RR6 是一种强效、选择性、可逆、竞争性且具有口服活性的vanin抑制剂，对重组vanin-1的IC50为540nM。
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.
RR6 是一种强效、选择性、可逆、竞争性且具有口服活性的vanin抑制剂，对重组vanin-1的IC50为540nM[1]。Vanin是一种膜结合的泛酸酶，可将泛酸硫胺水解为半胱胺，并调控氧化应激与炎症[2]。RR6常用于感染、炎症及代谢相关研究[3][4]。
体外实验显示，RR6（100µM；30min）可降低HepG2细胞内Vanin-1水平并升高总GSH含量[5]。
体内实验中，RR6（3mg/mL；饮水给予；8天）几乎完全抑制ZDF糖尿病大鼠的血浆vanin活性，但并未改变肝脏脂肪变性、胰岛素敏感性或葡萄糖生成[6]。RR6（3mg/mL；饮水给予；4周）可缩小Dark-Agouti至Brown-Norway大鼠主动脉移植模型的新生内膜面积及新生内膜/中膜比值，并抑制新生内膜巨噬细胞浸润[7]。
| 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 | ||
| 分子式 | C16H23NO4 | 分子量 | 293.36 |
| 溶解度 | DMSO : ≥ 100 mg/mL (340.88 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| 制备储备液 | |||
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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 |
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动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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