2.8).(In Vivo):In male Sprague-Dawley rats, GSK163090 (compound 36) treatment shows clear dose-dependent inhibition of the 8-OH-DPAT-induced hyperlocomotor activity (hLMA), with ED50 values ranging from 0.03 to 1 mg/kg.
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In VitroGSK163090 (compound 36) is devoid of agonist activity at R1 receptors, but rather it demonstrates a moderate functional antagonismof the phenylephrineinduced contraction of rabbit aorta (pIC50=6.9).At 1 μM concentration, the ratio of the apparent permeabilities measured from basolateral-to-apical (BA) to apical-to-basolateral (AB) indicated that GSK163090 is a moderate P-glycoprotein (P-gp) substrate (BA/AB = 2.8).
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In VivoIn male Sprague-Dawley rats, GSK163090 (compound 36) treatment shows clear dose-dependent inhibition of the 8-OH-DPAT-induced hyperlocomotor activity (hLMA), with ED50 values ranging from 0.03 to 1 mg/kg.
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Synonyms——
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PathwayEndocrinology/Hormones
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Target5-HT Receptor
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Recptor5-HT1A|5-HT1B|5-HT1D|Dopamine
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Research Area——
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Indication——
Chemical Information
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CAS Number844903-58-8
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Formula Weight415.53
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Molecular FormulaC25H29N5O
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Purity>98% (HPLC)
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SolubilityDMSO:14.29 mg/mL (34.39 mM; Need ultrasonic)
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SMILESCc1ccc(c(N2CCN(CCc3cccc(N(CCN4)C4=O)c3)CC2)ccc2)c2n1
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Chemical Name——
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
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CART (62-76) (rat, h...
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