1. GPCR/G Protein
  2. EBI2/GPR183

GSK682753A 

Cat. No.: HY-101192 Purity: 98.47%
Handling Instructions

GSK682753A is a selective and highly potent inverse agonist of the epstein-barr virus-induced receptor 2 (EBI2) with an IC50 of 53.6 nM.

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

GSK682753A Chemical Structure

GSK682753A Chemical Structure

CAS No. : 1334294-76-6

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 172 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
5 mg USD 156 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
10 mg USD 264 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
25 mg USD 576 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
50 mg USD 996 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
100 mg USD 1680 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
200 mg   Get quote  
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Description

GSK682753A is a selective and highly potent inverse agonist of the epstein-barr virus-induced receptor 2 (EBI2) with an IC50 of 53.6 nM.

IC50 & Target

IC50: 53.6 nM (EBI2)[1]

In Vitro

GSK682753 is a selective and highly potent inverse agonist for murine as well as human EBI2 with inhibition of G protein-dependent signals as well as signals that are probably G protein-independent. In cAMP-response element-binding protein-based reporter and guanosine5'-3-O-(thio)-triphosphate (GTPγS) binding assays, the potency of this compound is 2.6-53.6 nM, and its inhibitory efficacy is 75%. GSK682753A dose-dependently inhibits EBI2 with an IC50of 53.6 nM. GSK682753A inhibits ERK phosphorylation, GTPγS binding, and cAMP-response element-binding protein activation with similar potency[1].

Solvent & Solubility
In Vitro: 

DMSO : ≥ 27 mg/mL (56.28 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0843 mL 10.4214 mL 20.8429 mL
5 mM 0.4169 mL 2.0843 mL 4.1686 mL
10 mM 0.2084 mL 1.0421 mL 2.0843 mL
*Please refer to the solubility information to select the appropriate solvent.
Cell Assay
[1]

The effect of GSK682753A on cAMP-induced CREB activation is measured. GSK682753A at varying concentrations is added when the transfection is stopped with a DMSO concentration after compound addition of 0.1%. The CREB activity is determined 24 h after transfection using the LucLite substrate[1].

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

Molecular Weight

479.78

Formula

C₂₃H₂₁Cl₃N₂O₃

CAS No.

1334294-76-6

SMILES

O=C1OC2(CCN(C(/C=C/C3=CC=C(Cl)C=C3)=O)CC2)CN1CC4=CC=C(Cl)C(Cl)=C4

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
GSK682753A
Cat. No.:
HY-101192
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GSK682753A

Cat. No.: HY-101192