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| | Olumacostat Glasaretil Basic information |
| Product Name: | Olumacostat Glasaretil | | Synonyms: | Olumacostat Glasaretil;Olumacostat;DRM 01B.;DRM01B;DRM-01B;OLUMACOSTAT GLASARETIL; DRM01B; DRM-01B; DRM 01B.;2-Furancarboxylic acid, 5-(tetradecyloxy)-, 2-[(2-ethoxy-2-oxoethyl)methylamino]-2-oxoethyl ester;inhibit,Olumacostat Glasaretil,ACC, Acetyl Coenzyme A Carboxylase,Inhibitor,Acetyl-CoA Carboxylase | | CAS: | 1261491-89-7 | | MF: | C26H43NO7 | | MW: | 481.62 | | EINECS: | | | Product Categories: | | | Mol File: | 1261491-89-7.mol |  |
| | Olumacostat Glasaretil Chemical Properties |
| 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 |
| | Olumacostat Glasaretil Usage And Synthesis |
| 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]. | | 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 |
| | Olumacostat Glasaretil Preparation Products And Raw materials |
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