GW 280264X
(Synonyms: ((S)-5-((2R,3S)-3-(N-羟基甲酰胺基)-2-异丁基六氨基)-2-氧代-6-(噻唑-2-基氨基)己基)氨基甲酸苄酯) 目录号 : GC48421An ADAM17/TACE and ADAM10 inhibitor
Cas No.:866924-39-2
Sample solution is provided at 25 µL, 10mM.
GW 280264X is an inhibitor of disintegrin and metalloproteinase domain-containing protein 17/TNF-α converting enzyme (ADAM17/TACE) and ADAM10 (IC50s = 8 and 11.5 nM, respectively).1 It inhibits TNF-α-induced cleavage of endomucin in human umbilical vein endothelial cells (HUVECs) when used at a concentration of 10 µM.2 GW 280264X (1 and 10 µM) inhibits angiotensin-converting enzyme 2 (ACE2) ectodomain shedding induced by phorbol 12-myristate 13-acetate in HEK-ACE2 cells.3 It reduces ACE2 shedding and prevents severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) infection in HK-2 cells.4
1.Hundhausen, C., Misztela, D., Berkout, T.A., et al.The disintegrin-like metalloproteinase ADAM10 is involved in constitutive cleavage of CX3CL1 (fractalkine) and regulates CX3CL1-mediated cell-cell adhesionBlood102(4)1186-1195(2003) 2.Yang, J., LeBlanc, M.E., Cano, I., et al.ADAM10 and ADAM17 proteases mediate proinflammatory cytokine-induced and constitutive cleavage of endomucin from the endothelial surfaceJ. Biol. Chem.295(19)6641-6651(2020) 3.Lambert, D.W., Yarski, M., Warner, F.J., et al.Tumor necrosis factor-alpha convertase (ADAM17) mediates regulated ectodomain shedding of the severe-acute respiratory syndrome-coronavirus (SARS-CoV) receptor, angiotensin-converting enzyme-2 (ACE2)J. Biol. Chem.280(34)30113-30119(2005) 4.Yeung, M.L., Teng, J.L.L., Jia, L., et al.Soluble ACE2-mediated cell entry of SARS-CoV-2 via interaction with proteins related to the renin-angiotensin systemCell1841-17(2021)
Cas No. | 866924-39-2 | SDF | |
别名 | ((S)-5-((2R,3S)-3-(N-羟基甲酰胺基)-2-异丁基六氨基)-2-氧代-6-(噻唑-2-基氨基)己基)氨基甲酸苄酯 | ||
Canonical SMILES | O=CN(O)[C@@H](CCC)[C@@H](CC(C)C)C(N[C@@H](CCCCNC(OCC1=CC=CC=C1)=O)C(NC2=NC=CS2)=O)=O | ||
分子式 | C28H41N5O6S | 分子量 | 575.7 |
溶解度 | DMSO: soluble | 储存条件 | -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 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 1.737 mL | 8.6851 mL | 17.3702 mL |
5 mM | 0.3474 mL | 1.737 mL | 3.474 mL |
10 mM | 0.1737 mL | 0.8685 mL | 1.737 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。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet