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| Other Sizes |
| Targets |
Hydroxycitric acid tripotassium hydrate targets ATP citrate lyase (ACL), a key enzyme in the de novo lipogenesis pathway that converts citrate to acetyl-CoA and oxaloacetate. By competitively inhibiting ACL, the compound reduces the availability of acetyl-CoA for fatty acid and cholesterol synthesis. This mechanism underlies its potential effects on weight management and metabolic regulation. The compound also inhibits hypoxia-inducible factor (HIF), a transcription factor involved in cellular responses to hypoxia, and has antioxidant and anti-inflammatory activities. These multiple targets contribute to its diverse biological effects, including antitumor activity.
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| ln Vitro |
Citrate exhibited inhibitory effects on HIF in ARPE19 cells and 661W cells when compared to pyramids. comparable to citric acid, which in 661W and ARPE19 cells can inhibit downstream genes including Hif1a. Citric acid has the ability to suppress HIF in ARPE19 and 661W cells. HIF-1α protein expression is increased by inhibiting CoCl2 [2]. Citric acid speeds up energy activation and decreases lipid droplet accumulation in chicken liver cells. Otherwise, citric acid boosts mitochondrial performance and antioxidant status to shield cells against apoptotic ER stress [2].
Hydroxycitric acid tripotassium hydrate exhibits a range of in vitro biological activities. It competitively inhibits ATP citrate lyase, reducing fatty acid synthesis in vitro. The compound also inhibits stone formation in crystallization assays and inhibits HIF activity. It has been shown to possess antioxidant properties, likely through its ability to chelate metal ions or scavenge free radicals. Anti-inflammatory activity has been demonstrated in cell-based assays measuring cytokine production or inflammatory marker expression. Antitumor activity has been observed in cancer cell lines, where the compound inhibits cell proliferation and induces apoptosis. These in vitro activities confirm the compound’s potential as a multi-target therapeutic agent. |
| ln Vivo |
Treatment with 100–200 mg/kg of citric acid decreased serum muscle nutrition and blood urea nitrogen, two indicators of renal failure. First, citric acid inhibits inflammatory cytokines including MCP-1, IL-1β, and IL-6 that are generated by calcium oxalate. This is demonstrated by the crystal deposits of calcium oxalate in electrodes treated with citric acid (C57BL/6J electrode). It can lessen the harm that calcium oxalate crystals bring to renal tubules and cell necrosis [1].
In vivo studies with hydroxycitric acid tripotassium hydrate have been conducted in animal models of obesity, metabolic syndrome, and cancer. As a Garcinia Cambogia extract component, it has been studied for its effects on weight loss and fat metabolism. By inhibiting ATP citrate lyase, the compound reduces fatty acid synthesis and may promote fat oxidation. In animal models, it has shown efficacy in reducing body weight, lowering serum lipid levels, and improving insulin sensitivity. Its anti-inflammatory and antioxidant activities have been demonstrated in models of inflammation and oxidative stress. Antitumor activity has been observed in xenograft models, where the compound inhibits tumor growth. |
| Enzyme Assay |
In vitro enzyme assays for hydroxycitric acid tripotassium hydrate typically measure its inhibition of ATP citrate lyase activity. The enzyme is incubated with citrate, CoA, and ATP in the presence of varying concentrations of the compound. The production of acetyl-CoA and oxaloacetate is measured spectrophotometrically or by coupled enzymatic assays. The competitive nature of inhibition is confirmed by kinetic analysis. HIF inhibition assays involve measuring HIF-1α protein levels or HIF transcriptional activity using reporter gene assays in hypoxic conditions. Antioxidant activity is assessed using standard assays such as DPPH radical scavenging or FRAP.
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| Cell Assay |
In vitro cellular assays for hydroxycitric acid tripotassium hydrate are conducted in various cell lines, including cancer cells, adipocytes, and hepatocytes. Cells are treated with the compound at various concentrations, and cell proliferation is measured using MTT or CellTiter-Glo assays. Fatty acid synthesis is measured by incorporating radiolabeled acetate or glucose into lipids. HIF activity is assessed using luciferase reporter assays under hypoxic conditions or by measuring HIF-1α protein levels via Western blot. Inflammatory markers (e.g., TNF-α, IL-6) are measured by ELISA or qPCR. Apoptosis is assessed using Annexin V staining or caspase activity assays.
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| Animal Protocol |
In vivo animal experiments with hydroxycitric acid tripotassium hydrate are typically conducted in rodent models. Obesity and metabolic syndrome models include high-fat diet-fed mice or genetically obese rodents. The compound is administered orally via gavage or mixed with food. Body weight, food intake, and serum lipid profiles are monitored. Glucose tolerance tests and insulin sensitivity tests are performed. In cancer models, tumor xenografts are established in immunodeficient mice, and the compound is administered orally or intraperitoneally. Tumor volume is measured over time, and tumor tissues are harvested for histology and biomarker analysis. Inflammation models (e.g., carrageenan-induced paw edema) are used to assess anti-inflammatory activity.
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| ADME/Pharmacokinetics |
Pharmacokinetic parameters such as absorption and bioavailability are assessed by measuring compound levels in plasma and tissues. Hydroxycitric acid tripotassium hydrate is water-soluble (100 mg/mL) and is typically administered orally. Its bioavailability is influenced by its potassium salt form and the presence of food. The compound is metabolized in the liver and excreted in the urine. Storage at 4°C is recommended for stability. Further detailed PK studies are needed to fully characterize its absorption, distribution, metabolism, and excretion profile. The compound’s water solubility facilitates formulation for in vivo studies.
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| Toxicity/Toxicokinetics |
Toxicological data for hydroxycitric acid tripotassium hydrate have been evaluated in the context of its use as a dietary supplement ingredient. Garcinia Cambogia extracts containing hydroxycitric acid have been generally recognized as safe (GRAS) at recommended doses. However, high doses may cause gastrointestinal discomfort, including nausea and diarrhea. Liver toxicity has been reported in rare cases with commercial supplements, though causality is not well-established. In preclinical studies, the compound has been administered at various doses without significant toxicity reported. Standard toxicological evaluations, including acute and chronic toxicity studies, have been conducted for Garcinia Cambogia extracts. The compound should be used within recommended guidelines.
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| References |
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| Additional Infomation |
Potassium citrate monohydrate is the monohydrate form of potassium citrate and has a diuretic effect. It contains anhydrous potassium citrate. This product is a water-soluble powder, taken orally, and used as a diuretic, expectorant, systemic alkalizing agent, and electrolyte supplement. See also: Potassium citrate (note moved to).
Hydroxycitric acid tripotassium hydrate is the potassium salt of hydroxycitric acid, the main active ingredient of Garcinia Cambogia. It is used in research for its effects on lipid metabolism, weight management, and as a dietary supplement ingredient. The compound is also known as potassium citrate monohydrate. Its mechanism involves competitive inhibition of ATP citrate lyase, reducing fatty acid and cholesterol synthesis. It also inhibits stone formation and HIF, and exhibits antioxidant, anti-inflammatory, and antitumor activities. The compound is soluble in water and is stored at 4°C. It is available in high purity (≥98%) for research applications. |
| Molecular Formula |
C6H7K3O8
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|---|---|
| Molecular Weight |
324.4099
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| Exact Mass |
323.905
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| CAS # |
6100-05-6
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| Related CAS # |
Lithium citrate tetrahydrate;6080-58-6;Sodium citrate dihydrate;6132-04-3;Citric acid;77-92-9;Hydroxycitric acid;6205-14-7
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| PubChem CID |
2735208
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| Appearance |
White to off-white solid powder
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| Density |
1.98
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| Boiling Point |
309.6ºC at 760 mmHg
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| Melting Point |
275 °C (dec.)(lit.)
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| Flash Point |
155.2ºC
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
17
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| Complexity |
211
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
PJAHUDTUZRZBKM-UHFFFAOYSA-K
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| InChi Code |
InChI=1S/C6H8O7.3K.H2O/c7-3(8)1-6(13,5(11)12)2-4(9)10;;;;/h13H,1-2H2,(H,7,8)(H,9,10)(H,11,12);;;;1H2/q;3*+1;/p-3
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| Chemical Name |
tripotassium;2-hydroxypropane-1,2,3-tricarboxylate;hydrate
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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) |
H2O : ~120 mg/mL (~369.90 mM)
DMSO :< 1 mg/mL |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 100 mg/mL (308.25 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.0825 mL | 15.4126 mL | 30.8252 mL | |
| 5 mM | 0.6165 mL | 3.0825 mL | 6.1650 mL | |
| 10 mM | 0.3083 mL | 1.5413 mL | 3.0825 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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