Pam2CSK4
目录号 : GC10058
Pam2CSK4是一种有效的TLR2/TLR6激动剂，EC50值为0.015ng/ml。
Cas No.:868247-72-7
Sample solution is provided at 25 µL, 10mM.
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Pam2CSK4 is a potent agonist of TLR2/TLR6, with an EC50 value of 0.015ng/ml[1]. Pam2CSK4 can activate the platelet nuclear factor-κB and Bruton's tyrosine kinase signaling pathway to promote platelet-endothelial cell interaction[2]. Pam2CSK4 has been widely used as an adjuvant for the development of novel vaccines that can significantly improve the titer of antigen-specific neutralizing antibodies and the persistence of humoral immunity[3].
In vitro, Pam2CSK4 treatment (100ng/ml) of nucleus pulposus (NP) cells isolated from nondegenerative intervertebral discs for 48 hours significantly increased the secretion of several proinflammatory cytokines and chemokines such as IL-6, IL-8, CXCL1, GRO, and CCL2[4]. Treatment of RAW264.7 cells with 100ng/ml Pam2CSK4 for 6 hours significantly promoted the expression of iNOS and stimulated the production of NO[5]. Treatment of peripheral blood mononuclear cells (PBM) with 100ng/ml Pam2CSK4 for 24 hours synergistically enhanced IgG-mediated TNFα production and significantly upregulated Fcγ receptor (FcγR) expression[6].
In vivo, Pam2CSK4 administration via intraperitoneal injection at a dose of 250μg/kg/day for 8 days significantly promoted weight gain and colon length increase during colitis onset and alleviated colitis damage in mice[7].
References:
[1] Irvine K L, Hopkins L J, Gangloff M, et al. The molecular basis for recognition of bacterial ligands at equine TLR2, TLR1 and TLR6[J]. Veterinary research, 2013, 44(1): 50.
[2] Parra-Izquierdo I, Lakshmanan H H S, Melrose A R, et al. The toll-like receptor 2 ligand Pam2CSK4 activates platelet nuclear factor-κB and Bruton’s tyrosine kinase signaling to promote platelet-endothelial cell interactions[J]. Frontiers in Immunology, 2021, 12: 729951.
[3] Qiao Y, Zhan Y, Zhang Y, et al. Pam2CSK4-adjuvanted SARS-CoV-2 RBD nanoparticle vaccine induces robust humoral and cellular immune responses[J]. Frontiers in immunology, 2022, 13: 992062.
[4] Krock E, Rosenzweig D H, Currie J B, et al. Toll-like receptor activation induces degeneration of human intervertebral discs[J]. Scientific reports, 2017, 7(1): 17184.
[5] Kulsantiwong P, Pudla M, Srisaowakarn C, et al. Pam2CSK4 and Pam3CSK4 induce iNOS expression via TBK1 and MyD88 molecules in mouse macrophage cell line RAW264. 7[J]. Inflammation Research, 2017, 66(10): 843-853.
[6] Shah P, Fatehchand K, Patel H, et al. Toll-like receptor 2 ligands regulate monocyte Fcγ receptor expression and function[J]. Journal of Biological Chemistry, 2013, 288(17): 12345-12352.
[7] Wang Y, Han J, Yang G, et al. Therapeutic potential of the secreted Kazal-type serine protease inhibitor SPINK4 in colitis[J]. Nature Communications, 2024, 15(1): 5874.
Pam2CSK4是一种有效的TLR2/TLR6激动剂，EC50值为0.015ng/ml[1]。Pam2CSK4可通过激活血小板核因子κB和Bruton's tyrosine kinase信号通路，促进血小板与内皮细胞的相互作用[2]。Pam2CSK4已广泛用作疫苗佐剂，能显著提升抗原特异性中和抗体滴度及体液免疫的持久性[3]。
在体外，使用100ng/ml的Pam2CSK4处理从非退变椎间盘分离的髓核（NP）细胞48小时，能显著促进多种促炎因子和趋化因子的分泌，包括IL-6、IL-8、CXCL1、GRO和CCL2[4]。用100ng/ml的Pam2CSK4处理RAW264.7细胞6小时，可显著促进iNOS表达并刺激一氧化氮生成[5]。以100ng/ml的Pam2CSK4处理人外周血单核细胞(PBM)24小时，能协同增强IgG介导的TNFα产生，并显著上调Fcγ受体(FcγR)表达[6]。
在体内，通过腹腔注射的方式，以250μg/kg/day的剂量给小鼠连续8天服用 Pam2CSK4，显著促进了结肠炎发作期间小鼠体重的增加和结肠长度的延长，并减轻了结肠炎对小鼠的损伤[7]。
| Cell experiment [1]: | |
Cell lines | Caco-2 cells |
Preparation Method | Caco-2 cells were cultured in Dulbecco's modified Eagle's medium (DMEM) supplemented with 10% fetal bovine serum, 100U/ml penicillin, and 100μg/ml streptomycin in a humidified incubator at 37℃ with 5% CO2. Caco-2 cells (4×105cells/ml) were seeded in 96-well culture plates and cultured until complete confluence. Cells were cultured in serum-free DMEM medium for 18h and then treated with 0.1µg/ml Pam2CSK4 for 24h. Cell culture supernatants were collected and IL-8 production was measured. |
Reaction Conditions | 0.1µg/ml; 24h |
Applications | Pam2CSK4 treatment significantly enhanced IL-8 levels in Caco-2 cells. |
| Animal experiment [2]: | |
Animal models | BALB/c mice |
Preparation Method | BALB/c mice were raised in a standard environment and had free access to food and water. 3% dextran sulfate sodium (DSS), with a molecular weight of 36,000-50,000Da, was added to the drinking water of the mice for 7 days. At the same time, from the first day of DSS administration, Pam2CSK4 was intraperitoneally injected for 8 consecutive days at a dose of 250μg/kg/day. The mouse samples were collected for analysis. |
Dosage form | 250μg/kg/day for 8 days; i.p. |
Applications | Pam2CSK4 treatment promoted weight gain and colon length increase during colitis onset and alleviated colitis damage in mice. |
References: | |
| Cas No. | 868247-72-7 | SDF | |
| 化学名 | (2S,3Z,5S,6Z,8S,9Z,11S,12Z,14S,15Z,17R,21R)-17-amino-2,5,8,11-tetrakis(4-aminobutyl)-4,7,10,13,16-pentahydroxy-14-(hydroxymethyl)-24-oxo-21-(palmitoyloxy)-23-oxa-19-thia-3,6,9,12,15-pentaazanonatriaconta-3,6,9,12,15-pentaen-1-oic acid | ||
| Canonical SMILES | CCCCCCCCCCCCCCCC(OC[C@](OC(CCCCCCCCCCCCCCC)=O)([H])CSC[C@@](N)([H])/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)=O | ||
| 分子式 | C65H126N10O12S | 分子量 | 1271.83 |
| 溶解度 | Soluble to 1 mg/ml in 0.25% acetic acid | 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 786.3 μL | 3.9313 mL | 7.8627 mL |
| 5 mM | 157.3 μL | 786.3 μL | 1.5725 mL |
| 10 mM | 78.6 μL | 393.1 μL | 786.3 μL |
| 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
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- Purity: >99.00%
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