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编 号:F137014
分子式:C25H31N5O4
分子量:465.54
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10mM*1mL in DMSO
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1mg
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5mg
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10mg
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25mg
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50mg
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100mg
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生物活性:
BRD5529 is an effective dose-dependent CARD9-TRIM62 protein–protein interaction (PPI) inhibitor with an IC50 value of 8.6 μM. BRD5529 has potency and complete inhibition of CARD9 ubiquitinylation in vitro, also has favorable solubility. BRD5529 can be used for the research of inflammatory bowel disease (IBD) such as Crohn’s disease (CD) and ulcerative colitis (UC).

体内研究:
BRD5529 (i.p.; 0.1 or 1.0 mg/kg; daily, for 2 weeks) displays no inherent safety concerns in initial general safety and toxicology assessments.Animal Model:Pneumocystis pneumonia (PCP) model
Dosage:0.1 or 1.0 mg/kg
Administration:intraperitoneally (IP), daily, for 2 weeks
Result:Resulted no significant changes in daily or final weight gain and proinflammatory cytokines showed no major differences.Showed no significant change of lung, liver, and kidney in pathology scoring.

体外研究:
BRD5529 has effective dose-dependent CARD9-TRIM62 inhibitory activity with an IC50 value of 8.6 μM.BRD5529 directly binds CARD9, but not TRIM62, and disrupt its ubiquitinylation in vitro.BRD5529 (40 μM) produces dose-dependent inhibition of TRIM62-mediated CARD9 ubiquitinylation in vitro.BRD5529 (200 μM, 0-50 min; 200μM, 2-4 h) inhibits CARD9-dependent signaling in innate immune cells.
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