CU-CPT-8m
Based on 2 publication(s) in Google Scholar
CU-CPT-8m is a specific TLR8 antagonist, with an IC50 of 67 nM.
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- 純度: 99.98%
- CAS 番号: 125079-83-6
- 分子式: C14H12N4O
- 分子量:252.27
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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MedChemExpress（MCE）の使用を引用している文献 CU-CPT-8m
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RT-PCR
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RT-PCR
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WB
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WB
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Cell Migration/Invasion Assay
生物活性
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TLR8 67 nM (IC50) |
CU-CPT-8m is a specific TLR8 antagonist, with an IC50 of 67±10 nM and negligible cytotoxicity. The Kd value of CU-CPT-8m is determined to be 220 nM. CU-CPT-8m only reduces the proinflammatory response in the TLR8-overexpressing cells strongly supports that CU-CPT-8m directly recognizes TLR8 in cells. It is particularly notable that TLR7 signaling is not affected at concentrations up to 75 μM. TLR7 and TLR8 are closely related and share many common ligands. Treatment of 1 μM CU-CPT-8m completely abolishes the elevation of TNF-α and IL-8 mRNA levels induced by R848. CU-CPT-8m inhibits R848-induced TNF-α production in the differentiated THP-1 monocytes cells in a dose-dependent manner with an IC50 of 90±10 nM, which is in good agreement with its IC50 value determined in HEK-Blue TLR8 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 125079-83-6
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性状 Solid
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分子量 252.27
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分子式 C14H12N4O
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Color White to off-white
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SMILES
O=C(C1=C2N=CC=C(C3=CC=CC(C)=C3)N2N=C1)N
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別名
TLR8-specific antagonist
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (2)
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Journal Impact Factor
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Most Recent
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Rheumatology (Oxford)
TLR8 aggravates skin inflammation and fibrosis by activating skin fibroblasts in systemic sclerosis. [Abstract]2024 May 3;63(6):1710-1719. PMID: 37665747
CU-CPT-8m purchased from MedChemExpress. Usage Cited in: Rheumatology (Oxford). 2024 May 3;63(6):1710-1719. [Abstract]
Cu-cpt-8m (HY-112050; 60 μM) inhibited the upregulation of IL-6, IL-1β, TNF-α, COLI and COLIII induced by VTX-2337 (Motolimod; HY-13773; 10 μM).
CU-CPT-8m purchased from MedChemExpress. Usage Cited in: Rheumatology (Oxford). 2024 May 3;63(6):1710-1719. [Abstract]
Blockade of TLR8 inhibited the fibrosis of human skin fibroblasts. Cu-cpt-8m with 20, 40 or 60 μM inhibited the expression of the α-SMA gene expression in healthy skin fibroblasts induced by TGF-β (10 ng/ml).
CU-CPT-8m purchased from MedChemExpress. Usage Cited in: Rheumatology (Oxford). 2024 May 3;63(6):1710-1719. [Abstract]
Cu-cpt-8m with 20, 40 or 60 μM inhibited the expression of COLI, COLIII and α-SMA proteins in healthy skin fibroblasts induced by TGF-β (10 ng/ml) in 48 h.
CU-CPT-8m purchased from MedChemExpress. Usage Cited in: Rheumatology (Oxford). 2024 May 3;63(6):1710-1719. [Abstract]
The effects of CU-CPT-8m (10 ng/ml) on expression of TLR8, MyD88, p38, P-p38, JNK, P-JNK, JUN, p-JUN, p65, P-p65, smad2/3 and P-smad2/3 induced by TGF-β (10 ng/ml) in healthy skin fibroblasts. Data are represented as mean (s.d.). *P < 0.05. **P < 0.01, ***P < 0.001, ****P < 0.0001
CU-CPT-8m purchased from MedChemExpress. Usage Cited in: Rheumatology (Oxford). 2024 May 3;63(6):1710-1719. [Abstract]
To observe the role of CU-CPT-8m (60 μM) in the migration capability of SSc skin fibroblasts, TGF-β (10 ng/ml) and CU-CPT-8m (60 μM) were used to treat the cells together for 24 h, then the migration capability of the fibroblasts was evaluated.
CU-CPT-8m purchased from MedChemExpress. Usage Cited in: Rheumatology (Oxford). 2024 May 3;63(6):1710-1719. [Abstract]
Inhibition of CU-CPT-8m in the fibrosis and inflammation of skin tissues in BLM-induced SSc mice. The SSc skin fibrosis model was established by s.c. injection of BLM (100 μl/d, 1 mg/ml) once daily for 4 weeks in mice. After BLM was injected subcutaneously for 1 week, the CU-CPT-8m (1 mg/kg/d) was injected subcutaneously for 3 weeks. Masson’s staining was conducted in mouse skin tissues to observe the effect of CU-CPT-8m on the fibrosis of mouse skin tissues.
CU-CPT-8m purchased from MedChemExpress. Usage Cited in: Rheumatology (Oxford). 2024 May 3;63(6):1710-1719. [Abstract]
Inhibition of CU-CPT-8m in the fibrosis and inflammation of skin tissues in BLM-induced SSc mice. The SSc skin fibrosis model was established by s.c. injection of BLM (100 μl/d, 1 mg/ml) once daily for 4 weeks in mice. After BLM was injected subcutaneously for 1 week, the CU-CPT-8m (1 mg/kg/d) was injected subcutaneously for 3 weeks. The effect of CU-CPT-8m on the protein expression level of α-SMA in mouse skin tissues.
CU-CPT-8m purchased from MedChemExpress. Usage Cited in: Rheumatology (Oxford). 2024 May 3;63(6):1710-1719. [Abstract]
Inhibition of CU-CPT-8m in the fibrosis and inflammation of skin tissues in BLM-induced SSc mice. The SSc skin fibrosis model was established by s.c. injection of BLM (100 μl/d, 1 mg/ml) once daily for 4 weeks in mice. After BLM was injected subcutaneously for 1 week, the CU-CPT-8m (1 mg/kg/d) was injected subcutaneously for 3 weeks. Immunohistochemistry was used to evaluate the effect of CU-CPT-8m on the protein expression levels of COLIII, Fn1, CTGF and COLI in skin tissues.
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Infect Immun
Toll-Like Receptor 2 (TLR2) and TLR4 Mediate the IgA Immune Response Induced by Mycoplasma hyopneumoniae. [Abstract]2019 Dec 17;88(1):e00697-19. PMID: 31611272
溶剤 & 溶解度
DMSO : 12.5 mg/mL (49.55 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (9.91 mM); Suspended solution; Need ultrasonic and warming
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 1.25 mg/mL (4.96 mM); Clear solution; Need ultrasonic and warming
This protocol yields a clear solution of 1.25 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
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取扱説明書 (2659 KB)
参考文献
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.9640 mL | 19.8200 mL | 39.6401 mL | 99.1002 mL |
| 5 mM | 0.7928 mL | 3.9640 mL | 7.9280 mL | 19.8200 mL | |
| 10 mM | 0.3964 mL | 1.9820 mL | 3.9640 mL | 9.9100 mL | |
| 15 mM | 0.2643 mL | 1.3213 mL | 2.6427 mL | 6.6067 mL | |
| 20 mM | 0.1982 mL | 0.9910 mL | 1.9820 mL | 4.9550 mL | |
| 25 mM | 0.1586 mL | 0.7928 mL | 1.5856 mL | 3.9640 mL | |
| 30 mM | 0.1321 mL | 0.6607 mL | 1.3213 mL | 3.3033 mL | |
| 40 mM | 0.0991 mL | 0.4955 mL | 0.9910 mL | 2.4775 mL |
CU-CPT-8m 関連分類
HY-112050 関連分類
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