Your shopping cart is empty!
Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
Catalog: | HY-17641 |
Brand: | MCE |
CAS: | 1261491-89-7 |
MDL | - |
---|---|
Molecular Weight | 481.62 |
Molecular Formula | C26H43NO7 |
SMILES | O=C(C1=CC=C(OCCCCCCCCCCCCCC)O1)OCC(N(CC(OCC)=O)C)=O |
Olumacostat glasaretil is a small molecule inhibitor of acetyl coenzyme A carboxylase ( ACC ).
Acetyl coenzyme A carboxylase controls the first, rate limiting step in fatty acid biosynthesis. Olumacostat glasaretil inhibits de novo lipid synthesis in primary and transformed human sebocytes. At 3 μM, olumacostat glasaretil reduces fatty acid synthesis to at or below baseline levels. 14 C-acetate incorporation levels are 85%-90% lower for SEB-1 cultures treated with olumacostat glasaretil at 20 μM compared to control samples. At 3 μM, olumacostat glasaretil reduces sebocyte triacylglycerol, cholesteryl/wax ester, diacylglycerol, cholesterol and phospholipid levels from control values on average by approximately 86%, 57%, 51%, 39% and 37%, respectively [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Olumacostat glasaretil is a pro-drug of the ACC inhibitor 5-(tetradecyloxy)-2-furoic acid (TOFA) and is designed to enhance delivery in vivo . Topical application of olumacostat glasaretil but not TOFA significantly reduces hamster ear sebaceous gland size. HPLC analyses of hamster ear extracts shows that olumacostat glasaretil treatment increases ACC levels and the ratio of acetyl-CoA to free CoA in tested animals, indicating increased fatty acid oxidation. These changes are consistent with ACC inhibition. Matrix-assisted laser desorption/ionization (MALDI) imaging reveals that OG applied onto Yorkshire pig ears accumulates in sebaceous glands relative to the surrounding dermis [1] . At week 12, OG treatment shows greater reductions from baseline in inflammatory lesions and noninflammatory lesions, and more patients with greater than or equal to 2-grade improvement in investigator global assessment score than vehicle [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
NCT Number | Sponsor | Condition | Start Date | Phase |
---|---|---|---|---|
NCT02431052 | Dermira, Inc.|Eli Lilly and Company |
Acne Vulgaris
|
April 2015 | Phase 2 |
NCT01936324 | Dermira, Inc.|Eli Lilly and Company |
Acne Vulgaris
|
August 2013 | Phase 1|Phase 2 |
NCT03028363 | Dermira, Inc.|Eli Lilly and Company |
Acne Vulgaris
|
December 27, 2016 | Phase 3 |
NCT03073486 | Dermira, Inc.|Eli Lilly and Company |
Acne Vulgaris
|
February 6, 2017 | Phase 3 |
NCT03127956 | Dermira, Inc.|Eli Lilly and Company |
Acne Vulgaris
|
March 21, 2017 | Phase 3 |
Solid
Room temperature in continental US; may vary elsewhere.
Powder | -20°C | 3 years |
---|---|---|
4°C | 2 years | |
In solvent | -80°C | 6 months |
-20°C | 1 month |
DMSO : 125 mg/mL ( 259.54 mM ; Need ultrasonic)
Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
---|
1 mM | 2.0763 mL | 10.3816 mL | 20.7633 mL |
5 mM | 0.4153 mL | 2.0763 mL | 4.1527 mL |
10 mM | 0.2076 mL | 1.0382 mL | 2.0763 mL |
Arctom is a premier supply platform offering over 600K unique items of Building Blocks, Bioactive Molecules, Natural Products, ADC PEG Linkers, Antibodies, and other Research Chemicals for global pharmaceutical, biotech, university, and industrial customers. We accelerate your research by providing better and faster purchasing experience & services.