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Olumacostat glasaretil (OG) is a novel and potent acetyl-CoA carboxylase inhibitor with anti-inflammatory effects. Acetyl-COA carboxylase is the key enzyme for the first, rate-limiting step in de novo fatty acid synthesis. Olumacostat glasaretil can inhibit in vitro human sebocyte lipid production, it can also reduce in vivo sebaceous gland size in hamster ears.
| ln Vitro |
The acetyl coenzyme One rate-limiting step in the production of fatty acids is controlled by a carboxylase. The de novo lipid synthesis in both primary and modified human sebocytes is inhibited by olumacostat glasaretil. Olumbacostat glasaretil lowers fatty acid synthesis to baseline levels or less at 3 μM. For SEB-1 cells treated with olumacostat glasaretil at 20 μM, 14C-acetate incorporation levels are 85%-90% lower than those of control samples. Lumacostat glasaretil, at 3 μM, decreases control values in sebocyte triacylglycerol, cholesteryl/wax ester, diacylglycerol, cholesterol, and phospholipid by, on average, 86%, 57%, 51%, 39%, and 37%, respectively[1].
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| ln Vivo |
Olumacostat glasaretil is a pro-drug intended to improve in vivo administration of 5-(tetradecyloxy)-2-furoic acid (TOFA), an ACC inhibitor. The size of the sebaceous glands in hamster ears is greatly reduced by topical application of olumacostat glasaretil, but not TOFA. The olumacostat glasaretil administration raises ACC levels and the ratio of acetyl-CoA to free CoA in the studied animals, indicating accelerated fatty acid oxidation, according to HPLC analysis of hamster ear extracts. These modifications align with the inhibition of ACC. In comparison to the surrounding dermis, OG administered to Yorkshire pig ears accumulates in sebaceous glands, according to matrix-assisted laser desorption/ionization (MALDI) imaging[1]. By week 12, patients receiving OG therapy had more patients with investigator global evaluation score improvements of at least two grades and more decreases in both inflammatory and noninflammatory lesions from baseline[2].
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| 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.
[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 |
| Molecular Formula |
C26H43NO7
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|---|---|
| Molecular Weight |
481.63
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| Exact Mass |
481.304
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| CAS # |
1261491-89-7
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| SMILES |
O(C1=C([H])C([H])=C(C(=O)OC([H])([H])C(N(C([H])([H])[H])C([H])([H])C(=O)OC([H])([H])C([H])([H])[H])=O)O1)C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H]
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| Synonyms |
DRM-01B DRM01B Olumacostat glasaretil
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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 : ~125 mg/mL (~259.54 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.32 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 20.8 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: 2.08 mg/mL (4.32 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 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: ≥ 2.08 mg/mL (4.32 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 | 2.0763 mL | 10.3814 mL | 20.7628 mL | |
| 5 mM | 0.4153 mL | 2.0763 mL | 4.1526 mL | |
| 10 mM | 0.2076 mL | 1.0381 mL | 2.0763 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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