貨號	規格	價格	上海	北京	武漢	南京
S82634-1mg	98.2%	￥660.00 S82634-1mg ￥660.00 現貨	5 5	-	-	-
S82634-5mg	98.2%	￥1100.00 S82634-5mg ￥1100.00 現貨	5 5	-	-	-
S82634-10mg	98.2%	￥1670.00 S82634-10mg ￥1670.00 現貨	5 5	-	-	-
S82634-50mg	98.2%	￥5000.00 S82634-50mg ￥5000.00 現貨	3 3	-	-	-

產品介紹

Olumacostat glasaretil (DRM01) is a small molecule inhibitor of acetyl coenzyme A carboxylase (ACC).

產品描述：

Olumacostat glasaretil (DRM01) is a small molecule inhibitor of acetyl coenzyme A carboxylase (ACC).

靶點：

Acetyl-CoA Carboxylase;Acetyl-CoACarboxylase

體外研究：

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. 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

體內研究：

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. 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

參考文獻：

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.

溶解性：

soluble in DMSO

保存條件：

-20℃

配置溶液濃度參考：

	1mg	5mg	10mg
1 mM	2.076 ml	10.382 ml	20.763 ml
5 mM	0.415 ml	2.076 ml	4.153 ml
10 mM	0.208 ml	1.038 ml	2.076 ml
50 mM	0.042 ml	0.208 ml	0.415 ml

注意：

部分產品我司僅能提供部分信息，我司不保證所提供信息的權威性，僅供客戶參考交流研究之用。

參考文獻

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