CAS NO: | 1642857-69-9 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
1mg | 电议 |
5mg | 电议 |
10mg | 电议 |
50mg | 电议 |
100mg | 电议 |
生物活性 | TLR7 agonist2 is a potent and selectiveToll-like Receptor7(TLR7) agonist with aLECof 0.4 μM. | ||||||||||||||||
IC50& Target | LEC: 0.4 μM (TLR7)[1] | ||||||||||||||||
体外研究 (In Vitro) | TLR7 agonist 2 is a potent and selective Toll-like Receptor 7 (TLR7) agonist with a lowest effective concentration (LEC) of 0.4 μM in HEK293 cell. TLR7 agonist 2 is found to be selective for TLR7 over TLR8 with LEC of >100 μM for human TLR8. TLR7 agonist 2 demonstrates low inhibition across five CYP450 isozymes (IC50>10 μM) and is also not a time dependent inhibitor of CYP450 3A4. TLR7 agonist 2 has limited inhibition of the hERG potassium ion channel3H-dofetilide bindingin vitro(IC50>50 μM)[1]. | ||||||||||||||||
体内研究 (In Vivo) | TLR7 agonist 2 is found to be rapidly cleared in conjunction with our target profile. Both Cmaxand AUC increase less than dose proportionally between 0.3 and 3 mg/kg and more than dose-proportionally between 3 and 10 mg/kg. TLR7 agonist 2 can induce an antiviral interferon stimulated gene (ISG) response without inducing an IFNα response at a low dose. TLR7 agonist 2 also induces a 2.7 log decrease in serum HBV viral load from 0.3 mg/kg, and a maximum 3.1 log decrease is observed for doses between 1 and 5 mg/kg[1]. | ||||||||||||||||
分子量 | 336.35 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C17H16N6O2 | ||||||||||||||||
CAS 号 | 1642857-69-9 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
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溶解性数据 | In Vitro: DMSO : 160 mg/mL(475.69 mM;Need ultrasonic and warming) 配制储备液
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