Pam3CSK4toll-like receptor 1/2 agonist |
Sample solution is provided at 25 µL, 10mM.
Quality Control & MSDS
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- Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
Chemical structure
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Cas No. | 112208-00-1 | SDF | Download SDF |
Chemical Name | (2S,3Z,5S,6Z,8S,9Z,11S,12Z,14S,15Z,17R)-2,5,8,11-tetrakis(4-aminobutyl)-4,7,10,13,16-pentahydroxy-17-((Z)-(1-hydroxyhexadecylidene)amino)-14-(hydroxymethyl)-24-oxo-21-(palmitoyloxy)-23-oxa-19-thia-3,6,9,12,15-pentaazanonatriaconta-3,6,9,12,15-pentaen-1-oi | ||
Canonical SMILES | CCCCCCCCCCCCCCC/C(O)=N/[C@@](/C(O)=N/[C@@](/C(O)=N/[C@@](/C(O)=N/[C@@](/C(O)=N/[C@@](/C(O)=N/[C@@](C(O)=O)([H])CCCCN)([H])CCCCN)([H])CCCCN)([H])CCCCN)([H])CO)([H])CSCC(OC(CCCCCCCCCCCCCCC)=O)([H])COC(CCCCCCCCCCCCCCC)=O | ||
Formula | C81H156N10O13S | M.Wt | 1510.24 |
Solubility | Soluble to 1 mg/ml in 50% Ethanol / H2O | Storage | Store at -20°C |
Physical Appearance | White lyophilised solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. |
Pam3CSK4 is an agonist of Toll-like receptor 1/2 (TLR1/2) [1].
Toll-like receptors (TLRs) are proteins that play an important role in the innate immune system. TLRs are mainly expressed in sentinel cells that recognize molecules derived from microbes and then activate immune cell responses.
Pam3CSK4 is a TLR1/2 agonist. Pam3CSK4 increased tyrosine phosphorylation of PLCγ2 and the adaptor protein LAT in a Syk- and src-dependent way. Also, Pam3CSK4 evoked platelet activation [1].
In a mouse rhinitis model sensitized to dermatophagoides farinae allergen, Pam3CSK4 significantly improved the nasal allergic symptoms and reduced total inflammation cells and the eosinophils in bronchoalveolar lavage fluid (BALF). Also, Pam3CSK4 significantly increased IFN-γ release and decreased the levels of IL-13 and total IgE [2]. Pam3CSK4 induced the production of both NO and TNF-ɑ by macrophages [3]. In a murine asthma model challenged with OVA, Pam3CSK4 significantly reduced eosinophilia and total inflammatory cell infiltrate in BALF and inhibited the secretion of IL-4 and IL-5 induced by OVA. Also, Pam3CSK4 reduced the level of IgE and increased the production of IL-12 [4].
References:[1]. F?lker K, Klarstr?m-Engstr?m K, Bengtsson T, et al. The Toll-like receptor 2/1 (TLR2/1) complex initiates human platelet activation via the src/Syk/LAT/PLCγ2 signalling cascade. Cell Signal, 2014, 26(2): 279-286. [2]. Zhou C, Kang XD, Chen Z. A synthetic Toll-like receptor 2 ligand decreases allergic immune responses in a mouse rhinitis model sensitized to mite allergen. J Zhejiang Univ Sci B, 2008, 9(4): 279-285.[3]. Han SH, Kim JH, Seo HS, et al. Lipoteichoic acid-induced nitric oxide production depends on the activation of platelet-activating factor receptor and Jak2. J Immunol, 2006, 176(1): 573-579.[4]. Patel M, Xu D, Kewin P, et al. TLR2 agonist ameliorates established allergic airway inflammation by promoting Th1 response and not via regulatory T cells. J Immunol, 2005, 174(12): 7558-7563.
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《血管紧张素转换酶抑制剂在心血管病中应用的中国专家共识》.PDF(242.69k)
1、测定酶比活力:底物需要过量么?测定时间多长?是否可以加入过量的底物,然后测定3min吸光度的增加值,从吸光度的变化值计算比活力。
2、在酶抑制剂筛选的过程中,是否需要保证底物过量?还是要水浴一定时间让反应完全?我看到文献说用终浓度为0.1μmol/mL的底物,终浓度为45U/ml的酶,我想问,假设总体积为1ml,那么终浓度为45U/ml的酶岂不是每分钟能转化4.8μmol的底物?那么0.1μmol/mL的底物不就几秒钟就反应完了?那么怎么测定初速度?
1.对于抑制剂筛选工作(求ic50)是不是体系内酶与底物的量(底物应该是过量的)对实验结果影响不大。
2.如果要求算Km值,是不是需要知道反应产物的绝对量。反应时间文献上都是5分钟,反应速度就用反应产物量除以反应时间即可。
3.酶是进口分装的,规格5U,一次用不完,用PBS稀释后如何保存
谢谢
2、可逆抑制剂:包括
a、竞争性抑制剂,抑制剂与底物竞争性结合酶反应中心,使Km增大,而Vmax不变 b、非竞争性抑制剂,酶与抑制剂结合后还能与底物结合,但活性降低,使Vmax减小,而Km不变
c、反竞争性抑制剂,酶只能与底物结合后才能与抑制剂结合,Vmax与Km都减小
可逆抑制剂可用透析等方法除去,使酶恢复作用
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