SR9011 is the agonist for REV-ERB-α with IC50 of 670 nM and REV-ERB-β with IC50 of 800 nM.
SR9011 HCl 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Melanoma cells
20µM
72 hours
SR9011 induces apoptosis in melanoma cells
Nature. 2018 Jan 18;553(7688):351-355.
Breast cancer cells
20µM
72 hours
SR9011 induces apoptosis in breast cancer cells
Nature. 2018 Jan 18;553(7688):351-355.
Acute T cell leukemia cells
20µM
72 hours
SR9011 shows significant cytotoxicity to acute T cell leukemia cells
Nature. 2018 Jan 18;553(7688):351-355.
BV2 cells
0–10μM
4 hours
SR9011 inhibited LPS-induced iNOS and COX-2 protein expression
Acta Pharmacol Sin. 2019 Jan;40(1):26-34.
SR9011 HCl 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Mice
GBM mouse model
Intraperitoneal injection
100 mg/kg
Once daily for 10 days
To evaluate the effect of SR9009 on tumor angiogenesis
Cell Rep. 2023 Feb 28;42(2):112127.
Mice
C57BL/6 mice
Intraperitoneal injection
100 mg/kg SR9011
Every 3 days for 24 hours
To study the effect of Rev-erb α activation on EPO production under hypoxic conditions, results showed that SR9011 significantly reduced DMOG-induced EPO mRNA levels
Blood Adv. 2024 Jul 23;8(14):3705-3717.
Mice
C57BL6 and Balb/c male mice
Intraperitoneal injection
100 mg/kg
Twice daily for 3 to 10 days
Evaluate the effects of SR9011 on sleep and anxiety behavior
Nat Commun. 2014 Dec 23;5:5759
Mice
C57BL6 and Balb/c mice
Intraperitoneal injection
100 mg/kg
Twice per day for 10-12 days
Evaluate the effects of SR9011 and SR9009 on circadian behavior and metabolism
Nature. 2012 Mar 29;485(7396):62-8
Mice
OVA-induced asthma model
Intraperitoneal injection
100 mg/kg
Once daily until the final challenge day (day 24)
Evaluate the alleviating effect of SR9011 on asthma severity, results showed SR9011 eased disease severity by suppressing Th2 responses
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