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Citric acid trilithium salt tetrahydrate

Alias: 6080-58-6; Trilithium citrate tetrahydrate; LITHIUM CITRATE TETRAHYDRATE; Lithium citrate tribasic tetrahydrate; Lithonate s; Lithonate (TN); Lithium citrate [USP]; trilithium;2-hydroxypropane-1,2,3-tricarboxylate;tetrahydrate;
Cat No.:V29936 Purity: ≥98%
Lithium citrate (Litarex) tetrahydrate is the main active ingredient in Garcinia Cambogia.
Citric acid trilithium salt tetrahydrate
Citric acid trilithium salt tetrahydrate Chemical Structure CAS No.: 6080-58-6
Product category: New1
This product is for research use only, not for human use. We do not sell to patients.
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Other Forms of Citric acid trilithium salt tetrahydrate:

  • Sodium citrate dihydrate
  • Dimethyl Citric acid
  • Hydroxycitric acid
  • Citric acid-2,4-13C2 (citric acid-2,4-13C2)
  • 2-Methylcitric acid-d3 (Methylcitric acid-d3)
  • Isocitric acid
  • Citric acid
  • Hydroxycitric acid tripotassium hydrate
  • Lithium citrate (lithium citrate; Litarex)
Official Supplier of:
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Top Publications Citing lnvivochem Products
Product Description
Lithium citrate (Litarex) tetrahydrate is the main active ingredient in Garcinia Cambogia. Lithium citrate tetrahydrate can competitively inhibit citrate lyase (ATP citrate lyase) and has a weight loss effect. Lithium citrate tetrahydrate effectively inhibits stone formation and inhibits HIF, and has antioxidant, anti~inflammatory and anti-tumor effects.
Biological Activity I Assay Protocols (From Reference)
Targets
apoptosis
ln Vitro
When compared to the control group, lithium citrate tetrahydrate exhibited HIF inhibitory effects in ARPE19 and 661W cells. In ARPE19 cells and 661W cells, lithium citrate tetrahydrate can down-regulate Hif1a and its downstream genes. The treatment of CoCl2 to ARPE19 and 661W cells can lead to enhanced HIF-1α protein expression, which can be inhibited by lithium citrate tetrahydrate [2]. Lithium citrate tetrahydrate decreases lipid droplet accumulation and speeds up energy metabolism in chicken hepatocytes. Lithium citrate tetrahydrate boosts mitochondrial activity and antioxidant status to shield cells against endoplasmic reticulum stress [2].
ln Vivo
Treatment with 100–200 mg/kg of lithium citrate tetrahydrate lowers serum creatinine and blood urea nitrogen, two indicators of renal damage. When lithium citrate tetrahydrate was administered to male C57BL/6J mice, the amount of calcium oxalate crystal formation was considerably decreased. The oxidative stress brought on by calcium oxalate crystals is lessened by lithium citrate tetrahydrate. MCP-1, IL-1β, and IL-6 are examples of inflammatory cytokines that are stimulated by calcium oxalate and are inhibited by lithium citrate tetrahydrate. Furthermore, calcium oxalate crystal-induced renal tubular damage and apoptosis can be lessened by lithium citrate tetrahydrate [1]. Giving animals lithium citrate tetrahydrate can prevent them from gaining weight or accumulating fat [3].
Enzyme Assay
Lithium citrate (LC) as a common food additive and also a psychiatric drug, usually in the form of tetrahydrate can gradually lose its crystalline water and convert into LC anhydrate at temperatures higher than the room temperature. In order to quickly distinguish the tetrahydrate from the anhydrate and to study the dehydration kinetics of the LC hydrates under the influence of the temperature, terahertz time-domain spectroscopy (THz-TDS) is utilized in this work. Experimental results show that the LC tetrahydrate at room temperature has an obvious absorption peak around 1.66 THz, while the LC anhydrate has no absorption peak at 0.5-3.0 THz. The absorption peak intensity of the LC tetrahydrate decreases continuously upon heating from 25 to 100 °C. Based on the normalized absorption peak area of the LC tetrahydrate around 1.66 THz, variation of its dehydration rate with the heating temperature is investigated and their relationship is fitted by the Arrhenius equation. The reaction activation energy of the LC tetrahydrate is derived to be 495.1 ± 17.8 J/g with a deviation of about 3.7% from the traditional difference scanning calorimetry (DSC) measurement. These results indicate that THz-TDS can provide an efficient method to detect crystalline hydrates and can be applied to study the dehydration kinetics of crystalline hydrates with advantages of being fast, label-free and accurate. [1]
Salbutamol is a drug used to treat the pulmonary diseases by ameliorate the medium and large airways in the lungs. Partitioning of salbutamol drug on the aqueous two-phase systems (ATPSs) of PEG1000,1500,2000,4000,6000 + trilithium citrate + water was determined at T = 298.15 K. The effect of molecular mass of polymer (MMP) on the binodal and tie-line compositions were studied. Results showed that the biphasic area was extended as the MMP was increased. The salting-out ability were quantified using the Setschenow model, and the binodal curves were modeled by a nonlinear 3-parameter equation. Furthermore, electrolyte Wilson along with the osmotic virial models have adequately been implemented to fit the tie-line compositions. Also, the studied ATPSs were implemented to study the partitioning of salbutamol drug on the salt-affluent and polymer-affluent phases. It is observed that, ATPSs of PEG1000 is premium to extract the salbutamol to the polymer-affluent phase, where, the ATPSs of PEG6000 is more favorable to extract the drug to the salt-affluent phase. [2]
References

[1].Terahertz spectroscopy detection of lithium citrate tetrahydrate and its dehydration kinetics. Spectrochim Acta A Mol Biomol Spectrosc . 2022 Feb 5:266:120470.

[2]. Phase diagrams of PEG1000,1500,2000,4000,6000 + lithium citrate + water ATPSs, and the partitioning of salbutamol at T = 298.15 K. Sci Rep. 2023 Jan 19;13:1045.

Additional Infomation
Lithium citrate may cause developmental toxicity depending on state or federal labeling requirements. Lithium citrate tetrahydrate is the tetrahydrate form of lithium citrate. It is used as a lithium source to treat anxiety, bipolar disorder, and depression. It has antidepressant effects. It contains anhydrous lithium citrate. Lithium citrate is the citrate salt of lithium, a monovalent cation with antimanic activity. While the exact mechanism is unclear, lithium may exert its mood-stabilizing effect by reducing catecholamine concentrations, which is achieved through sodium-potassium-stimulated adenosine triphosphatase (Na-K-ATPase)-mediated transneuronal sodium ion transport. Alternatively, lithium may reduce cyclic adenosine monophosphate (cAMP) concentrations, thereby desensitizing hormone-sensitive adenylate cyclase receptors. Furthermore, lithium at recommended doses inhibits the activity of inositol-1-phosphatase, leading to decreased levels of the postsynaptic second messengers diacylglycerol and inositol triphosphate, which promote chronic cellular stimulation by altering neuronal electrical activity. See also: Lithium citrate (note moved here).
Drug Indications
Lithium is used as a mood stabilizer to treat depression and mania. It is commonly used to treat bipolar disorder.
Mechanism of Action
The exact mechanism of action of lithium ions as a mood stabilizer is not yet clear. Lithium ions may act through interactions with the transport of monovalent or divalent cations in neurons. A growing number of scientists believe that the excitatory neurotransmitter glutamate is a key factor in understanding the mechanism of lithium action. Lithium has been shown to alter the inward and outward currents of glutamate receptors, particularly GluR3, without changing their inversion potential. Studies have found that lithium has a dual effect on glutamate receptors, maintaining a stable and healthy concentration of active glutamate in the intercellular space—neither too much nor too little. Some studies speculate that too much glutamate in the interneuronal space leads to mania, while too little glutamate leads to depression. Another mechanism by which lithium regulates mood may be through the non-competitive inhibition of an enzyme called inositol monophosphatase. Furthermore, the effects of lithium may also be enhanced by inhibiting the activity of the GSK-3B enzyme. Lithium regulation of GSK-3B may affect the circadian rhythm. GSK-3 is known for phosphorylating and inactivating glycogen synthase. GSK-3B is also involved in regulating cellular responses to DNA damage. GSK-3 normally phosphorylates β-catenin, leading to β-catenin degradation. When GSK-3 is inhibited, β-catenin levels increase, and transgenic mice overexpressing β-catenin exhibit behavior similar to lithium-treated mice. These results suggest that elevated β-catenin levels may be one pathway by which lithium exerts its therapeutic effects.
Pharmacodynamics
Although lithium has been used to treat bipolar disorder for over 50 years, its mechanism of action remains unclear. The therapeutic effects of lithium may stem from a variety of effects, including inhibition of enzymes such as glycogen synthase kinase 3 and inositol phosphatase, or regulation of glutamate receptors.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C6H13LI3O11
Molecular Weight
281.9838
Exact Mass
282.093
CAS #
6080-58-6
Related CAS #
Sodium citrate dihydrate;6132-04-3;Citric acid;77-92-9;Hydroxycitric acid tripotassium hydrate;6100-05-6;Lithium citrate;919-16-4
PubChem CID
2724118
Appearance
White to off-white solid powder
Boiling Point
309.6ºC at 760 mmHg
Melting Point
112 °C
Flash Point
155.2ºC
Hydrogen Bond Donor Count
5
Hydrogen Bond Acceptor Count
11
Rotatable Bond Count
2
Heavy Atom Count
20
Complexity
211
Defined Atom Stereocenter Count
0
SMILES
[Li+].[Li+].[Li+].C(C(=O)[O-])C(CC(=O)[O-])(C(=O)[O-])O.O.O.O.O
InChi Key
HXGWMCJZLNWEBC-UHFFFAOYSA-K
InChi Code
InChI=1S/C6H8O7.3Li.4H2O/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);;;;4*1H2/q;3*+1;;;;/p-3
Chemical Name
trilithium;2-hydroxypropane-1,2,3-tricarboxylate;tetrahydrate
Synonyms
6080-58-6; Trilithium citrate tetrahydrate; LITHIUM CITRATE TETRAHYDRATE; Lithium citrate tribasic tetrahydrate; Lithonate s; Lithonate (TN); Lithium citrate [USP]; trilithium;2-hydroxypropane-1,2,3-tricarboxylate;tetrahydrate;
HS Tariff Code
2934.99.9001
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)
Solubility Data
Solubility (In Vitro)
H2O : ≥ 100 mg/mL (~354.64 mM)
Solubility (In Vivo)
Solubility in Formulation 1: 50 mg/mL (177.32 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 3.5464 mL 17.7318 mL 35.4635 mL
5 mM 0.7093 mL 3.5464 mL 7.0927 mL
10 mM 0.3546 mL 1.7732 mL 3.5464 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.

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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.
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Clinical Trial Information
Lithium versus cariprazine in the acute phase treatment of bipolar depression: a pragmatic head-to-head open, randomized multicenter study. The 9th study of the Danish University Antidepressant Group (DUAG 9).
EudraCT: 2021-006706-69
Phase: Phase 4
Status: Trial now transitioned
Date: 2022-06-22
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