GLPBio

RR6

Catalog No.: GC32740Purity:>98%
COASDSData Sheet
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.

RR6
Cas No.: 1351758-37-6
10mM (in 1mL DMSO)In Stock
$135.00
1
1mgIn Stock
$42.00
1
5mgIn Stock
$125.00
1
10mgIn Stock
$186.00
1
25mgIn Stock
$305.00
1
50mgIn Stock
$416.00
1
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Description

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.

Protocol

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:
[1] 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.
[2] 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.

Chemical Properties

CAS No.
1351758-37-6
SMILES
CC(C)(CO)[C@@H](O)C(NCCC(CC1=CC=CC=C1)=O)=O
Molecular Formula
C16H23NO4
Molecular Weight
293.36
Solubility
DMSO : ≥ 100 mg/mL (340.88 mM)
Storage
Store at -20°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.

CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility

g/mol

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