Inositol hexanicotinate, also known as inositol hexaniacinate, no-flush niacin or inositol-bound niacin, is a form of vitamin B3 (niacin) bonded to inositol. It is used for its cardiovascular and metabolic health benefits, offering an alternative to traditional niacin without causing the common side effect of flushing. Here are some of the main uses and benefits of Inositol hexaniacinate.
Cardiovascular Health Support. Inositol hexanicotinate is known to help maintain healthy cholesterol levels (1), supporting heart and circulatory system health. It helps improve blood circulation, potentially benefiting conditions such as intermittent claudication (leg pain caused by exercise due to poor circulation).
Reduced Risk of Flushing. Unlike traditional niacin, this form offers the benefits of vitamin B3 while significantly reducing the risk of flushing and hot flashes (2), due to the slow dissociation of inositol from niacin in the body.
Antioxidant Effects. Inositol hexanicotinate may have antioxidant effects (3), protecting cells from damage caused by free radicals.
Blood Sugar Levels Management. It has been suggested that it can help in managing blood sugar levels, supporting people with or at risk of diabetes.
Dietary Supplements. Often used in dietary supplements for those seeking the benefits of niacin without the side effects of flushing, especially for metabolic and cardiovascular support.
Inositol hexanicotinate combines the benefits of niacin with improved tolerability, making it a popular choice for cardiovascular and metabolic health support without the common side effects of niacin.
It appears in the form of a white powder
Chemical Industrial Synthesis Process
- Synthesis of Inositol and Nicotinic Acid. The production begins with the chemical synthesis of inositol and nicotinic acid (niacin) as precursors. These compounds are prepared and purified to ensure their reactivity in the subsequent esterification reaction.
- Esterification Reaction. Inositol and nicotinic acid are then combined in an esterification reaction. During this process, six molecules of nicotinic acid are esterified with one molecule of inositol, forming inositol hexaniacinate. The reaction requires specific catalysts and controlled reaction conditions to achieve high yield.
- Purification. The crude inositol hexaniacinate product is purified to remove impurities and by-products of the reaction. This may include techniques such as crystallization, vacuum distillation, and chromatography.
- Quality Control. The purified product undergoes quality control checks to verify its purity, chemical composition, and absence of impurities. These tests can include spectroscopic analyses, chromatographic analyses, and purity tests.
- Formulation. The purified inositol hexaniacinate can be formulated into various forms for use in dietary supplements, such as capsules, tablets, or powders.
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Molecular Formula C42H30N6O12
Molecular Weight 810.7 g/mol
CAS 6556-11-2
UNII A99MK953KZ
EC Number 229-485-9
Synonyms
Inositol nicotinate
Inositol niacinate
References_____________________________________________________________________
(1) Jariwalla, R. J. (1999). Inositol hexaphosphate (IP6) as an anti-neoplastic and lipid-lowering agent. Anticancer research, 19(5A), 3699-3702.
Abstract. IP6, a major dietary source of inositol phosphates, is a physiological antioxidant with potential to form complexes with cations linked to cell proliferation and hypercholesterolemia. Accordingly, we have examined the action of IP6 on dietary modulation of neoplasia and hyperlipidemia in a Fischer rat model (1, 2). Two studies were conducted on the effects of naturally-derived IP6, administered as purified phytate, a salt form of phytic acid (inositol hexaphosphoric acid). One study examined the effect on the growth of tumors promoted in syngeneic rats transplanted with a viral oncogene-transformed cell line. Increases in tumor incidence and growth rate of fibrosarcomas seen following administration of a special diet (containing 5% saturated fatty acids and 1.2% magnesium oxide) were completely mitigated by supplementation of the same diet with purified potassium-magnesium phytate (8.9% phytic acid by weight). The other study examined the IP6 effect on serum lipid and mineral levels in animals fed a cholesterol-enriched or standard diet. Elevated levels of serum total cholesterol, triglycerides and zinc/copper ratio associated with administration of the cholesterol-enriched diet were significantly lowered by supplementation of this diet with monopotassium phytate. Addition of monopotassium phytate to the standard diet also reduced serum lipid levels but did not significantly affect the zinc/copper ratio. These studies support a role for IP6 as a potential therapeutic agent in the treatment of cancer and hyperlipidemia.
(2) Aguilar, F., Charrondiere, U. R., Dusemund, B., Galtier, P., Gilbert, J., Gott, D. M., ... & Woutersen, R. A. (2008). Inositol hexanicotinate (inositol hexaniacinate) as a source of niacin (vitamin B3) added for nutritional purposes in food supplements. EFSA JOURNAL, 949, 1-20.
Abstract. No genotoxicity data are available on inositol hexanicotinate. However, as inositol hexanicotinate is hydrolysed to inositol and nicotinic acid, which are endogenous compounds and occur in several dietary products as well, the Panel concluded that the absence of genotoxicity data does not raise any concern. The petitioners indicate that inositol hexanicotinate acts as a slow-release supply of nicotinic acid and that therefore, the flushing effect is not likely to occur when inositol hexanicotinate is used as a source of niacin since the nicotinic acid molecules slowly hydrolyse from the inositol. The Panel notes that given the slow release of nicotinic acid from inositol hexanicotinate, the flushing effect, on the basis of which both the SCF and EVM have given Tolerable Upper Intake Levels for nicotinic acid, may be conservative for inositol hexanicotinate. However, given the absence of studies adequately supporting the absence of a flushing effect when dosing inositol hexanicotinate, the Panel concludes that the upper limit for nicotinic acid of 10 mg/day should also be used to judge the safety of inositol hexanicotinate. A daily dose of 10 mg nicotinic acid given as inositol hexanicotinate would amount to a daily dose of 11 mg inositol hexanicotinate, resulting in release of 2.4 mg inositol upon hydrolysis. Given the estimated normal dietary intake of inositol that amounts to 335-1500 mg myo-inositol (the most important form of naturally occurring inositol)/day, the Panel concludes that the intake of 2.4 mg inositol/day, resulting from intake of inositol hexanicotinate at a level that corresponds to a daily dose of 10 mg nicotinic acid, would not be of safety concern. The Panel concludes that the use of inositol hexanicotinate as a source for niacin, when added for nutritional purposes in food supplements intended for the general population, would be of no safety concern provided that use levels are in compliance with the defined upper safe use level for nicotinic acid (10 mg/day). However, the Panel is concerned that the use levels of inositol hexanicotinate proposed by the petitioners are 40 and 495 mg/day providing 36.4 and 450 mg nicotinic acid/day. These proposed use levels provide levels of nicotinic acid that are 4 to 45 times higher than the Tolerable Upper Intake Level of 10 mg nicotinic acid/day defined by the SCF in 2002.
(3) Foster, S. R., Dilworth, L. L., Thompson, R. K., Alexander-Lindo, R. L., & Omoruyi, F. O. (2017). Effects of combined inositol hexakisphosphate and inositol supplement on antioxidant activity and metabolic enzymes in the liver of streptozotocin-induced type 2 diabetic rats. Chemico-Biological Interactions, 275, 108-115.
Abstract. Diabetes mellitus is associated with elevated reactive oxygen species, lipid abnormalities, reduced antioxidant activity and organ damage. This study examines the effects of combined inositol hexakisphosphate (IP6) and inositol supplement on antioxidant levels and other biochemical parameters in the liver of type 2 diabetic rats. Five groups of Sprague-Dawley rats were studied. Six rats were fed normal diet (non-diabetic control), while 24 rats were fed high-fat diet (HFD) for 4 weeks. Diabetes was induced in 18 of the rats fed HFD by intraperitoneal administration of streptozotocin. The diabetic rats were separated into three groups namely: combined IP6 and inositol, glibenclamide and diabetic control. The non-diabetic group fed high-fat diet was classified as a high-fat control group. For the final four weeks of the experiment, all rats were fed normal diet and given their respective treatment regimes. Hepatic antioxidant status, metabolic enzyme activity, lipid profile, peroxidative damage and liver histology, as well as, serum aminotransferase and alkaline phosphatase activities, and total bilirubin concentration were assessed. Treatment with combined IP6 and inositol supplement significantly increased liver reduced glutathione and high-density lipoprotein levels while liver triglyceride levels and serum alkaline phosphatase activity were significantly reduced by 27%, 50%, 38.5%, and 69.2% respectively compared to the diabetic control. Hepatic superoxide dismutase, catalase, glucose-6-phosphate dehydrogenase activities were significantly upregulated by 55%, 26% and 53% respectively in the diabetic rats treated with combined IP6 and inositol compared to the diabetic control. Combined IP6 and inositol treatment resulted in the preservation of liver cell integrity and improved antioxidant status in type 2 diabetic rats.
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Molecular Formula C42H30N6O12
Molecular Weight 810.7 g/mol
CAS 6556-11-2
UNII A99MK953KZ
EC Number 229-485-9
Synonyms
Inositol nicotinate
Inositol niacinate
References_____________________________________________________________________
(1) Jariwalla, R. J. (1999). Inositol hexaphosphate (IP6) as an anti-neoplastic and lipid-lowering agent. Anticancer research, 19(5A), 3699-3702.
Abstract. IP6, a major dietary source of inositol phosphates, is a physiological antioxidant with potential to form complexes with cations linked to cell proliferation and hypercholesterolemia. Accordingly, we have examined the action of IP6 on dietary modulation of neoplasia and hyperlipidemia in a Fischer rat model (1, 2). Two studies were conducted on the effects of naturally-derived IP6, administered as purified phytate, a salt form of phytic acid (inositol hexaphosphoric acid). One study examined the effect on the growth of tumors promoted in syngeneic rats transplanted with a viral oncogene-transformed cell line. Increases in tumor incidence and growth rate of fibrosarcomas seen following administration of a special diet (containing 5% saturated fatty acids and 1.2% magnesium oxide) were completely mitigated by supplementation of the same diet with purified potassium-magnesium phytate (8.9% phytic acid by weight). The other study examined the IP6 effect on serum lipid and mineral levels in animals fed a cholesterol-enriched or standard diet. Elevated levels of serum total cholesterol, triglycerides and zinc/copper ratio associated with administration of the cholesterol-enriched diet were significantly lowered by supplementation of this diet with monopotassium phytate. Addition of monopotassium phytate to the standard diet also reduced serum lipid levels but did not significantly affect the zinc/copper ratio. These studies support a role for IP6 as a potential therapeutic agent in the treatment of cancer and hyperlipidemia.
(2) Aguilar, F., Charrondiere, U. R., Dusemund, B., Galtier, P., Gilbert, J., Gott, D. M., ... & Woutersen, R. A. (2008). Inositol hexanicotinate (inositol hexaniacinate) as a source of niacin (vitamin B3) added for nutritional purposes in food supplements. EFSA JOURNAL, 949, 1-20.
Abstract. No genotoxicity data are available on inositol hexanicotinate. However, as inositol hexanicotinate is hydrolysed to inositol and nicotinic acid, which are endogenous compounds and occur in several dietary products as well, the Panel concluded that the absence of genotoxicity data does not raise any concern. The petitioners indicate that inositol hexanicotinate acts as a slow-release supply of nicotinic acid and that therefore, the flushing effect is not likely to occur when inositol hexanicotinate is used as a source of niacin since the nicotinic acid molecules slowly hydrolyse from the inositol. The Panel notes that given the slow release of nicotinic acid from inositol hexanicotinate, the flushing effect, on the basis of which both the SCF and EVM have given Tolerable Upper Intake Levels for nicotinic acid, may be conservative for inositol hexanicotinate. However, given the absence of studies adequately supporting the absence of a flushing effect when dosing inositol hexanicotinate, the Panel concludes that the upper limit for nicotinic acid of 10 mg/day should also be used to judge the safety of inositol hexanicotinate. A daily dose of 10 mg nicotinic acid given as inositol hexanicotinate would amount to a daily dose of 11 mg inositol hexanicotinate, resulting in release of 2.4 mg inositol upon hydrolysis. Given the estimated normal dietary intake of inositol that amounts to 335-1500 mg myo-inositol (the most important form of naturally occurring inositol)/day, the Panel concludes that the intake of 2.4 mg inositol/day, resulting from intake of inositol hexanicotinate at a level that corresponds to a daily dose of 10 mg nicotinic acid, would not be of safety concern. The Panel concludes that the use of inositol hexanicotinate as a source for niacin, when added for nutritional purposes in food supplements intended for the general population, would be of no safety concern provided that use levels are in compliance with the defined upper safe use level for nicotinic acid (10 mg/day). However, the Panel is concerned that the use levels of inositol hexanicotinate proposed by the petitioners are 40 and 495 mg/day providing 36.4 and 450 mg nicotinic acid/day. These proposed use levels provide levels of nicotinic acid that are 4 to 45 times higher than the Tolerable Upper Intake Level of 10 mg nicotinic acid/day defined by the SCF in 2002.
(3) Foster, S. R., Dilworth, L. L., Thompson, R. K., Alexander-Lindo, R. L., & Omoruyi, F. O. (2017). Effects of combined inositol hexakisphosphate and inositol supplement on antioxidant activity and metabolic enzymes in the liver of streptozotocin-induced type 2 diabetic rats. Chemico-Biological Interactions, 275, 108-115.
Abstract. Diabetes mellitus is associated with elevated reactive oxygen species, lipid abnormalities, reduced antioxidant activity and organ damage. This study examines the effects of combined inositol hexakisphosphate (IP6) and inositol supplement on antioxidant levels and other biochemical parameters in the liver of type 2 diabetic rats. Five groups of Sprague-Dawley rats were studied. Six rats were fed normal diet (non-diabetic control), while 24 rats were fed high-fat diet (HFD) for 4 weeks. Diabetes was induced in 18 of the rats fed HFD by intraperitoneal administration of streptozotocin. The diabetic rats were separated into three groups namely: combined IP6 and inositol, glibenclamide and diabetic control. The non-diabetic group fed high-fat diet was classified as a high-fat control group. For the final four weeks of the experiment, all rats were fed normal diet and given their respective treatment regimes. Hepatic antioxidant status, metabolic enzyme activity, lipid profile, peroxidative damage and liver histology, as well as, serum aminotransferase and alkaline phosphatase activities, and total bilirubin concentration were assessed. Treatment with combined IP6 and inositol supplement significantly increased liver reduced glutathione and high-density lipoprotein levels while liver triglyceride levels and serum alkaline phosphatase activity were significantly reduced by 27%, 50%, 38.5%, and 69.2% respectively compared to the diabetic control. Hepatic superoxide dismutase, catalase, glucose-6-phosphate dehydrogenase activities were significantly upregulated by 55%, 26% and 53% respectively in the diabetic rats treated with combined IP6 and inositol compared to the diabetic control. Combined IP6 and inositol treatment resulted in the preservation of liver cell integrity and improved antioxidant status in type 2 diabetic rats.
Inositol hexanicotinate 
