MK-8245 Trifluoroacetate
(Synonyms: 5-[3-[4-(2-溴-5-氟苯氧基)-1-哌啶基]-5-异恶唑基]-2H-四唑-2-乙酸三氟乙酸盐) 目录号 : GC36626
A stearoyl-CoA desaturase inhibitor
Cas No.:1415559-41-9
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
MK-8245 is a liver-targeted inhibitor of stearoyl-CoA desaturase (SCD; IC50s = 3, 3, and 1 nM for rat, mouse, and human SCD1, respectively).1 It is selective for SCD1 over Δ5- and Δ6-desaturases (IC50s = >100,000 nM). MK-8245 (20-60 mg/kg) reduces the hepatic, but not Harderian gland, ratio of oleic acid to stearic acid, a marker of chronic SCD activity, and blood glucose levels, without inducing the formation of skin lesions or eye squinting behavior, in a mouse model of high-fat diet-induced obesity. It also inhibits hepatitis C virus (HCV) replication without inducing cytotoxicity in LucNeo2 cells (IC50 = 39.8 nM).2
1.Oballa, R.M., Belair, L., Black, W.C., et al.Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemiaJ. Med. Chem.54(14)5082-5096(2011) 2.Nio, Y., Hasegawa, H., Okamura, H., et al.Liver-specific mono-unsaturated fatty acid synthase-1 inhibitor for anti-hepatitis C treatmentAntiviral Res.132262-267(2016)
| Cas No. | 1415559-41-9 | SDF | |
| 别名 | 5-[3-[4-(2-溴-5-氟苯氧基)-1-哌啶基]-5-异恶唑基]-2H-四唑-2-乙酸三氟乙酸盐 | ||
| Canonical SMILES | O=C(CN1N=C(N=N1)C2=CC(N3CCC(CC3)OC4=CC(F)=CC=C4Br)=NO2)O.FC(C(O)=O)(F)F | ||
| 分子式 | C19H17BrF4N6O6 | 分子量 | 581.27 |
| 溶解度 | Soluble in DMSO | 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。 |
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| 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。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.7204 mL | 8.6019 mL | 17.2037 mL |
| 5 mM | 0.3441 mL | 1.7204 mL | 3.4407 mL |
| 10 mM | 0.172 mL | 0.8602 mL | 1.7204 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。