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Purity: ≥98%
SR-18292 (SR18292) is a novel and potent inhibitor of PGC-1α (PPAR gamma coactivator-1α), which is able to reduce blood glucose, strongly increase hepatic insulin sensitivity, and improve glucose homeostasis in dietary and genetic mouse models of T2D. SR-18292 can increase PGC-1α acetylation, suppress gluconeogenic gene expression, and reduce glucose production in hepatocytes.
| ln Vitro |
PGC-1α, a transcriptional coactivator, co-activates transcription factors that control glucose and fat metabolism, which is essential for maintaining energy homeostasis. PGC-1α's association with the acetyl transferase GCN5 is enhanced by SR-18292, whilst PGC-1α's co-activation of the nuclear hormone receptor HNF4α is decreased. The gluconeogenic transcriptional function of HNF4α/PGC-1α is suppressed by SR-18292. SR-18292 enhances the interaction between GCN5 and PGC-1α, leading to the acetylation of particular lysine residues in PGC-1α. This process may potentially reduce the gluconeogenic activity of PGC-1α.
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| ln Vivo |
In diabetic mice, SR-18292 lowers fasting blood glucose, boosts hepatic insulin sensitivity, and enhances glucose homeostasis. A dietary model of obesity and type 2 diabetes (T2D) using mice on a high-fat diet (HFD) are administered SR-18292 (45 mg/kg) by IP injection for three days in a row, and then again on the fourth day, prior to the measurement of fasting blood glucose. Surprisingly, SR-18292-treated animals exhibit noticeably lower fasting blood glucose concentrations than control mice given the same vehicle. One regulating aspect of the body's reaction to fasting is the activation of gluconeogenic gene expression. Importantly, livers removed from mice given SR-18292 treatment exhibit decreased gluconeogenic gene expression, particularly that of Pck1[1].
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| References |
[1]. Sharabi K, et al. Selective Chemical Inhibition of PGC-1α Gluconeogenic Activity Ameliorates Type 2 Diabetes. Cell. 2017 Mar 23;169(1):148-160.e15
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| Molecular Formula |
C23H30N2O2
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| Molecular Weight |
366.496506214142
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| CAS # |
2095432-55-4
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| SMILES |
CC(C=C1)=CC=C1CN(C(C)(C)C)CC(O)COC2=CC=CC3=C2C=CN3
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| InChi Key |
BNRANURXPKRRKP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H30N2O2/c1-17-8-10-18(11-9-17)14-25(23(2,3)4)15-19(26)16-27-22-7-5-6-21-20(22)12-13-24-21/h5-13,19,24,26H,14-16H2,1-4H3
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| Chemical Name |
1-((1H-indol-4-yl)oxy)-3-(tert-butyl(4-methylbenzyl)amino)propan-2-ol
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| Synonyms |
SR18292 SR-18292 SR 18292
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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) |
Ethanol : ~100 mg/mL (~272.85 mM)
DMSO : ≥ 100 mg/mL (~272.85 mM) H2O : < 0.1 mg/mL |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.82 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.82 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.82 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7285 mL | 13.6426 mL | 27.2851 mL | |
| 5 mM | 0.5457 mL | 2.7285 mL | 5.4570 mL | |
| 10 mM | 0.2729 mL | 1.3643 mL | 2.7285 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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