SR9011 (hydrochloride)
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- CAS号:
- 2070014-94-5
- 英文名:
- SR9011 (hydrochloride)
- 英文别名:
- SR9011 (hydrochloride)
- 中文名:
- SR9011 (hydrochloride)
- 中文别名:
- REV-ERBΑ/Β激动剂(SR9011 HYDROCHLORIDE);3-((4-氯苄基)(5-硝基噻吩-2-基)甲基)氨基)甲基)-N-戊基吡咯烷-1-甲酰胺盐酸盐
- CBNumber:
- CB63122349
- 分子式:
- C??H??Cl?N?O?S
- 分子量:
- 0
- MOL File:
- Mol file
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SR9011 (hydrochloride)化学性质
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形态:
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Solid
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颜色:
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Light yellow to brown
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SR9011 (hydrochloride)性质、用途与生产工艺
SR9011 hydrochloride 是一种 REV-ERBα/β 激动剂,作用于 REV-ERBα 和 REV-ERBβ,IC50s 分别为 790 nM 和 560 nM。
IC50: 790 nM (Rev-ErbBα), 560 nM (Rev-ErbBβ)
SR9011 dose-dependently increases the REV-ERB-dependent repressor activity assessed in HEK293 cells expressing a chimeric Gal4 DNA Binding Domain (DBD) - REV-ERB ligand binding domain (LBD) α or β and a Gal4-responsive luciferase reporter (REV-ERBα IC
50
=790 nM, REV-ERBβ IC
50
=560 nM). SR9011 potently and efficaciously suppresses transcription in a cotransfection assay using full-length REV-ERBα along with a luciferase reporter driven by the
Bmal1
promoter (SR9011 IC
50
=620 nM). SR9011 suppresses the expression ofBMAL1 mRNA in HepG2 cells in a
REV-ERBα/β
-dependent manner SR9011 suppresses proliferation of the breast cancer cell lines regardless of their ER or HER2 status. SR9011 appears to pause the cell cycle of the breast cancer cells prior to M phase. Cyclin A (
CCNA2
) is identified as a direct target gene of REV-ERB suggesting that suppression of expression of this cyclin by SR9011 may mediate the cell cycle arrest. Treatment with SR9011 results in an increase in cells in the G
0
/G
1
phase and a decrease of cells in S and G
2
/M phase suggesting that activation of REV-ERB may be resulting in decreased transition from G
1
to S phase and/or from S to G
2
/M phase.
SR9011 displays reasonable plasma exposure, thus, the expression of REV-ERB responsive genes is examined in the liver of mice treated with various doses of SR9011 for 6-days. The
plasminogen activator inhibitor type 1
gene (
Serpine1
) is a REV-ERB target gene and displays dose-dependent suppression of expression in response to SR9011. The
cholesterol 7α-hydroxylase
(
Cyp7a1
) and
sterol response element binding protein
(
Srepf1
) genes have also been shown to be responsive to REV-ERB and are dose-dependently suppressed with increasing amounts of SR9011. After 12 days in D:D conditions mice are injected with a single dose of SR9011 or vehicle at CT6 (peak expression of
Rev-erbα
). Vehicle injection causes no disruption in circadian locomotor activity. However, administration of a single dose of SR9011 results in loss of locomotor activity during the subject dark phase. Normal activity returns the next circadian cycle, consistent with clearance of the drugs in less than 24h. The SR9011-dependent decrease in wheel running behavior in the mice under constant darkness conditions is dose-dependent and that the potency (ED
50
=56 mg/kg) is similar to the potency of SR9011-mediated suppression of a REV-ERB responsive gene,
Srebf1
, in vivo (ED
50
=67mg/kg).
SR9011 (hydrochloride)
上下游产品信息
上游原料
下游产品
更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
---|
2024/04/30 | HY-16988A | SR9011 (hydrochloride) SR9011 hydrochloride | 2070014-94-5 | 2mg | 900元 |
2024/04/30 | HY-16988A | SR9011 (hydrochloride) SR9011 hydrochloride | 2070014-94-5 | 5mg | 1600元 |
SR9011 (hydrochloride)
生产厂家
2070014-94-5, SR9011 (hydrochloride) 相关搜索:
- 细胞生物学试剂
- 3-((4-氯苄基)(5-硝基噻吩-2-基)甲基)氨基)甲基)-N-戊基吡咯烷-1-甲酰胺盐酸盐
- REV-ERBΑ/Β激动剂(SR9011 HYDROCHLORIDE)
- 2070014-94-5
- SR9011 (hydrochloride)