[CAS NO. ]  GB-110hydrochloride

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PRODUCTS SPECIFICATIONS

Store
Catalog
HY-120528A
Brand
MCE
CAS
-

DESCRIPTION

Overview

MDL-
Molecular Weight645.23
Molecular FormulaC33H49ClN6O5
SMILESO=C(C1=CC=NO1)N[C@@H](CC2CCCCC2)C(N[C@@H]([C@@H](C)CC)C(NCC3=CC=CC(C(N4CCC(CN)CC4)=O)=C3)=O)=O.Cl

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


Summary

GB-110 hydrochloride is a potent, orally active, and nonpeptidic protease activated receptor 2 (PAR2) agonist. GB-110 hydrochloride selectively induces PAR2-mediated intracellular Ca 2+ release in HT29 cells with an EC 50 of 0.28 μM [1] .


IC50 & Target

Protease activated receptor 2 [1]


In Vitro

In an intracellular Ca 2+ (iCa 2+ ) mobilization assay using HT29 colon cancer cells, GB110 (EC 50 240±20 nM; pEC 50 6.7±0.05) is equipotent with the peptide agonist 2f-LIGRLO-NH2 (EC 50 210±30 nM; pEC 50 6.6±0.05), 10-fold more potent than SLIGRL-NH2, but ~35-fold less potent than trypsin (EC 50 6±0.5 nM; pEC 50 8.2±0.8) [2] .

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, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)


Solvent & Solubility

In Vitro:

DMSO : 125 mg/mL ( 193.73 mM ; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.5498 mL 7.7492 mL 15.4983 mL
5 mM 0.3100 mL 1.5498 mL 3.0997 mL
10 mM 0.1550 mL 0.7749 mL 1.5498 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: ≥ 2.33 mg/mL (3.61 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.33 mg/mL (3.61 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.33 mg/mL (3.61 mM); Clear solution

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