| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 100mg | |||
| Other Sizes |
| Targets |
Group VIA calcium-independent phospholipase A2 (GVIA iPLA2).
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|---|---|
| ln Vitro |
GK187 is a potent and specific inhibitor of Group VIA calcium-independent phospholipase A2 (GVIA iPLA2) with an XI(50) value of 0.0001. This extremely low XI(50) value indicates picomolar or sub-picomolar potency. The compound is a polyfluoroalkyl ketone inhibitor with a chemical name of 1,1,1,2,2-pentafluoro-7-(4-methoxyphenyl)heptan-3-one. GK187 may be utilized in the research and study of a variety of neurological diseases. Specific IC50 values for GVIA iPLA2 inhibition are not extensively detailed in publicly available literature but the XI(50) value of 0.0001 suggests extremely high potency.
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| ln Vivo |
In vivo efficacy of GK187 has not been extensively characterized in publicly available literature. As a GVIA iPLA2 inhibitor, it would be expected to have effects on inflammation, lipid metabolism, and possibly neurological function in vivo. Its potential use in neurological disease research suggests that it may have neuroprotective or anti-inflammatory effects in animal models of neurological disorders. Specific animal model data and dosing regimens are limited in publicly available sources.
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| Enzyme Assay |
GVIA iPLA2 inhibition is assessed using in vitro enzyme assays with recombinant or purified GVIA iPLA2 enzyme and a phospholipid substrate (e.g., arachidonoyl-thio-PC). The release of arachidonic acid or other fatty acids is measured. XI(50) values are calculated from dose-response curves. Selectivity is evaluated by testing against other phospholipase A2 isoforms (e.g., cytosolic PLA2, secretory PLA2, other iPLA2 isoforms).
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| Cell Assay |
Cellular activity is evaluated in cells expressing GVIA iPLA2. Cells are treated with GK187 at various concentrations (typically 0.001-100 µM) for appropriate time periods. GVIA iPLA2 activity is measured by assessing the release of arachidonic acid or other lipid mediators. Cell viability, proliferation, and inflammatory responses may be assessed. The effect of GK187 on downstream signaling pathways (e.g., MAPK, NF-κB) may be measured.
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| Animal Protocol |
In vivo studies for GK187 are limited. Potential studies could be conducted in animal models of neurological diseases, such as stroke, traumatic brain injury, Alzheimer's disease, or Parkinson's disease. GK187 would be administered via various routes (oral, intraperitoneal, intravenous). Neurological function, inflammatory markers, and lipid mediator levels would be assessed. Specific protocols are not detailed in publicly available literature.
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| ADME/Pharmacokinetics |
GK187 has a molecular formula of C14H15F5O2 and a molecular weight of 310.26 g/mol. CAS Number: 1071001-50-7. Appearance: Colorless to light yellow liquid. LogP: 5.32. Purity is typically ≥98%. The compound is soluble in DMSO (~100 mg/mL). Storage: Powder at -20°C for 3 years or at 4°C for 2 years; in solvent at -80°C for 6 months or at -20°C for 1 month. It is a polyfluoroalkyl ketone.
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| Toxicity/Toxicokinetics |
Specific toxicological data for GK187 are not extensively published. As a potent enzyme inhibitor, it should be handled with appropriate safety precautions. The compound is for research use only and not for human therapeutic applications without appropriate regulatory approval. Standard laboratory safety practices should be followed, including the use of personal protective equipment and adequate ventilation.
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| References | |
| Additional Infomation |
GK187 is a research tool compound for studying GVIA iPLA2 biology and lipid signaling. It is not approved for clinical use. The compound is a potent and specific inhibitor of GVIA iPLA2, making it a valuable tool for understanding the role of this enzyme in various physiological and pathological processes, including inflammation, cell proliferation, and neurological disorders. GK187's extremely high potency (XI(50) = 0.0001) allows for the selective inhibition of GVIA iPLA2 at very low concentrations, minimizing off-target effects. It is used in research to investigate the therapeutic potential of GVIA iPLA2 inhibition in neurological diseases.
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| Molecular Formula |
C14H15F5O2
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|---|---|
| Molecular Weight |
310.264
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| Exact Mass |
310.099
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| CAS # |
1071001-50-7
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| PubChem CID |
25060072
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| Appearance |
Colorless to light yellow liquid
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
330.3±42.0 °C at 760 mmHg
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| Flash Point |
148.5±22.8 °C
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| Vapour Pressure |
0.0±0.7 mmHg at 25°C
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| Index of Refraction |
1.438
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| LogP |
5.32
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
21
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| Complexity |
333
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| Defined Atom Stereocenter Count |
0
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| SMILES |
FC(C(F)(F)F)(C(CCCCC1C=CC(=CC=1)OC)=O)F
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| InChi Key |
CICDFDPOGZQTQB-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C14H15F5O2/c1-21-11-8-6-10(7-9-11)4-2-3-5-12(20)13(15,16)14(17,18)19/h6-9H,2-5H2,1H3
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| Chemical Name |
1,1,1,2,2-pentafluoro-7-(4-methoxyphenyl)heptan-3-one
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| Synonyms |
GK 187; GK-187; GK187
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~322.31 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.06 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 25.0 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: ≥ 2.5 mg/mL (8.06 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 25.0 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: ≥ 2.5 mg/mL (8.06 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 | 3.2231 mL | 16.1155 mL | 32.2310 mL | |
| 5 mM | 0.6446 mL | 3.2231 mL | 6.4462 mL | |
| 10 mM | 0.3223 mL | 1.6116 mL | 3.2231 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.
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