| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| 100mg | |||
| Other Sizes |
| Targets |
GPR84 antagonist 8 targets GPR84, a member of the metabolic G protein-coupled receptor family expressed largely in immune cells. GPR84 is involved in various physiological processes, including immune response and inflammation. The compound acts as a selective antagonist of this receptor.
|
|---|---|
| ln Vitro |
GPR84 is a member of the metabolic G protein-coupled receptor family, whose expression has been largely documented in immune cells. To test the notion that preventing GPR84 activation could be a possible anti-inflammatory therapy in diverse inflammatory disorders, GPR84 antagonists 8 were utilized. The efficacy and specificity of GPR84 antagonist 8 was investigated in cAMP assay employing GPR84-CHO cells. GPR84 antagonist 8 significantly suppresses the effect of 6-OAU on decreasing cAMP generation in GPR84-CHO cells. To investigate the inhibitory effect of GPR84 antagonist 8 on the proinflammatory consequences of GPR84 activation in macrophages, LPS-pretreated BMDM were incubated with 10 µM GPR84 antagonist 8 for 30 min, and then 1 µM 6-OAU was added. Western Blot protein analysis showed that GPR84 antagonist 8 partly prevented 6-OAU-induced AKT and ERK phosphorylation [1].
In vitro, GPR84 antagonist 8 significantly suppresses the effect of 6-OAU on decreasing cAMP generation in GPR84-CHO cells. The compound (10 microM, 30 minutes) is used to treat lipopolysaccharide (LPS)-pretreated bone marrow-derived macrophages (BMDMs), followed by the addition of 1 microM 6-OAU. It abrogates the enhanced inflammatory response mediated by 6-OAU. |
| ln Vivo |
In vivo activity data for GPR84 antagonist 8 are not extensively documented. As a selective GPR84 antagonist, the compound is expected to reduce inflammatory responses associated with GPR84 activation in vivo. It is applicable for investigating inflammatory and fibrotic diseases. Further in vivo studies would be needed to characterize its pharmacokinetic and efficacy profile.
|
| Enzyme Assay |
The in vitro receptor binding and functional assay for GPR84 uses GPR84-CHO cells. Cells are treated with GPR84 antagonist 8 at various concentrations, then stimulated with 6-OAU (a GPR84 agonist). cAMP levels are measured by ELISA or homogeneous time-resolved fluorescence (HTRF) to assess receptor antagonism. IC₅0 values are calculated from dose-response curves.
|
| Cell Assay |
For in vitro cell-based assays, bone marrow-derived macrophages (BMDMs) are isolated and cultured. Cells are pre-treated with LPS to induce an inflammatory state, then treated with GPR84 antagonist 8 (10 microM, 30 minutes) followed by 6-OAU (1 microM). Inflammatory cytokine production (such as TNF-alpha, IL-6) is measured by ELISA. Cell viability is assessed using standard proliferation assays. Experiments are typically performed in triplicate.
|
| Animal Protocol |
In vivo animal studies for GPR84 antagonist 8 would typically involve mouse models of inflammation or fibrosis. The compound is administered orally or intraperitoneally at various doses. Inflammatory markers are measured in serum or tissue samples. Efficacy is evaluated by reduction in inflammatory or fibrotic parameters. Target engagement may be confirmed by assessing GPR84 signaling in tissues.
|
| ADME/Pharmacokinetics |
Pharmacokinetic properties of GPR84 antagonist 8 are not extensively documented. The compound has molecular weight 421.45 and molecular formula C23H23N3O₅. It is soluble in DMSO and typically formulated for in vitro and in vivo studies. Further detailed PK parameters (half-life, Cmax, AUC, bioavailability) would require dedicated studies. Storage at -20degC is recommended.
|
| Toxicity/Toxicokinetics |
Toxicological data for GPR84 antagonist 8 are not well characterized in the public domain. As a research chemical, standard safety precautions should be observed. The compound is for laboratory use only and not intended for human therapeutic applications. GPR84 antagonists as a class may have potential effects on immune function. Comprehensive toxicity profiling would be required for therapeutic development.
|
| References | |
| Additional Infomation |
GPR84 antagonist 8 (CAS# 1445846-30-9) is a selective GPR84 antagonist. It inhibits 6-OAU-mediated cAMP reduction in GPR84-CHO cells and abrogates enhanced inflammatory responses. The compound has molecular formula C23H23N3O₅ and molecular weight 421.45. It is used in inflammation and fibrosis research and is not approved for clinical use.
|
| Molecular Formula |
C23H23N3O5
|
|---|---|
| Molecular Weight |
421.445825815201
|
| Exact Mass |
421.163
|
| CAS # |
1445846-30-9
|
| PubChem CID |
71598639
|
| Appearance |
Off-white to light yellow solid powder
|
| LogP |
1.5
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
6
|
| Heavy Atom Count |
31
|
| Complexity |
711
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
C12=CC(OCC3COCCO3)=NC(=O)N1CCC1=C2C=CC(OCC2=NC=CC=C2)=C1
|
| InChi Key |
KSGKMLVYIUJQMZ-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C23H23N3O5/c27-23-25-22(31-15-19-14-28-9-10-29-19)12-21-20-5-4-18(11-16(20)6-8-26(21)23)30-13-17-3-1-2-7-24-17/h1-5,7,11-12,19H,6,8-10,13-15H2
|
| Chemical Name |
2-(1,4-dioxan-2-ylmethoxy)-9-(pyridin-2-ylmethoxy)-6,7-dihydropyrimido[6,1-a]isoquinolin-4-one
|
| 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) |
DMSO : ~5 mg/mL (~11.86 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.54 mg/mL (1.28 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 5.4 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 0.54 mg/mL (1.28 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 5.4 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 0.54 mg/mL (1.28 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3728 mL | 11.8638 mL | 23.7276 mL | |
| 5 mM | 0.4746 mL | 2.3728 mL | 4.7455 mL | |
| 10 mM | 0.2373 mL | 1.1864 mL | 2.3728 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
