[CAS NO. 1334294-76-6]  GSK682753A

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PRODUCTS SPECIFICATIONS [1334294-76-6]

Catalog
HY-101192
Brand
MCE
CAS
1334294-76-6

DESCRIPTION [1334294-76-6]

Overview

MDL-
Molecular Weight479.78
Molecular FormulaC23H21Cl3N2O3
SMILESO=C1OC2(CCN(C(/C=C/C3=CC=C(Cl)C=C3)=O)CC2)CN1CC4=CC=C(Cl)C(Cl)=C4

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


Summary

GSK682753A is a selective and highly potent inverse agonist of the epstein-barr virus-induced receptor 2 ( EBI2 ) with an IC 50 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 IC 50 of 53.6 nM. GSK682753A inhibits ERK phosphorylation, GTPγS binding, and cAMP-response element-binding protein activation with similar potency [1] .

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


Appearance

Solid


Shipping

Room temperature in continental US; may vary elsewhere.


Storage

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)


Solvent & Solubility

In Vitro:

DMSO : ≥ 100 mg/mL ( 208.43 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.
In Vivo:
  • 1.

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

    Solubility: 2.5 mg/mL (5.21 mM); Suspended solution; Need ultrasonic

  • 2.

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

    Solubility: 2.08 mg/mL (4.34 mM); Suspended solution; Need ultrasonic

  • 3.

    Add each solvent one by one: 10% DMSO >> 90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.34 mM); Clear solution

* All of the co-solvents are available by MCE.