Name | C-176 |
---|---|
Synonyms |
2-Furancarboxamide, N-(4-iodophenyl)-5-nitro-
N-(4-Iodophenyl)-5-nitro-2-furamide MFCD00784208 |
Description | C-176 is a strong and covalent mouse STING inhibitor. |
---|---|
Related Catalog | |
Target |
STING[1]. |
In Vitro | C-176 strongly reduces STING-mediated, but not RIG-I- or TBK1-mediated, IFNβ reporter activity. Pretreatment with C-176 markedly reduce the CMA-mediated induction of serum levels of type I IFNs and IL-6[1]. |
In Vivo | Notably, treatment of Trex1−/− mice with C-176 resulted in a significant reduction in serum levels of type I IFNs and in a strong suppression of inflammatory parameters in the heart. Wild-type mice on a two-week treatment with C-176 show no evident signs of overt toxicity. We next conducted a three-month trial with C-176 in Trex1−/− mice, which demonstrated marked amelioration of various signs of systemic inflammation[1]. |
Animal Admin | Mice[1] C57BL/6J mice are used in the study. For the pharmacokinetic studies, wild-type mice are injected intraperitoneally with 750 nM C-176 per mouse in 200 μL corn oil. To assess the in vivo inhibitory effect of C-176, wild-type mice (8-12 weeks of age) are injected either with vehicle or C-176. To assess the in vivo inhibitory effect of H-151, wild-type mice are injected intraperitoneally with 750 nM H-151 per mouse in 200 μl 10% Tween-80 in PBS. After 1 h CMA (112 mg/kg) is administered, and after 4 h mice are euthanized and the serum is collected. The efficacy study in Trex1−/− mice is conducted as follows: mice (2-5 weeks of age) are injected with 7.5 μL of C-176 or DMSO dissolved in 85 μl corn oil twice per day for 11 consecutive days. Mice are euthanized by anaesthetization in a CO2 chamber followed by cervical dislocation[1]. |
References |
Density | 1.9±0.1 g/cm3 |
---|---|
Boiling Point | 361.2±37.0 °C at 760 mmHg |
Molecular Formula | C11H7IN2O4 |
Molecular Weight | 358.089 |
Flash Point | 172.3±26.5 °C |
Exact Mass | 357.945038 |
LogP | 3.38 |
Vapour Pressure | 0.0±0.8 mmHg at 25°C |
Index of Refraction | 1.714 |
Storage condition | 2-8℃ |