SR9009 (Synonyms: REV-ERB Agonist II) |
| Catalog No.GC12035 |
SR9009 is a synthetic REV-ERB agonist used for treatment with metabolic diseases such as obesity, bipolar, anxiety and depressive disorders.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1379686-30-2
Sample solution is provided at 25 µL, 10mM.
SR9009 is a synthetic REV-ERB agonist used for treatment with metabolic diseases such as obesity, bipolar, anxiety and depressive disorders.[1]
In vitro experiment it demonstrated that treatment with 10µM of SR9009 induced obvious apoptosis in SCLC cells.[1] In vitro, treatment with 0 µM, 2.5 µM, 5 µM, or 10 µM of SR9009 cardiomyocytes showed no difference in hypoxia-induced cell death versus vehicle-treated controls. SR9009 treatment also did not significantly rescue cardiomyocyte cell death under any conditions.[2] Treatment with 10 μM of SR9009 for 2 days reduced the viability of wild-type mESCs in a dose-dependent manner. And SR9009 also had strong metabolic effects on mESC mitochondria, decreasing both their stimulated and basal.[3] SR9009 had a cytotoxic effect on tumor cells from brain, leukemia, breast, colon and melanoma at the 20 µM concentrations.[5]
In vivo, LPS-induced sepsis mice were treated with 50 mg/kg SR9009, the pathological lesions such as hemorrhage and edema in the lung tissue and the infiltration of inflammatory cells was obviously decreased.[4] In vivo efficacy study it shown that treatment with 100 mg/kg of SR9009 orally reduced weight gain as well as less severe hyperlipidemia and hepatic steatosis as compared to the control group. However, SR9009 gavage had no effect on the expression of lipogenic genes in the liver, TAG synthesis genes in the WAT, and genes involved in fatty acid oxidation in the skeletal muscle. [6]
References:
[1]. Shen W, et al. SR9009 induces a REV-ERB dependent anti-small-cell lung cancer effect through inhibition of autophagy. Theranostics. 2020 Mar 15;10(10):4466-4480.
[2]. Reitz CJ, et al. SR9009 administered for one day after myocardial ischemia-reperfusion prevents heart failure in mice by targeting the cardiac inflammasome. Commun Biol. 2019 Oct 3;2:353.
[3]. Dierickx P, et al. SR9009 has REV-ERB-independent effects on cell proliferation and metabolism. Proc Natl Acad Sci U S A. 2019 Jun 18;116(25):12147-12152.
[4]. Griffin P, et al. Circadian clock protein Rev-erbα regulates neuroinflammation. Proc Natl Acad Sci U S A. 2019 Mar 12;116(11):5102-5107.
[5]. Sulli G, et al. Pharmacological activation of REV-ERBs is lethal in cancer and oncogene-induced senescence. Nature. 2018 Jan 18;553(7688):351-355.
[6]. Yu F, et al. Deficiency of intestinal Bmal1 prevents obesity induced by high-fat feeding. Nat Commun. 2021 Sep 7;12(1):5323.
| Cell experiment [1]: | |
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Cell lines |
HepG2 cells |
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Preparation Method |
5 × 103 HepG2 cells were allowed to attach overnight at 37°C in a 96-well plate. Cultured cells were incubated with DMSO (vehicle) or REV-ERB agonist (SR9009) at different concentrations (5, 10, 20, and 40 µM) for 96 h. Then, cell viability was analyzed by MTT assay considering vehicle-treated cells (DMSO) as 100% of viability. |
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Reaction Conditions |
5, 10, 20, and 40 µM; 96 h |
|
Applications |
SR9009 significant effects on cell morphology and reduction in cell viability were observed at final concentrations of 20 and 40 µM for 48 and 72 h. |
| Animal experiment [2]: | |
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Animal models |
BALB/c nude mice |
|
Preparation Method |
SCLC cells were harvested and suspended in culture medium, and 1 × 107 cells were subcutaneously injected to establish the SCLC xenograft model. When tumors reached an average size of 100 mm3, mice were randomly divided into four groups. Then, SR9009 (50 mg/kg) was administered intraperitoneally once every two days. Mice were intraperitoneally injected with physiological saline containing chemotherapeutics or physiological saline alone as a control. |
|
Dosage form |
50 mg/kg; i.p. |
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Applications |
SR9009 treatment led to marked tumor growth inhibition in both the chemosensitive and chemoresistant tumor models. |
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References: [1]. Wagner PM, et al. Chemotherapeutic Effect of SR9009, a REV-ERB Agonist, on the Human Glioblastoma T98G Cells. ASN Neuro. 2019 Jan-Dec;11:1759091419892713. [2]. Shen W, et al. SR9009 induces a REV-ERB dependent anti-small-cell lung cancer effect through inhibition of autophagy. Theranostics. 2020 Mar 15;10(10):4466-4480. |
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| Cas No. | 1379686-30-2 | SDF | |
| Synonyms | REV-ERB Agonist II | ||
| Chemical Name | ethyl 3-(((4-chlorobenzyl)((5-nitrothiophen-2-yl)methyl)amino)methyl)pyrrolidine-1-carboxylate | ||
| Canonical SMILES | CCOC(N1CCC(C1)CN(CC(S2)=CC=C2[N+]([O-])=O)CC3=CC=C(Cl)C=C3)=O | ||
| Formula | C20H24ClN3O4S | M.Wt | 437.94 |
| Solubility | ≥ 43.8mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.2834 mL | 11.4171 mL | 22.8342 mL |
| 5 mM | 0.4567 mL | 2.2834 mL | 4.5668 mL |
| 10 mM | 0.2283 mL | 1.1417 mL | 2.2834 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 36 reference(s) in Google Scholar.)
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