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Olumacostat Glasaretil

Catalog No. T3510   CAS 1261491-89-7

Olumacostat glasaretil is a small molecule inhibitor of acetyl coenzyme A carboxylase (ACC). It has been used in trials studying the treatment of Acne Vulgaris.

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Olumacostat Glasaretil, CAS 1261491-89-7
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Purity: 98%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Olumacostat glasaretil is a small molecule inhibitor of acetyl coenzyme A carboxylase (ACC). It has been used in trials studying the treatment of Acne Vulgaris.
In vitro 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. Olumacostat glasaretil reduces fatty acid synthesis to at or below baseline levels at 3 μM. 14C-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].
In vivo 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 which suggests 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].
Cell Research Primary human sebocytes are grown to confluence in 96-well plates in sebocyte growth medium and stimulated with 1 μM human insulin and 1 μM liver X receptor (LXR) agonist T0901317 in the presence of increasing concentrations of TOFA or olumacostat glasaretil in culture medium containing 0.1% DMSO. After 24 hours, stimulation/treatment medium is removed and test articles are reapplied in labeling medium containing [14C]-acetate. Following an additional 16 hours, cells are harvested using trypsin/EDTA. Lipid extracts are prepared and the amount of [14C]-acetate incorporation is determined by liquid scintillation as a measure of de novo fatty acid synthesis[1].
Molecular Weight 481.63
Formula C26H43NO7
CAS No. 1261491-89-7


Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

H2O: < 0.1 mg/mL (insoluble)

DMSO: 125 mg/mL (259.54 mM), Need ultrasonic

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Hunt DW, et al. Inhibition of Sebum Production with the Acetyl Coenzyme A Carboxylase Inhibitor OlumacostatGlasaretil. J Invest Dermatol. 2017 Mar 1. pii: S20022-202X(17)320186-0. 2. Bissonnette R, et al. Olumacostat glasaretil, a novel topical sebum inhibitor, in the treatment of acne vulgaris: A phase IIa, multicenter, randomized, vehicle-controlled study. J Am Acad Dermatol. 2017 Jan;76(1):33-39.

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Olumacostat Glasaretil 1261491-89-7 Metabolism Acetyl-CoA Carboxylase inhibit ACC, Acetyl Coenzyme A Carboxylase Inhibitor inhibitor