2. GPCR/G Protein Neuronal Signaling
  3. 5-HT Receptor Dopamine Receptor
  4. GSK163090

GSK163090 

Cat. No.: HY-14348 Purity: 99.77%
COA Handling Instructions

GSK163090 is a potent, selective and orally active 5-HT1A/1B/1D receptor antagonist with pKi values of 9.4/8.5/9.7, respectively. GSK163090 inhibits the functional activity of serotonin reuptake transporter (SerT) with a pKi value of 6.1. GSK163090 has antidepressant and anxiolytic activities.

For research use only. We do not sell to patients.

GSK163090 Chemical Structure

GSK163090 Chemical Structure

CAS No. : 844903-58-8

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 209 In-stock
Solution
10 mM * 1 mL in DMSO USD 209 In-stock
Solid
5 mg USD 190 In-stock
10 mg USD 330 In-stock
50 mg USD 1050 In-stock
100 mg USD 1750 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

GSK163090 Related Antibodies

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5-HT1 Receptor 5-HT2 Receptor 5-HT3 Receptor 5-HT4 Receptor 5-HT5 Receptor 5-HT6 Receptor 5-HT7 Receptor 5-HT Receptor

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

GSK163090 is a potent, selective and orally active 5-HT1A/1B/1D receptor antagonist with pKi values of 9.4/8.5/9.7, respectively. GSK163090 inhibits the functional activity of serotonin reuptake transporter (SerT) with a pKi value of 6.1. GSK163090 has antidepressant and anxiolytic activities[1].

IC50 & Target[1]

5-HT1A Receptor

9.4 (pKi)

5-HT1B Receptor

8.5 (pKi)

5-HT1D Receptor

9.7 (pKi)

D2 Receptor

6.3 (pKi)

D3 Receptor

6.7 (pKi)

5-HT2A Receptor

6 (pKi)

5-HT2B Receptor

6.3 (pKi)

5-HT2C Receptor

5.8 (pKi)

Human 5-HT6 Receptor

<5.3 (pKi)

Human 5-HT7 Receptor

6.8 (pKi)

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)[1].
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)[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

GSK163090 Related Antibodies
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[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
Molecular Weight

415.53

Appearance

Solid

Formula

C25H29N5O
CAS No.
SMILES

O=C1NCCN1C2=CC=CC(CCN3CCN(C4=C5C=CC(C)=NC5=CC=C4)CC3)=C2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 14.29 mg/mL (34.39 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4066 mL 12.0328 mL 24.0657 mL
5 mM 0.4813 mL 2.4066 mL 4.8131 mL
10 mM 0.2407 mL 1.2033 mL 2.4066 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 1.43 mg/mL (3.44 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 1.43 mg/mL (3.44 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 1.43 mg/mL (3.44 mM); Clear solution

*All of the co-solvents are available by MedChemExpress (MCE).
Purity & Documentation

Purity: 99.77%

COA (248 KB) LCMS (93 KB)

Handling Instructions (2659 KB)
References
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GSK163090 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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The dilution calculator equation

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This equation is commonly abbreviated as: C1V1 = C2V2

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Keywords:

GSK163090844903-58-8GSK 163090GSK-1630905-HT ReceptorDopamine ReceptorSerotonin Receptor5-hydroxytryptamine Receptor5-HT1A5-HT1B5-HT1DantidepressantanxiolyticSerTP-glycoproteinInhibitorinhibitorinhibit

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