| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 100mg | |||
| Other Sizes |
| Targets |
SR-10067 targets Rev-Erbα and Rev-Erbβ, which are nuclear receptors involved in the regulation of the circadian rhythm and metabolism. It is a potent and selective agonist, with IC₅₀ values of 170 nM for Rev-Erbα and 160 nM for Rev-Erbβ.
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| ln Vitro |
SR10067 exhibits a high affinity for Rev-Erbβ and Rev-Erbα, as evidenced by its respective IC50 values of 160 and 170 nM [1].
In vitro, SR-10067 exhibits high affinity for Rev-Erbβ and Rev-Erbα. Its activity is characterized in cell-based reporter assays, where it activates transcription from Rev-Erb response elements. |
| ln Vivo |
In mice, SR10067 (ip injection; 30 mg/kg) exhibits favorable pharmacokinetic characteristics [1].
In vivo, SR-10067 (30 mg/kg, intraperitoneal injection) in mice exhibits favorable pharmacokinetic characteristics. A single injection inhibits the circadian rhythm of Npas2 gene expression in the mouse hypothalamus, reduces nighttime wheel running activity in a dose-dependent manner, induces wakefulness, reduces slow-wave sleep (SWS) and REM sleep, and exhibits high anxiolytic activity. |
| Enzyme Assay |
In vitro receptor binding assays measure the compound's affinity for Rev-Erbα and Rev-Erbβ. These assays typically involve competition binding with a radiolabeled ligand, and the IC₅₀ is determined.
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| Cell Assay |
In vitro cell-based assays use reporter gene systems to measure the transcriptional activity of Rev-Erb. Cells are transfected with a reporter construct containing a Rev-Erb response element and treated with the compound, and reporter activity is measured.
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| Animal Protocol |
Animal/Disease Models: Mice [1]
Doses: 30 mg/kg Route of Administration: intraperitoneal (ip) injection Experimental Results: The IC50 value of the receptor in plasma and brain concentrations remained above. A single injection inhibited the circadian rhythm of Npas2 gene expression in the mouse hypothalamus and had a dose-dependent effect on reducing nighttime wheel running activity. Induces wakefulness and reduces SWS and REM sleep, and exhibits high anxiolytic activity. In vivo animal studies are conducted in mice. The compound is administered intraperitoneally at 30 mg/kg. Endpoints include analysis of circadian gene expression, measurement of locomotor activity, assessment of sleep patterns, and evaluation of anxiolytic effects. |
| ADME/Pharmacokinetics |
Pharmacokinetic (PK) properties of SR-10067 indicate it is brain-penetrant and has favorable characteristics in mice. Following intraperitoneal injection at 30 mg/kg, the plasma and brain concentrations remain above the IC₅₀.
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| Toxicity/Toxicokinetics |
The toxicity profile of SR-10067 has not been detailed in the provided search results. The compound is for research use only. It is supplied as a white to off-white solid powder with a purity of ≥98%.
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| References |
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| Additional Infomation |
SR-10067 is also known as SR10067. It is a brain-penetrant compound and can be used for research of metabolic diseases and neuropsychiatric disorders.
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| Molecular Formula |
C31H31NO3
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|---|---|
| Molecular Weight |
465.582748651505
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| Exact Mass |
465.23
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| CAS # |
1380548-02-6
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| PubChem CID |
60168097
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| Appearance |
White to off-white solid powder
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| LogP |
6.8
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
35
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| Complexity |
694
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C(N1C(COC2=CC=C(OC(C)(C)C)C=C2)CC2=C(C1)C=CC=C2)(C1=C2C(C=CC=C2)=CC=C1)=O
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| InChi Key |
MOPAGKWBFUICQT-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C31H31NO3/c1-31(2,3)35-27-17-15-26(16-18-27)34-21-25-19-23-10-4-5-11-24(23)20-32(25)30(33)29-14-8-12-22-9-6-7-13-28(22)29/h4-18,25H,19-21H2,1-3H3
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| Chemical Name |
[3-[[4-[(2-methylpropan-2-yl)oxy]phenoxy]methyl]-3,4-dihydro-1H-isoquinolin-2-yl]-naphthalen-1-ylmethanone
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~214.79 mM)
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1479 mL | 10.7393 mL | 21.4786 mL | |
| 5 mM | 0.4296 mL | 2.1479 mL | 4.2957 mL | |
| 10 mM | 0.2148 mL | 1.0739 mL | 2.1479 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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