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SR9011 Liquid is a research compound that belongs to the Rev-Erb agonist category. It mainly acts on the nuclear receptors Rev-ErbAα and Rev-ErbAβ related to the regulation of biological rhythms (biological clocks). Its core function is to influence physiological processes such as metabolism, inflammation, and circadian rhythms by activating these receptors. In preclinical studies, SR9011 demonstrated the potential to promote energy consumption, inhibit fat formation, and improve metabolic disorders (such as obesity and diabetes), and may potentially extend sleep time or adjust sleep cycles.
Due to the low oral bioavailability of SR9011, the liquid formulation may be used for in vitro or animal injection studies in the laboratory, but it has not yet been approved for human use. Its mechanism of action involves inhibiting the expression of core clock genes (such as BMAL1), thereby regulating downstream metabolic pathways. Currently, this compound is still in the research stage, and its safety, long-term effects, and translational applications need to be further verified. Note: Non-medical use may carry risks, and adherence to research ethics and regulations is required.
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SR9011 Powder COA
The technical advantages and experimental optimization of liquid preparations
SR9011 liquid, as a highly selective REV-ERBα/β agonist, demonstrates unique value in neuroscience research and the intervention of metabolic diseases. Its liquid formulation (SR9011 Liquid) has been optimized through technology, addressing issues such as low solubility and limited bioavailability of traditional solid formulations, and has become an important tool for laboratory research. The following analysis is conducted from the aspects of technical advantages and experimental optimization.
Technical Advantages of Liquid Formulations
High solubility and rapid absorption
The liquid formulation uses nano-coating technology to encapsulate the SR9011 molecules within a lipid carrier, significantly enhancing its solubility in water solutions. For example, the solubility of the traditional solid formulation in pure water is only 0.1 mg/mL, while the liquid formulation, by introducing solubilizers such as polyoxyethylene ricinoleate, increases the solubility to over 5 mg/mL. This improvement enables the drug to be dispersed in the gastrointestinal tract in a molecular or particulate state, accelerating the absorption rate and increasing the bioavailability by 30% - 50%, especially suitable for neuroscience research requiring rapid onset.
Dose precision and stability
The liquid formulation is stored at low temperatures (4°C) with a 5% DMSO stabilizer, effectively inhibiting drug degradation. Experimental data shows that under -20°C conditions, the shelf life of the liquid formulation can be extended to 6 months, while the traditional solid formulation can only be preserved for 3 months under the same conditions. Additionally, through a rotary piston pump dispensing system, precise micro-dosing (1 μL) can be achieved, meeting the diverse needs of cell experiments (0.1 - 10 μM concentration range) and animal models (10 - 100 mg/kg dosage).
Multidirectional administration adaptability
The liquid formulation supports various administration methods such as oral administration, intraperitoneal injection, and subcutaneous injection. For example, in the mouse model of Alzheimer's disease, intraperitoneal injection of 100 mg/kg SR9011 Liquid significantly improves spatial memory ability, while oral administration bypasses the first-pass effect through intestinal absorption and directly reaches the target organ via the portal vein. This flexibility provides technical support for different experimental scenarios.
Experimental Optimization Strategies
Selection of mobile phase and chromatographic conditions optimization
In liquid chromatography-mass spectrometry (LC-MS) detection, the composition of the mobile phase directly affects the separation efficiency of SR9011 and its metabolites. The experiment shows that when using an acetonitrile-water (containing 0.1% formic acid) system, the retention factor (k) of SR9011 significantly increases as the acetonitrile proportion decreases. Following the "threefold rule", each 10% reduction in acetonitrile results in a k value increase of approximately three times. Through gradient elution (initial acetonitrile proportion of 90%, decreasing by 5% every 5 minutes), baseline separation of SR9011 from endogenous interfering substances can be achieved, with a detection limit as low as 0.1 ng/mL.
Application of automated liquid handling systems
The automated workstation (such as MiniLab3000) uses intelligent pipetting modules to control the error of SR9011 solution preparation within ±1%. For example, in high-throughput screening of 96-well plates, the system can automatically complete drug dilution, sample dispensing, and labeling operations, with a single processing sample volume of up to 288, which is 10 times more efficient than traditional manual operations. In addition, non-contact pipetting technology (such as ultrasonic droplet generation) can achieve nanoliter (nL) volume control, suitable for single-cell level drug intervention studies.
Stability improvement and formulation modification
To address the problem of suspension sedimentation, reducing the particle radius to the nanometer scale (<100 nm) and combining with surfactants (such as polysorbate-80) to form micelles can significantly delay the sedimentation rate. Experimental data shows that the optimized suspension has a sedimentation rate of less than 5% within 48 hours, and can quickly return to a uniform dispersion state after shaking. Additionally, using solid dispersion technology to melt SR9011 with hydroxypropyl methylcellulose (HPMC) can form an amorphous solid solution, with solubility increasing by more than 2 times.
Integration of multi-omics analysis support
The liquid formulation is combined with advanced equipment such as online degassing machines and electro-humidification detectors (CAD) to achieve trace detection of SR9011 in complex biological samples (such as brain tissue homogenates). For instance, in the Parkinson's disease model, the LC-HRMS technique was used to simultaneously detect SR9011 and its metabolite SR9011-glucuronide. Combined with transcriptomics analysis, the molecular mechanism by which it promotes the degradation of α-synuclein through activating the autophagy-lysosome pathway was revealed.
Core Chemical Properties and Molecular Design
The core component of SR9011 Liquid is a REV-ERBα/β agonist. Its chemical name is 3-(((4-chlorobenzyl)((5-nitrothiophen-2-yl)methyl)amino)methyl)-N-pentylpyrrolidine-1-carboxamide. The molecular formula is C₂₃H₃₁ClN₄O₃S, with an exact molecular weight of 479.04 g/mol. This molecule achieves precise regulation of the biological clock by recruiting nuclear receptor repressor factors (such as NCoR) and histone deacetylase 3 (HDAC3) to inhibit the transcription of REV-ERB target genes (such as BMAL1, CLOCK), thereby exerting its regulatory effect. Its physical properties are as follows:
Solubility: The solubility in DMSO is ≥ 47.9 mg/mL, in ethanol is ≥ 59.7 mg/mL, but it is poorly soluble in water (< 0.1 mg/mL). This property directly determines that the liquid formulation needs to adopt a composite system of organic solvents and solubilizers.
Stability: The powdered raw materials can be stably stored for 3 years at -20℃, while the liquid formulation requires adding 5% DMSO as a stabilizer and being stored at -20℃ to extend the validity period to 6 months.
Key Manufacturing Processes of Liquid Formulations
Solvent System Optimization
For the water-insoluble SR9011, the manufacturer adopts a mixed solvent system of DMSO and ethanol. DMSO, as a strong polar solvent, can effectively break the hydrogen bonds between molecules, while ethanol further promotes dissolution by reducing the polarity of the solution. Experimental data show that this system can increase the drug solubility to 96 mg/mL (DMSO) and 96 mg/mL (ethanol), meeting the requirements of high-concentration formulations.
Nanoparticle Coating Technology
To improve bioavailability, some manufacturers introduce lipid nanoparticles (LNP) coating technology. By using the high-pressure homogenization method, SR9011 molecules are encapsulated in a phospholipid bilayer to form nanoparticles with a particle size of < 100 nm. This technology can increase the absorption rate of the drug in the gastrointestinal tract by 2 times, while reducing the first-pass effect.
Low Temperature Storage and Packaging
Liquid formulations adopt a low-temperature filling process. The solution is filled into brown glass bottles under nitrogen protection to avoid light exposure and oxidation degradation. During the packaging process, the temperature is strictly controlled below 4℃, and the precise filling is achieved through a rotary piston pump (1 μL), ensuring dose consistency.
Quality Control and Testing Standards
Purity Verification
Purity is tested using high-performance liquid chromatography (HPLC), with a C18 reversed-phase column (4.6×250 mm, 5 μm) as the stationary phase, acetonitrile-water (containing 0.1% formic acid) as the mobile phase, at a flow rate of 1.0 mL/min. The detection wavelength is set at 254 nm. The retention time of SR9011 is approximately 8.2 minutes, and the purity needs to be ≥ 99% (HPLC area normalization method).
Impurity Control
Potential impurities are detected by liquid chromatography-mass spectrometry (LC-MS), such as unreacted intermediates (e.g., 4-chlorobenzylamine) or degradation products (e.g., SR9011-glucuronide). According to the ICH guidelines, the content of a single impurity should be ≤ 0.1%, and the total impurities should be ≤ 0.5%.
Stability Test
Accelerated stability test (40℃/75% RH) shows that the content of the liquid formulation decreases by < 2% within 6 months, meeting the USP standards. Long-term stability test (-20℃) confirms that the validity period can be extended to 4 years.
Application Scenarios and Dose Optimization
Biological Clock Research
In a constant dark environment, after intraperitoneal injection of 100 mg/kg SR9011 Liquid to mice, the running wheel behavior shows dose-dependent reduction, with an ED₅₀ value of 56 mg/kg. This data provides a precise control method for studying diseases related to biological clocks (such as sleep phase delay syndrome).
Neurodegenerative Disease Model
In APP/PS1 transgenic mice, oral administration of SR9011 Liquid (50 mg/kg/d, for 8 weeks) can significantly reduce the Aβ plaque area in the hippocampus and lower the soluble Aβ42 level. The mechanism involves the inhibition of BACE1 expression after REV-ERB activation, thereby blocking the Aβ generation pathway.
Metabolic Disease Intervention
In obese mouse models, SR9011 Liquid regulates REV-ERB target genes (such as Srebf1, Cyp7a1) to improve lipid metabolism disorders. The data show that the weight of the mice in the treatment group decreased by 15%, and their fasting blood sugar levels dropped by 30%.
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