产品说明书
C-176
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同义名 : | - |
| CAS号 : | 314054-00-7 | |
| 货号 : | A927435 | |
| 分子式 : | C11H7IN2O4 | |
| 纯度 : | 99% | |
| 分子量 : | 358.089 | |
| MDL号 : | MFCD00784208 | |
| 存储条件： |
粉末 Keep in dark place,Sealed in dry,2-8°C 液体 -20°C:1个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 60 mg/mL(167.56 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO 无水乙醇: 2.5 mg/mL(6.98 mM)，配合低频超声，并水浴加热至45℃助溶，注意：无水乙醇开封后，易挥发，也会吸收空气中的水分，导致溶解能力下降，请避免使用开封较久的乙醇 |
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| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | Stimulator of interferon genes (STING) is an intracellular signaling molecule that senses cytosolic DNA to regulate the production of type I interferons (IFNs) and other inflammatory cytokines. C-176 is a covalent STING inhibitor that effectively decreases STING-mediated IFNβ reporter activity at the dosage of 0.01 – 1.25 μM. Treatment of [3H]-palmitate labelled HEK293T cells with 1 μM C-176 inhibited STING palmitoylation. In wild-type C57BL/6J mice, pretreatment with 750 nmol C-176 for 1h and 4h resulted in a significant reduction of STING agonist-induced IFNs and IL-6 production in serum. Two-week injection of Trex1 deficient mice with C-176 (7.5 μL/day) significantly decreased serum levels of type I IFNs and suppressed cardiac inflammatory parameters. Treatment with C-176 in Trex1-/- mice for three months attenuated systemic inflammatory signs in smooth muscle, tongue and stomach[1]. | ||
| 作用机制 | C-176 is a nitrofuran derivative that acts as a STING inhibitor by covalently binding to the Cys91 of mouse STING[1]. | ||
| 临床研究 | |||||
|---|---|---|---|---|---|
| NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
| NCT01308658 | Healthy | Phase 1 | Completed | - | Germany ... 展开 >> Berlin, Germany 收起 << |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.79mL 0.56mL 0.28mL |
13.96mL 2.79mL 1.40mL |
27.93mL 5.59mL 2.79mL |
| 参考文献 |
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