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GSK1940029 (SCD inhibitor 1) Sale

(Synonyms: SCD inhibitor 1) 目录号 : GC32780

GSK1940029 (SCD inhibitor 1) (SCD inhibitor 1) 是从专利 WO/2009060053 A1 化合物实施例 16 中提取的硬脂酰辅酶 A 去饱和酶 (SCD) 抑制剂。

GSK1940029 (SCD inhibitor 1) Chemical Structure

Cas No.:1150701-66-8

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥2,360.00
现货
1mg
¥1,097.00
现货
5mg
¥3,124.00
现货
10mg
¥4,463.00
现货
50mg
¥13,388.00
现货
100mg
¥16,450.00
现货

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Sample solution is provided at 25 µL, 10mM.

产品文档

Quality Control & SDS

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产品描述

GSK1940029 is a stearoyl-coa desaturase (SCD) extracted from patent WO/2009060053 A1, compound example 16.

GSK1940029 is a stearoyl-coa desaturase (SCD), which can be used to treat and/or preventing various diseases, including those mediated by SCD enzyme, such as diseases related to elevated lipid levels, cardiovascular disease, diabetes, obesity, metabolic syndrome, skin disorders such as acne, diseases or conditions related to cancer and the treatment of symptoms linked to the production of the amyloid plaque-forming Aβ42 peptide such as Alzheimer's disease[1].

[1]. Anne Marie Jeanne Bouillot, et al. 1, 2, 3-triazole derivatives for use as stearoyl-coa desaturase inhibitors . PCT Int. Appl. (2009), WO 2009060053 A1 20090514.

Chemical Properties

Cas No. 1150701-66-8 SDF
别名 SCD inhibitor 1
Canonical SMILES ClC(C=CC(CN1N=NC(C(NC2=CC=C(CO)C=C2)=O)=C1C)=C3)=C3Cl
分子式 C18H16Cl2N4O2 分子量 391.25
溶解度 DMSO : ≥ 32 mg/mL (81.79 mM) 储存条件 Store at -20°C
General tips 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

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1 mg 5 mg 10 mg
1 mM 2.5559 mL 12.7796 mL 25.5591 mL
5 mM 0.5112 mL 2.5559 mL 5.1118 mL
10 mM 0.2556 mL 1.278 mL 2.5559 mL
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Research Update

A Phase 1 Randomized, Placebo-Controlled Trial With a Topical Inhibitor of Stearoyl-Coenzyme A Desaturase 1 Under Occluded and Nonoccluded Conditions

Clin Pharmacol Drug Dev 2019 Apr;8(3):270-280.PMID:30650256DOI:PMC6590436

Stearoyl-coenzyme A desaturase 1 (SCD-1) in sebaceous glands is a key enzyme in the synthesis of monounsaturated fatty acids essential for acne development. GSK1940029 gel, a novel SCD-1 inhibitor, is being developed as a potential treatment for acne. To assess the irritation potential, pharmacokinetics (PK), and safety of topical GSK1940029 to the skin of healthy adults, two interdependent studies were conducted in parallel. Study 1 (n = 54) investigated the irritation potential of GSK1940029 (0.3% and 1%, occluded application) to allow for its application to larger surface areas in study 2 (n = 39), which investigated the safety, tolerability, and PK of GSK1940029 after single and repeat doses as occluded and nonoccluded applications. GSK1940029 was not a primary or cumulative irritant after 2 and 21 days of dosing in study 1. In study 2, single and repeat applications of GSK1940029 (0.1% to 1%) doses were well tolerated with little or no influence on AUC and Cmax under occluded or unoccluded conditions. Systemic exposure increased proportionally with surface area and was higher in occluded conditions. Design of these interdependent studies allowed for the assessment of the irritation potential for topical GSK1940029 in parallel with the investigation of PK and safety profiles.