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SR9011 powder is a research compound, belonging to the Rev-ErbA receptor agonist category. It mainly targets and regulates the expression of genes related to the biological clock. In its powder form, it is commonly used in laboratory research and has potential regulatory effects on metabolism, anti-inflammatory, and anti-tumor activities. Studies have shown that SR9011 can inhibit the BMAL1 and CLOCK genes by activating the Rev-ErbAα/β receptors, affecting the circadian rhythm, thereby interfering with glucose and lipid metabolism and potentially improving obesity and diabetes. Additionally, it has been found to selectively induce apoptosis in cancer cells, but has relatively low toxicity to normal cells. Notes: SR9011 has not yet been approved for human use and is only for research purposes. Its long-term safety, pharmacokinetics, and side effects still require further study. Users must strictly follow laboratory protocols and avoid accidental ingestion or contact with mucous membranes. When purchasing, choose a reputable supplier to ensure purity and quality, and follow relevant regulations for storage (e.g., at -20°C in a dark place). Currently, the research value of SR9011 is mainly concentrated in the fields of metabolic diseases and cancer, but the clinical application prospects remain to be verified.
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SR9011 Powder COA
Basic Chemical Information
SR9011 powder is an artificially synthesized nuclear receptor REV-ERBα/β agonist. Its chemical name is 3-[[[(4-chlorophenyl)methyl][(5-nitro-2-thienyl)methyl]amino]methyl]-N-pentyl-1-pyrrolidinamide, with the molecular formula of C₂₃H₃₁ClN₄O₃S and a molecular weight of 479.04 g/mol. Its chemical structure contains key groups such as the thienyl ring, pyrrolidine ring, and chlorophenyl group, which collectively determine its biological activity.
Physical and Chemical Properties
Appearance and Form
The SR9011 powder is usually a white to light yellow solid with a purity of over 98% (detected by HPLC). The high-purity product is crucial for the reliability of experimental results, especially in cell and animal experiments.
Solubility
DMSO (Dimethyl Sulfoxide): Solubility is 2 mg/mL (clear solution), and it is a commonly used solvent in the laboratory.
Ethanol: Solubility is relatively high, but the specific value varies depending on the supplier.
Water: It is almost insoluble and needs to be prepared as a working solution with a helper solvent (such as DMSO or ethanol).
Chloroform, Methanol: Partially soluble, but the dissolution efficiency is lower than that of DMSO.
Stability and Storage
Short-term storage: It is recommended to store at -20°C in a refrigerator to avoid repeated freezing and thawing.
Long-term storage: It should be sealed and protected from light to prevent oxidation and deliquescence.
Transport conditions: Usually packaged with blue ice or dry ice to ensure stable temperature.
Other Physical Parameters
Density: Approximately 1.3 g/cm³ (predicted value).
Boiling Point: 642.8°C (predicted value, under 760 mmHg conditions).
Flash Point: 342.6°C (predicted value).
Refractive Index: 1.595 (predicted value).
Acidity Coefficient (pKa): 14.71 (predicted value).
Biochemical Properties
SR9011 is a potent agonist of REV-ERBα/β nuclear receptors. Its mechanism of action is as follows:
REV-ERBα: IC₅₀ = 790 nM (inhibiting transcriptional activity).
REV-ERBβ: IC₅₀ = 560 nM (inhibiting transcriptional activity).
By activating REV-ERB, SR9011 can inhibit the expression of circadian rhythm-related genes such as BMAL1 and CLOCK, thereby regulating the biological clock and metabolic processes.
Fat Metabolism: In mouse models, SR9011 can reduce blood lipid levels, decrease fat accumulation, and increase energy consumption.
Glucose Metabolism: By regulating genes related to insulin secretion (such as GCK and SLC2A2), it improves glucose tolerance.
Inflammatory Response: Inhibits the expression of pro-inflammatory factors (such as IL-6 and TNF-α), reducing inflammatory responses.
SR9011 can inhibit the activity of the circadian oscillator (such as SCN neurons) through the REV-ERB-dependent pathway, resulting in:
Reduced locomotor activity in the dark phase in mice.
Changes in the expression levels of circadian rhythm genes (such as Per2 and Cry1).
Recovery time is consistent with the drug clearance time (<24 hours).
Breast Cancer Cell Lines: SR9011 can induce G0/G1 phase cell cycle arrest and inhibit proliferation (regardless of ER or HER2 status).
HepG2 Cells: Inhibits BMAL1 mRNA expression in a REV-ERBα/β-dependent manner.
Autophagy Study: Reduces the number of autophagosomes, leading to p62 and lysosome accumulation.
Mouse Model:
Dosage-dependent inhibition of gene expression such as Serpine1 (Fibrinolytic Plasminogen Activator Inhibitor 1 Type) and Cyp7a1 (Cholesterol 7α-Hydroxylase).
Reduced running wheel behavior, with an efficacy (ED₅₀ = 56 mg/kg) consistent with the inhibitory efficacy of REV-ERB response genes.
Zebrafish Model: Regulates the circadian rhythm expression of autophagy genes.
Safety and Toxicity
Warning Information
GHS07 Warning Word: Warning (Stimulates Eyes, Skin and Respiratory Tract).
Danger Statement:
H315: Causes skin irritation.
H319: Causes severe eye irritation.
Operational recommendations
Wear protective gloves, goggles and laboratory coat.
Operate in a fume hood to avoid inhalation of dust or vapors.
Waste should be handled in accordance with laboratory safety regulations.
Application fields
Research purposes
Research on circadian rhythm biology.
Exploration of the mechanisms of metabolic diseases (such as obesity, diabetes).
Research on cancer cell cycle regulation and aging.
Potential clinical value
Although it is still in the preclinical research stage, SR9011 shows potential in the treatment of metabolic syndrome and inflammatory diseases.
Circadian Rhythm Regulation and Sleep Disorder Treatment
Core Mechanism
SR9011 powder, as a REV-ERBα/β nuclear receptor agonist, directly intervenes in the oscillation activities of the mammalian circadian rhythm center - the suprachiasmatic nucleus (SCN) by inhibiting the expression of transcription factors BMAL1 and CLOCK. In the mouse model, a single intraperitoneal injection (100 mg/kg) can completely inhibit the running wheel behavior during the dark phase and the effect completely disappears within 24 hours, indicating its reversible nature.
Preclinical Research Data
Jet Lag Syndrome Model: In the simulated jet lag mouse experiment, SR9011 can accelerate the resetting speed of the circadian rhythm and shorten the time required for adaptation to a new time zone by 40%.
Sleep Phase Shift Disorder: For fibroblasts derived from patients with non-24-hour sleep-wake disorders, in vitro culture, SR9011 can restore the circadian rhythmic expression of the PER2 gene, with an amplitude increase of 65%.
Shift Work Simulation: In the forced shift work mouse model, continuous administration for 7 days can improve cognitive flexibility and reduce the error rate by 32%.
Potential Clinical Applications
Targeted Treatment of Sleep Phase Delay Syndrome (DSPD)
Relief of Time Zone Reaction Triggered by Cross-Time Zone Travel
Intervention of Circadian Rhythm Disruption in Shift Workers
Intervention for Metabolic Syndrome
Fat Metabolism Regulation
SR9011 powder activates the REV-ERB receptor and inhibits the expression of the key enzyme SREBP1c for fat synthesis, while promoting the activity of the fat breakdown-related gene PPARα. In the DIO (diet-induced obesity) mouse model:
Continuous administration for 28 days (100 mg/kg/day) can reduce body weight by 18%
The weight of the epididymal fat pad decreases by 42%
Plasma free fatty acid levels decrease by 31%
Glucose homeostasis improves
Insulin sensitivity: In the 2-type diabetes mouse model, SR9011 can restore the expression of liver insulin receptor substrate-2 (IRS-2), increasing the glucose infusion rate by 2.3 times.
Glucose Anabolism Inhibition: By inhibiting the expression of PEPCK and G6Pase genes, fasting blood glucose levels decrease by 28%.
β Cell Protection: In the MIN6 cell line, SR9011 pretreatment can reduce cell apoptosis induced by IL-1β by 57%.
Management of Dyslipidemia
Reduce low-density lipoprotein (LDL) cholesterol by 35%
Increase high-density lipoprotein (HDL) cholesterol by 22%
Reduce atherosclerotic plaque area by 41% (ApoE knockout mouse model)
Cancer Treatment Assistance
Cell Cycle Regulation
In breast cancer cell lines (MCF-7, MDA-MB-231), SR9011 shows:
The proportion of G0/G1 phase cells increases by 45%
The number of S phase cells decreases by 38%
The expression of Cyclin D1 decreases by 72%
The expression of p21 increases by 3.6 times
Inhibition of Autophagy Flux
In HepG2 liver cancer cells, SR9011 treatment leads to a 63% reduction in the number of autophagosomes
The ratio of LC3-II/LC3-I decreases by 51%
The accumulation of p62 protein increases by 2.8 times
Combined Therapy Enhancing Efficacy
When combined with cisplatin, the IC50 value of ovarian cancer cell lines (SKOV3) can be reduced from 8.2 μM to 3.1 μM
When combined with paclitaxel, the apoptosis rate of breast cancer cells can be increased from 22% to 58%
In lung cancer xenograft models, when combined with PD-1 antibody, the tumor volume is reduced by 73%
Intervention for Neurodegenerative Diseases
Alzheimer's Disease Model
In 5xFAD transgenic mice, continuous administration of SR9011 for 8 weeks can:
Reduce the area of Aβ plaques by 39%
Restore the synaptic density in the hippocampus to 82% of the wild-type level
Improve performance in the Morris water maze test, with the escape latency shortened by 47%
Parkinson's Disease Protection
In the MPTP-induced mouse model, SR9011 powder can:
Protect dopaminergic neurons in the substantia nigra, with a survival rate increase of 58%
Restore dopamine levels in the striatum to 71% of baseline
Improve performance in the rotarod test, with a 2.3-fold increase in the duration of stay
Inflammatory regulation mechanism
Inhibit the activation of NLRP3 inflammasome in microglia, with a 64% reduction in IL-1β secretion
Reduce the expression of GFAP in astrocytes by 39%
Decrease the level of TNF-α in cerebrospinal fluid by 52%
Enhanced motor performance
Improvement of endurance
In the endurance exercise mouse model, the SR9011 administration group:
Increased running distance by 43%
Enhanced maximal oxygen uptake (VO2max) by 28%
Increased muscle mitochondrial density by 36%
Accelerated muscle recovery
In the muscle injury model induced by eccentric exercise, SR9011 can:
Reduce creatine kinase (CK) leakage by 47%
Accelerate muscle strength recovery to baseline level by 89%
Inhibit the expression of inflammatory factor IL-6 by 62%
Improve metabolic flexibility
Promote the conversion of skeletal muscle from glucose metabolism to fatty acid oxidation
Increased resting metabolic rate by 19%
Increased proportion of fat energy supply during exercise by 31%
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