产品
编 号：F756091
分子式：C21H25BF2N2O4
分子量：418.24
分子式：C21H25BF2N2O4
分子量：418.24
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
询价
询价
5mg
询价
询价
10mg
询价
询价
结构图
CAS No: 2806031-94-5
产品详情
生物活性：
NIC-0102 is an orally active proteasome inhibitor (pIC50=7.55) that specifically inhibits NLRP3 inflammatory vesicle activation. NIC-0102 shows potent anti-inflammatory effects in a model of dextran sulfate sodium (DSS)-induced ulcerative colitis. NIC-0102 also inhibits production of pro-IL-1β.
体内研究：
NIC-0102 (0.125, 0.25, 0.5 mg/kg; p.o.; single every 72 h for 10 days) shows strong protection against DSS-induced acute colitis in mice.Animal Model:Male C57BL/6 mice (6 to 8-week-old; DSS-induced ulcerative colitis model).
Dosage:0.125, 0.25, and 0.5 mg/kg
Administration:Oral gavage; single every 72 h for 10 days.
Result:Significantly suppressed weight and fecal occult blood. Decreased colonic length in a dose-dependent manner.Resulted in a dose-dependent reduction in tissue-associated IL-1β concentration and significantly inhibited pro-IL-1β.
Animal Model:Male C57BL/6 mice (6 to 8-week-old).
Dosage:0.5 mg/kg (for i.v.); 1 mg/kg (for p.o.)
Administration:Intravenous injection; Oral gavage; single.
Result:1.19Pharmacokinetic Parameters of NIC-0102 in male C57BL/6 mice.IV (0.5 mg/kg) PO (1 mg/kg)
T1/2 (h)4.738.36
Tmax (h)0.080.25
Cmax (ng/mL)376.6207.7
AUC0-∞ (h?ng/mL)448.8489.2
MRT0-∞ (h)6.14-
Vz (L/kg)7.7-
CL (mL/min/kg)18.8-
F (%)-48.1%
体外研究：
NIC-0102 (compound 27) (7.5, 15, 30, 60 nM; 1h) specifically suppresses NLRP3 inflammasome activation in LPS-primed J774A.1 and BMDM cells.NIC-0102 (7.5, 15, 30, 60 nM; 1h) induces polyubiquitination of NLRP3 via inhibition of the proteasome during the activation step in LPS-primed J774A.1 cells.NIC-0102 (7.5, 15, 30, 60 nM; 1h) exhibits inhibitory effects on NF-κB in the priming step of the NLRP3 pathway in LPS-primed J774A.1 cells.NIC-0102 (15, 60 nM; 1h) blocks NLRP3-ASC interaction and ASC oligomerization in LPS-primed J774A.1 cells.
NIC-0102 is an orally active proteasome inhibitor (pIC50=7.55) that specifically inhibits NLRP3 inflammatory vesicle activation. NIC-0102 shows potent anti-inflammatory effects in a model of dextran sulfate sodium (DSS)-induced ulcerative colitis. NIC-0102 also inhibits production of pro-IL-1β.
体内研究：
NIC-0102 (0.125, 0.25, 0.5 mg/kg; p.o.; single every 72 h for 10 days) shows strong protection against DSS-induced acute colitis in mice.Animal Model:Male C57BL/6 mice (6 to 8-week-old; DSS-induced ulcerative colitis model).
Dosage:0.125, 0.25, and 0.5 mg/kg
Administration:Oral gavage; single every 72 h for 10 days.
Result:Significantly suppressed weight and fecal occult blood. Decreased colonic length in a dose-dependent manner.Resulted in a dose-dependent reduction in tissue-associated IL-1β concentration and significantly inhibited pro-IL-1β.
Animal Model:Male C57BL/6 mice (6 to 8-week-old).
Dosage:0.5 mg/kg (for i.v.); 1 mg/kg (for p.o.)
Administration:Intravenous injection; Oral gavage; single.
Result:1.19Pharmacokinetic Parameters of NIC-0102 in male C57BL/6 mice.IV (0.5 mg/kg) PO (1 mg/kg)
T1/2 (h)4.738.36
Tmax (h)0.080.25
Cmax (ng/mL)376.6207.7
AUC0-∞ (h?ng/mL)448.8489.2
MRT0-∞ (h)6.14-
Vz (L/kg)7.7-
CL (mL/min/kg)18.8-
F (%)-48.1%
体外研究：
NIC-0102 (compound 27) (7.5, 15, 30, 60 nM; 1h) specifically suppresses NLRP3 inflammasome activation in LPS-primed J774A.1 and BMDM cells.NIC-0102 (7.5, 15, 30, 60 nM; 1h) induces polyubiquitination of NLRP3 via inhibition of the proteasome during the activation step in LPS-primed J774A.1 cells.NIC-0102 (7.5, 15, 30, 60 nM; 1h) exhibits inhibitory effects on NF-κB in the priming step of the NLRP3 pathway in LPS-primed J774A.1 cells.NIC-0102 (15, 60 nM; 1h) blocks NLRP3-ASC interaction and ASC oligomerization in LPS-primed J774A.1 cells.
产品资料
Copyright©2015-2024 沪ICP备2022026524号-1
沪公网安备