Cu-CPT22

製品コードS8677 バッチS867701

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₁₉H₂₂O₇

分子量

362.37

CAS No.

1416324-85-0

Solubility (25°C)*

体外

DMSO

72 mg/mL (198.69 mM)

Ethanol

9 mg/mL (24.83 mM)

Water

Insoluble

体内（毎回新しく調製した物を用意してください）

Clear solution

10%DMSO 1 40%PEG300 2 5%Tween80 3 45%ddH2O

3.6mg/ml

Taking the 1 mL working solution as an example, add 100 μL of 36 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify it; then continue to add 450 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	CU-CPT22 shows dose-dependent inhibitory effects blocking Pam3CSK4-induced TLR1/2 activation with an IC50 of 0.58 ± 0.09 µM while no significant inhibition to TLR2/6. It demonstrates minimal non-specific inhibition against a panel of 10 representative kinases (PDGFRB, MET, DDR2, SRC, MAPK1, PAK1, AKT1, PKC-γ, CAMK1, and PLK4).
in vitro	CU-CPT22 can compete with the synthetic triacylated lipoprotein (Pam3CSK4) binding to TLR1/2 with high inhibitory activity and specificity. The inhibition constant (Ki) is 0.41 ± 0.07 µM. CU-CPT22 inhibits TLR1/2 signaling without affecting other TLRs, showing it is highly selective in intact cells. It has no significant cytotoxicity at various concentrations up to 100 µM in RAW 264.7 cells using MTT assay. Kinase profiling shows that CU-CPT22 demonstrates minimal non-specific inhibition against a panel of 10 representative kinases (PDGFRB, MET, DDR2, SRC, MAPK1, PAK1, AKT1, PKC-γ, CAMK1, and PLK4). CU-CPT22 suppresses TLR1/2-mediated inflammation response. It inhibits about 60% of TNF-α and 95% of IL-1β at 8 µM in the RAW 264.7 cells^[1].
in vivo	Cu-CPT22 administered before myocardial infarction (MI) significantly suppresses MI-induced upregulation of kidney injury molecule-1 (KIM-1), TLR2, TLR4, MyD88, and chemokine (C-C motif) ligand 2 levels and activation of NF-κB, whereas neutrophil gelatinase-associated lipocalin (NGAL) levels and IL-6 and TNF-α expression levels are unchanged^[2].

プロトコル(参考用のみ)

細胞アッセイ	細胞株	MUTZ-3-derived Langerhans cells (MUTZ-LCs)
	濃度	10 and 25 μM
	反応時間	1 h
	実験の流れ	MUTZ-LCs are seeded in alpha medium without supple-ments and exposed to different microbial and pro-inflammatorystimuli for 24 h (2.5 × 10⁵ cells/ml): 1 μg/ml Pam3CSK4, 1 μg/mlPam2CSK4, 1 μg/ml poly(A:U), 1 μg/ml poly(I:C), 1 μg/ml ultrapurelipopolysaccharide (LPS) from Escherichia coli serotype 0111:B4, 50 ng/ml rh-TNF-α, 30 ng/ml rh-IL-1β, or a cytokine maturation cocktail(CMC) consisting of 50 ng/ml rh-TNF-α, 25 ng/ml rh-IL-1β,100 ng/ml rh-IL-6 and 1 μg/ml PGE2. Cytokines produced in E. coli, contained low endotoxinlevels (≤1.0 EU/μg cytokine) as determined by Limulus Amebo-cyte Lysate (LAL) assay. As control MUTZ-LCs (2.5 × 10⁵ cells/ml) are maintained for 24 hor 48 h in alpha medium only. The TLR2/1 antagonist CU-CPT22 is applied 1 h before stimulation with Pam3CSK4 and Pam2CSK4, respectively.
動物実験	動物モデル	Male LETO and OLETF rats
	投薬量	3 mg/kg
	投与方法	i.p.

参考

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Bifidobacterium adolescentis induces Decorin+ macrophages via TLR2 to suppress colorectal carcinogenesis [ J Exp Clin Cancer Res, 2023, 42(1):172]	PubMed: 37464382
Tongue sole creatine kinases function as DAMP and activate antimicrobial immunity via TLR2 [ Front Immunol, 2023, 14:1142488]	PubMed: 36936949
Lactobacillus johnsonii alleviates colitis by TLR1/2-STAT3 mediated CD206+ macrophagesIL-10 activation [ Gut Microbes, 2022, 14(1):2145843]	PubMed: 36398889
SAA1/TLR2 axis directs chemotactic migration of hepatic stellate cells responding to injury [ iScience, 2021, 24(5):102483]	PubMed: 34113824
MPMBP down-regulates Toll-like receptor (TLR) 2 ligand-induced proinflammatory cytokine production by inhibiting NF-κB but not AP-1 activation. [ Int Immunopharmacol, 2020, 79:106085]	PubMed: 31901621
Autophagy Inhibition and Inammation Activation Induced by Phosphorylated Alpha-synuclein Through Toll-like Receptor 2 Pathway in the Hippocampus of MPTP Mouse Model of Parkinson’s Disease Contribute to Its Cognitive Function Decline in the Early Stage [ Research Square, 2020, 10.21203/rs.3.rs-126752/v1]	PubMed: N/A
Autophagy Inhibition and Inflammation Activation Induced by Phosphorylated Alpha-synuclein Through Toll-like Receptor 2 Pathway in the Hippocampus of [ Research Square, 2020, 10.21203/rs.3.rs-126752/v1]	PubMed: None

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。