| Identification | Back Directory | [Name]
Olumacostat Glasaretil | [CAS]
1261491-89-7 | [Synonyms]
DRM01B
DRM-01B
DRM 01B.
Olumacostat
Olumacostat Glasaretil
OLUMACOSTAT GLASARETIL; DRM01B; DRM-01B; DRM 01B.
2-Furancarboxylic acid, 5-(tetradecyloxy)-, 2-[(2-ethoxy-2-oxoethyl)methylamino]-2-oxoethyl ester | [Molecular Formula]
C26H43NO7 | [MDL Number]
MFCD30533440 | [MOL File]
1261491-89-7.mol | [Molecular Weight]
481.62 |
| Chemical Properties | Back Directory | [Boiling point ]
583.9±50.0 °C(Predicted) | [density ]
1.057±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO:125.0(Max Conc. mg/mL);259.54(Max Conc. mM) | [form ]
Solid | [pka]
-1.44±0.70(Predicted) | [color ]
White to light yellow |
| Hazard Information | Back Directory | [Uses]
Olumacostat glasaretil (DRM01) is a small molecule inhibitor of acetyl coenzyme A carboxylase (ACC). | [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, 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]. | [storage]
Store at -20°C | [References]
[1] Hunt DW, et al. Inhibition of Sebum Production with the Acetyl Coenzyme A Carboxylase Inhibitor OlumacostatGlasaretil. J Invest Dermatol. 2017 Mar 1. pii: S0022-202X(17)30186-0. DOI:10.1016/j.jid.2016.12.031
[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. DOI:10.1016/j.jaad.2016.08.053 |
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