| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
The primary molecular target of GSK-269984B is the prostaglandin E2 receptor EP1, a G protein-coupled receptor that mediates the actions of prostaglandin E2 (PGE2). The EP1 receptor is involved in pain transmission, inflammation, and smooth muscle contraction. GSK-269984B acts as a selective antagonist, blocking PGE2-mediated signaling at the EP1 receptor.
|
|---|---|
| ln Vitro |
In vitro, GSK-269984B is a potent EP1 antagonist. It selectively blocks PGE2-induced signaling at the EP1 receptor. Specific IC50 values for EP1 antagonism have not been extensively reported. The compound demonstrates selectivity for EP1 over other prostanoid receptor subtypes.
|
| ln Vivo |
No dedicated in vivo efficacy studies have been published specifically for GSK-269984B. As an EP1 antagonist, its in vivo applications are primarily in preclinical models of inflammatory pain. No pharmacokinetic parameters, maximum tolerated doses, or in vivo efficacy data are available in the published literature.
|
| Enzyme Assay |
Non-cell-based assays for GSK-269984B use radioligand binding with [3H]PGE2 in membrane preparations from cells expressing recombinant EP1 receptor. Membranes are incubated with radioligand and increasing concentrations of GSK-269984B in assay buffer. Bound radioligand is separated by rapid filtration, and radioactivity is quantified. IC50 values are determined from dose-response curves.
|
| Cell Assay |
Cell-based assays for GSK-269984B use EP1 receptor-expressing cell lines such as HEK293-EP1 or CHO-EP1. Cells are cultured in standard medium, and EP1 receptor-mediated calcium mobilization is measured using Fluo-4 fluorescence. GSK-269984B is added at varying concentrations to determine antagonist potency.
|
| Animal Protocol |
No specific in vivo animal protocols have been established for GSK-269984B. For potential evaluation, the compound could be administered in rodent models of inflammatory pain (e.g., carrageenan-induced paw edema or formalin test). Doses would be determined from pharmacokinetic studies. Endpoints could include pain behavior and paw edema.
|
| References |
| Molecular Formula |
C20H14CL2FNO3
|
|---|---|
| Molecular Weight |
406.23
|
| Exact Mass |
405.033
|
| CAS # |
892664-17-4
|
| PubChem CID |
11495634
|
| Appearance |
Typically exists as solid at room temperature
|
| LogP |
5.395
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
6
|
| Heavy Atom Count |
27
|
| Complexity |
498
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
OC(C1C=CC=C(CC2=CC(Cl)=CC=C2OCC2=CC=C(Cl)C=C2F)N=1)=O
|
| InChi Key |
HJPAXYLYYQIFCK-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C20H14Cl2FNO3/c21-14-6-7-19(27-11-12-4-5-15(22)10-17(12)23)13(8-14)9-16-2-1-3-18(24-16)20(25)26/h1-8,10H,9,11H2,(H,25,26)
|
| Chemical Name |
6-[[5-chloro-2-[(4-chloro-2-fluorophenyl)methoxy]phenyl]methyl]pyridine-2-carboxylic acid
|
| Synonyms |
GSK269984B; GSK 269984B; GSK-269984B
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4617 mL | 12.3083 mL | 24.6166 mL | |
| 5 mM | 0.4923 mL | 2.4617 mL | 4.9233 mL | |
| 10 mM | 0.2462 mL | 1.2308 mL | 2.4617 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
