(S,S)-TAPI-1
(Synonyms: TAPI) 目录号 : GC64535A TACE inhibitor
Cas No.:171235-71-5
Sample solution is provided at 25 µL, 10mM.
TNF-α converting enzyme (TACE, also known as ADAM17) is a zinc metalloprotease that cleaves the membrane-bound precursor of TNF-α to give the mature soluble form of TNF-α.1,2 It also mediates the proteolytic release of several other cell-surface proteins, including TNF-α receptors (TNFRs). TAPI-1, known in the earlier literature as just TAPI, is an inhibitor of TACE that inhibits the cleavage of TNF-α, TNFRI (p60), and TNFRII (p80) with IC50 values ranging from 5-100 ?M.1,3,4 It also blocks the shedding of other TACE-dependent proteins, including IL-6R and Klotho, and may inhibit metalloproteases other than TACE.2,5,6 TAPI-1 differs from TAPI-0 , structurally, by the presence of an aminoethyl addition at the alanyl group, and is generally more stable in tissue culture and in vivo.
1.Mohler, K.M., Sleath, P.R., Fitzner, J.N., et al.Protection against a lethal dose of endotoxin by an inhibitor of tumour necrosis factor processingNature370(6486)218-220(1994) 2.Müllberg, J., Durie, F.H., Otten-Evans, C., et al.A metalloprotease inhibitor blocks shedding of the IL-6 receptor and the p60 TNF receptorJ. Immunol.155(11)5198-5205(1995) 3.Crowe, P.D., Walter, B.N., Mohler, K.M., et al.A metalloprotease inhibitor blocks shedding of the 80-kD TNF receptor and TNF processing in T lymphocytesJ. Exp. Med.181(3)1502-1210(1995) 4.Hooper, N.M., Karran, E.H., and Turner, A.J.Membrane protein secretasesBiochem. J.321(2)265-279(1997) 5.Chen, C.D., Podvin, S., Gillespie, E., et al.Insulin stimulates the cleavage and release of the extracellular domain of klotho by ADAM10 and ADAM17Proc. Natl. Acad. Sci. USA104(50)19796-19801(2007) 6.Yamamoto, K., Miyazaki, K., and Higashi, S.Pericellular proteolysis by matrix metalloproteinase-7 is differentially modulated by cholesterol sulfate, sulfatide, and cardiolipinFEBS J.281(15)3346-3356(2014)
Cas No. | 171235-71-5 | SDF | Download SDF |
别名 | TAPI | ||
分子式 | C26H37N5O5 | 分子量 | 499.6 |
溶解度 | DMSO : 25 mg/mL (50.04 mM; Need ultrasonic) | 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 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 2.0016 mL | 10.008 mL | 20.016 mL |
5 mM | 0.4003 mL | 2.0016 mL | 4.0032 mL |
10 mM | 0.2002 mL | 1.0008 mL | 2.0016 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