RR6 |
Catalog No.GC32740
One-Click Copy Product Info
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RR6 is a potent, selective, reversible, competitive and orally active vanin inhibitor with an IC50 of 540nM for recombinant vanin-1.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1351758-37-6
Sample solution is provided at 25 µL, 10mM.
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RR6 is a potent, selective, reversible, competitive and orally active vanin inhibitor with an IC50 of 540nM for recombinant vanin-1[1]. Vanin is a membrane-bound pantetheinase that hydrolyzes pantetheine to cysteamine and regulates oxidative stress and inflammation[2]. RR6 is usually used in the studies of infection, inflammation and metabolism[3][4].
In vitro, RR6 (100µM; 30min) lowered intracellular Vanin-1 level and raised total GSH level in HepG2 cells[5].
In vivo, RR6 (3mg/mL; drinking water; 8 days) almost completely suppressed plasma vanin activity but did not alter hepatic steatosis, insulin sensitivity or glucose production in ZDF diabetic rats[6]. RR6 (3mg/mL; drinking water; 4 weeks) reduced neointima area and neointima/media ratio, and suppressed neointimal macrophage influx in Dark-Agouti-to-Brown-Norway rat aortic allografts[7].
References:
[1] Jansen PA, van Diepen JA, Ritzen B, et al. Discovery of small molecule vanin inhibitors: new tools to study metabolism and disease. ACS Chem Biol. 2013;8(3):530-534.
[2] Bartucci R, Salvati A, Olinga P, Boersma YL. Vanin 1: Its Physiological Function and Role in Diseases. Int J Mol Sci. 2019;20(16):3891.
[3] Schalkwijk J, Jansen P. Chemical biology tools to study pantetheinases of the vanin family. Biochem Soc Trans. 2014;42(4):1052-1055.
[4] Lv L, Wang T, Xie W, et al. Revealing VNN1: An Emerging and Promising Target for Inflammation and Redox Balance. Immun Inflamm Dis. 2025;13(10):e70274.
[5] Lu P, Zhang C, Fu L, et al. Near-Infrared Fluorescent Probe for Imaging and Evaluating the Role of Vanin-1 in Chemotherapy. Anal Chem. 2021;93(29):10378-10387.
[6] van Diepen JA, Jansen PA, Ballak DB, et al. Genetic and pharmacological inhibition of vanin-1 activity in animal models of type 2 diabetes. Sci Rep. 2016;6:21906.
[7] Wedel J, Jansen PA, Botman PN, Rutjes FP, Schalkwijk J, Hillebrands JL. Pharmacological Inhibition of Vanin Activity Attenuates Transplant Vasculopathy in Rat Aortic Allografts. Transplantation. 2016;100(8):1656-1666.
| Cell experiment [1]: | |
Cell lines | HepG2 cells |
Preparation Method | HepG2 cells were cultured in complete Dulbecco’s Modified Eagle Medium (DMEM) supplemented with 4.5g/L glucose, 2mM L-glutamine, 1mM sodium pyruvate, 100U/mL penicillin-streptomycin, and 10% (v/v) fetal bovine serum (FBS) at 37°C in a humidified 5% CO₂ atmosphere. Cells were seed in a six-well plate. After the confluence rate was approximately 70%, 2μg of plasmid DNA (human Vanin-1 gene, cDNA clone expressing plasmid with the OFPSpark tag) and 2.5μL of lipofectamine 2000 were added to the serum-free medium. After 6h of culture, the culture medium was replaced with a complete medium for another 24h. Then cells were treated with or without 100μM RR6 for 30min. After treatments, all of the experimental cells were incubated with Cy-Pa at 37°C for 30min, and imaging was performed by laser scanning confocal microscopy. |
Reaction Conditions | 100µM; 30 min |
Applications | RR6 lowered intracellular Vanin-1 level and raised total GSH level in HepG2 cells. |
| Animal experiment [2]: | |
Animal models | Male Zucker Diabetic Fatty rats |
Preparation Method | Male Zucker Diabetic Fatty (ZDF) rats of 8 weeks old were housed in a temperature (23±1℃) and humidity (50%) controlled animal facility with 12:12h light-dark cycle. Food and water were available ad libitum. Rats were treated with the pantetheinase (vanin) inhibitor RR6 (3mg/mL; dissolved in drinking water) or vehicle for 8 days. Rats were sacrificed at the end of the RR6 treatment (non-fasted; between 9 am and 11am) and blood and organs were collected for further analysis. Each test was repeated three times, and the data was averaged. |
Dosage form | 3mg/mL; drinking water; 8 days |
Applications | RR6 almost completely suppressed plasma vanin activity but did not alter hepatic steatosis, insulin sensitivity or glucose production in ZDF diabetic rats. |
References: | |
| Cas No. | 1351758-37-6 | SDF | |
| Canonical SMILES | CC(C)(CO)[C@@H](O)C(NCCC(CC1=CC=CC=C1)=O)=O | ||
| Formula | C16H23NO4 | M.Wt | 293.36 |
| Solubility | DMSO : ≥ 100 mg/mL (340.88 mM) | 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 | 3.4088 mL | 17.0439 mL | 34.0878 mL |
| 5 mM | 681.8 μL | 3.4088 mL | 6.8176 mL |
| 10 mM | 340.9 μL | 1.7044 mL | 3.4088 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
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.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 37 reference(s) in Google Scholar.)