PPACKII (trifluoroacetate salt)
(Synonyms: H-D-Phe-Phe-Arg-Chloromethyl Ketone) 目录号 : GC17711An irreversible inhibitor of kallikreins
Cas No.:649748-23-2
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
PPACKII is a specific and irreversible inhibitor of glandular and plasma kallikreins [1].
Human tissue kallikreins (hKs) are a class of secreted serine proteases that involved in the release of vasodepressor peptides or kinins from a plasma substrate. Kallikrein has diverse expression patterns and physiological roles. Kallikrein has been primarily known as cancer biomarkers. Kallikrein has been implicated in many cancer-related processes, such as cell-growth regulation, angiogenesis, invasion and metastasis. Kallikrein could promote or inhibit neoplastic progression individually and/or with the interaction in cascades with other hKs and proteases [2].
PPACKII prevented apolipoprotein proteolysis in dextran sulfate-precipitated human plasma LDL and inhibited serum atrial natriuretic peptide cleavage at micromolar concentrations [1]. It has been reported that PPACKII inactivated the amidolytic activity of native human Hageman Factor (Factor XII) at 5.3 μM [3].
References:
[1]. Byrne R E, Scanu A M. Apolipoprotein B-100 of plasma low density lipoproteins undergoes proteolysis by contact activation factors when plasma is treated with dextran sulfate-500-MgCl2[J]. Journal of lipid research, 1989, 30(1): 109-120.
[2]. Borgoo C A, Diamandis E P. The emerging roles of human tissue kallikreins in cancer[J]. Nature Reviews Cancer, 2004, 4(11): 876-890.
[3]. Silverberg M, Kaplan A P. Enzymatic activities of activated and zymogen forms of human Hageman factor (factor XII)[J]. Blood, 1982, 60(1): 64-70.
Cas No. | 649748-23-2 | SDF | |
别名 | H-D-Phe-Phe-Arg-Chloromethyl Ketone | ||
化学名 | D-phenylalanyl-N-[(1S)-4-[(aminoiminomethyl)amino]-1-(chloroacetyl)butyl]-L-phenylalaninamide, bis(trifluoroacetate) | ||
Canonical SMILES | O=C([C@@H](CC1=CC=CC=C1)N)N[C@@H](CC2=CC=CC=C2)C(N[C@H](C(CCl)=O)CCCNC(N)=N)=O.FC(F)(C(O)=O)F.FC(F)(C(O)=O)F | ||
分子式 | C25H33ClN6O3 • 2CF3COOH | 分子量 | 729.1 |
溶解度 | ≤30mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide | 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 | 1.3716 mL | 6.8578 mL | 13.7155 mL |
5 mM | 0.2743 mL | 1.3716 mL | 2.7431 mL |
10 mM | 0.1372 mL | 0.6858 mL | 1.3716 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。