TLR7 agonist 1
Based on 1 Customer Validation
TLR7 agonist 1 is a selective TLR7 agonist with an LEC value of 90 nM. TLR7 agonist 1 activates downstream immune regulation and shows no activity against TLR8. TLR7 agonist 1 induces endogenous IFN-α production in mice.
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- 純度: 98.19%
- CAS 番号: 2178156-33-5
- 分子式: C21H25N5O
- 分子量:363.46
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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
生物活性
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TLR7 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | CC50 |
>25 μM
Compound: 48
|
Cytotoxic activity against HEK293 cells assessed as reduction in cell viability incubated for 6 hrs
Cytotoxic activity against HEK293 cells assessed as reduction in cell viability incubated for 6 hrs
|
[PMID: 29366653] |
TLR7 agonist 1 (compound 48) (0.09 μM) is a highly potent, TLR7-selective agonist (SI >200 over TLR8) in HEK-293 cells transiently transfected with human TLR7, with an hTLR7 LEC of 0.09 μM[1].
TLR7 agonist 1 (0.14 μM) induces IFN-α in hPBMCs with an LEC50 of 0.14 μM[1].
TLR7 agonist 1 (>25 μM) has low cytotoxicity in HEK-293 cells[1].
TLR7 agonist 1 (1 μM; 15 min) exhibits moderate metabolic stability in human liver microsomes[1].
TLR7 agonist 1 (10 μM) shows no CYP inhibition up to 10 μM in human liver microsomes[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | Tmax | Cmax | AUC0-last |
|---|---|---|---|---|---|
| Rat[1] | 5 mg/kg | p.o. | 1 h | 142 ng/mL | 365 ng·h/mL |
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 2178156-33-5
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性状 Solid
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分子量 363.46
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分子式 C21H25N5O
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Color Off-white to light yellow
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SMILES
NC1=NC2=C(C(C(N[C@@H](C)C3=CC=CC=C3)=O)=CC=C2)C(NCCCC)=N1
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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
溶剤 & 溶解度
DMSO : ≥ 100 mg/mL (275.13 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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)
純度とドキュメンテーション
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データシート (278 KB)
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SDS (251 KB)
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- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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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 | 2.7513 mL | 13.7567 mL | 27.5133 mL | 68.7834 mL |
| 5 mM | 0.5503 mL | 2.7513 mL | 5.5027 mL | 13.7567 mL | |
| 10 mM | 0.2751 mL | 1.3757 mL | 2.7513 mL | 6.8783 mL | |
| 15 mM | 0.1834 mL | 0.9171 mL | 1.8342 mL | 4.5856 mL | |
| 20 mM | 0.1376 mL | 0.6878 mL | 1.3757 mL | 3.4392 mL | |
| 25 mM | 0.1101 mL | 0.5503 mL | 1.1005 mL | 2.7513 mL | |
| 30 mM | 0.0917 mL | 0.4586 mL | 0.9171 mL | 2.2928 mL | |
| 40 mM | 0.0688 mL | 0.3439 mL | 0.6878 mL | 1.7196 mL | |
| 50 mM | 0.0550 mL | 0.2751 mL | 0.5503 mL | 1.3757 mL | |
| 60 mM | 0.0459 mL | 0.2293 mL | 0.4586 mL | 1.1464 mL | |
| 80 mM | 0.0344 mL | 0.1720 mL | 0.3439 mL | 0.8598 mL | |
| 100 mM | 0.0275 mL | 0.1376 mL | 0.2751 mL | 0.6878 mL |