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GW 280264X Sale

(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 : GC48421

An ADAM17/TACE and ADAM10 inhibitor

GW 280264X Chemical Structure

Cas No.:866924-39-2

规格 价格 库存 购买数量
1mg
¥1,097.00
现货
5mg
¥4,385.00
现货
10mg
¥7,648.00
现货

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Sample solution is provided at 25 µL, 10mM.

Description

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)

化学性质

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
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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 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
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