2. GPCR/G Protein
  3. Prostaglandin Receptor
  4. GSK-269984A

GSK-269984A is a Prostaglandin E2 Receptor 1 (EP1) antagonist with a pIC50 of 7.9.

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

GSK-269984A Chemical Structure

GSK-269984A Chemical Structure

CAS No. : 892664-04-9

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of GSK-269984A:

GSK-269984A Related Antibodies

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

GSK-269984A is a Prostaglandin E2 Receptor 1 (EP1) antagonist with a pIC50 of 7.9.

IC50 & Target[1]

EP1

7.9 (pIC50)

In Vitro

Results from [3H]-PGE2 binding assay in CHO cells overexpressing the human EP1 receptor demonstrate that GSK-269984A is an antagonist of EP1 receptor with a pIC50 of 7.9. GSK-269984A is found to cause a concentration-dependent rightward shift of the PGE2 dose-response curve and Schild analysis shows that GSK-269984A is a competitive antagonist with pA2 8.1±0.3 and slope 1.0[1].

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

GSK-269984A Related Antibodies
In Vivo

GSK-269984A demonstrates an ED50 of 2.6 mg/kg (po), with the 10 mg/kg dose showing equivalent reversal of hypersensitivity to the standard. GSK-269984A displays moderate blood clearance in the rat and dog and high clearance in the monkey which is reflected in the half-life for each species[1].

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

429.22

Formula

C20H14Cl2FNNaO3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

ClC1=CC(F)=C(COC2=CC=C(Cl)C=C2CC3=CC=CC(C(O)=O)=N3)C=C1.[Na]
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 7 mg/mL (16.31 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3298 mL 11.6490 mL 23.2981 mL
5 mM 0.4660 mL 2.3298 mL 4.6596 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

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g

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(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References
Animal Administration
[1]

Rats are used in this study. GSK-269984A is progressed to the rat CFA model of inflammatory pain. GSK-269984A is dosed orally at doses of 1, 3 and 10 mg/kg, 23 h after intraplantar administration of the adjuvant. Analgesia is assessed 1 h post-dose of GSK-269984A[1].

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

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3298 mL 11.6490 mL 23.2981 mL 58.2452 mL
5 mM 0.4660 mL 2.3298 mL 4.6596 mL 11.6490 mL
10 mM 0.2330 mL 1.1649 mL 2.3298 mL 5.8245 mL
15 mM 0.1553 mL 0.7766 mL 1.5532 mL 3.8830 mL
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GSK-269984A 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.

Keywords:

GSK-269984A892664-04-9Prostaglandin ReceptorInhibitorinhibitorinhibit

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