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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
  • 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 can cause developmental toxicity according to state or federal government labeling requirements.
Lithium citrate tetrahydrate is a hydrate that is the tetrahydrate form of lithium citrate. It is used as a source of lithium for the treatment of anxiety disorders, bipolar disorder, and depression. It has a role as an antidepressant. It contains a lithium citrate (anhydrous).
Lithium Citrate is the citrate salt of lithium, a monovalent cation with antimanic activity. Although the exact mechanism is unclear, lithium might exert its mood-stabilizing effect via reduction of catecholamine concentration mediated through transneuronal membrane transport of sodium ion by sodium-potassium-stimulated adenosine triphosphatase (Na-K-ATPase). Alternatively, lithium may decrease cyclic adenosine monophosphate (cAMP) concentrations, which would desensitize hormonal-sensitive adenylyl cyclase receptors. Furthermore, lithium, in recommended dosage, blocks the activity of inositol-1-phosphatase, thereby resulting in the subsequent decrease of postsynaptic second messengers, diacylglycerol and inositol triphosphate, that contribute to chronic cell stimulation by altering electrical activity in the neuron.
See also: Lithium Citrate (annotation moved to).
Drug Indication
Lithium is used as a mood stabilizer, and is used for treatment of depression and mania. It is often used in bipolar disorder treatment.
Mechanism of Action
The precise mechanism of action of Li+ as a mood-stabilizing agent is currently unknown. It is possible that Li+ produces its effects by interacting with the transport of monovalent or divalent cations in neurons. An increasing number of scientists have come to the conclusion that the excitatory neurotransmitter glutamate is the key factor in understanding how lithium works. Lithium has been shown to change the inward and outward currents of glutamate receptors (especially GluR3), without a shift in reversal potential. Lithium has been found to exert a dual effect on glutamate receptors, acting to keep the amount of glutamate active between cells at a stable, healthy level, neither too much nor too little. It is postulated that too much glutamate in the space between neurons causes mania, and too little, depression. Another mechanism by which lithium might help to regulate mood include the non-competitive inhibition of an enzyme called inositol monophosphatase. Alternately lithium's action may be enhanced through the deactivation of the GSK-3B enzyme. The regulation of GSK-3B by lithium may affect the circadian clock. GSK-3 is known for phosphorylating and thus inactivating glycogen synthase. GSK-3B has also been implicated in the control of cellular response to damaged DNA. GSK-3 normally phosphorylates beta catenin, which leads to beta catenin degratation. When GSK-3 is inhibited, beta catenin increases and transgenic mice with overexpression of beta catenin express similar behaviour to mice treated with lithium. These results suggest that increase of beta catenin may be a possible pathway for the therapeutic action of lithium.
Pharmacodynamics
Although lithium has been used for over 50 years in treatment of bipolar disorder, the mechanism of action is still unknown. Lithium's therapeutic action may be due to a number of effects, ranging from inhibition of enzymes such as glycogen synthase kinase 3, inositol phosphatases, or modulation 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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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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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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