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Acetylcarnitine

Cat No.:V72709 Purity: ≥98%
Acetylcarnitine is an endogenously produced metabolite.
Acetylcarnitine
Acetylcarnitine Chemical Structure CAS No.: 14992-62-2
Product category: Endogenous Metabolite
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
5mg
10mg
50mg
100mg
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Product Description
Acetylcarnitine is an endogenously produced metabolite.
Acetylcarnitine (ALCAR) is an endogenous acetylated derivative of carnitine that efficiently crosses the blood-brain barrier. It is a CNS-penetrant endogenous metabolite that plays a crucial role in mitochondrial metabolism. By facilitating the transport of fatty acids into mitochondria for beta-oxidation, it provides energy to neurons. Acetylcarnitine is formed naturally in the body and is involved in linking mitochondrial metabolism to histone acetylation and lipogenesis. It exhibits antioxidant and neuroprotective activities, making it a compound of interest in neurodegenerative disease research.
Biological Activity I Assay Protocols (From Reference)
Targets
Acetylcarnitine primarily targets mitochondria and is involved in the carnitine shuttle system, which transports fatty acids across the inner mitochondrial membrane via carnitine acyltransferases. It also acts as an acetyl group donor, influencing histone acetylation and gene expression. Additionally, it may interact with and activate carnitine acetyltransferase (CrAT) and other mitochondrial enzymes.
ln Vitro
In vitro, acetylcarnitine (10 mM) generates acetyl-CoA in ACLY/ACSS2-deficient cells, restoring histone acetylation and cell proliferation under lipid-depleted conditions. It attenuates oxidative stress and neuroinflammation in cultured neuronal cells. Studies have shown that acetylcarnitine improves glucose utilization in type 2 diabetic models by increasing glycogen synthase activity. It also exhibits protective effects against peripheral neuropathy and enhances sperm motility in vitro.
ln Vivo
In vivo, acetylcarnitine has demonstrated positive effects on mental fatigue, neurodegenerative diseases (including Alzheimer's disease), cognitive function, and peripheral neuropathy in animal models. It exhibits neuroprotective effects in Alzheimer's models, reducing oxidative damage and improving cognitive performance. Orally administered acetylcarnitine is absorbed and penetrates the CNS, where it exerts its bioactivity. It is also used as a candidate diagnostic and prognostic biomarker for hepatocellular carcinoma.
Enzyme Assay
For non-cellular enzyme assays, carnitine acetyltransferase (CrAT) activity can be measured spectrophotometrically using 5,5′-dithiobis(2-nitrobenzoic acid) (DTNB). The assay buffer (100 mM Tris-HCl, pH 8.0, 0.5 mM EDTA) contains 0.5 mM acetyl-CoA, 10 mM L-carnitine, and 0.2 mM DTNB. Acetylcarnitine (1-10 mM) is added, and the increase in absorbance at 412 nm (due to TNB formation) is recorded for 5-10 minutes at 37degC. Alternatively, mass spectrometry can quantify acetylcarnitine levels.
Cell Assay
For cell-based assays, neuronal cell lines (e.g., SH-SY5Y or primary rat cortical neurons) are seeded in 96-well plates (1×10⁴ cells/well) and cultured in DMEM/F12 with 10% FBS. After 24 hours, cells are treated with acetylcarnitine (0.1-10 mM) for 24-48 hours. Cell viability is measured by MTT assay (0.5 mg/mL, 4h). Oxidative stress is evaluated using DCFH-DA (10 uM, 30 min) fluorescence. For neuroprotection studies, cells are pre-treated with acetylcarnitine for 2 hours before exposure to Abeta peptide (10 uM) or H2O2 (200 uM). Apoptosis is quantified via caspase-3/7 activity using a luminescent assay.
Animal Protocol
For in vivo experiments, Alzheimer's disease model mice (e.g., APP/PS1 transgenic mice, 6 months old) are used. Acetylcarnitine is dissolved in saline and administered intraperitoneally (IP) or orally at doses of 50-300 mg/kg/day for 4-8 weeks. Behavioral tests such as Morris water maze (for spatial learning and memory) and novel object recognition are performed. After sacrifice, brain tissues are collected for analysis of amyloid-beta plaques (Thioflavin S staining), oxidative stress markers (MDA, SOD), and neuroinflammation (IL-1beta, TNF-alpha by ELISA).
ADME/Pharmacokinetics
Absorption, Distribution and Excretion
Acetylcarnitine supplements are absorbed in a similar manner to L-carnitine. Acetylcarnitine is excreted in a similar manner to L-carnitine. Both are excreted through the kidneys and involve renal tubular secretion.
Acetylcarnitine is an endogenous metabolite with high oral bioavailability and effective CNS penetration. It is transported across biological membranes via carnitine transporters. Its half-life in humans is approximately 4-6 hours. It is rapidly absorbed from the gastrointestinal tract and distributed to tissues, particularly the brain, heart, and skeletal muscle. It is metabolized via deacetylation to carnitine and excreted primarily in urine.
Toxicity/Toxicokinetics
Toxicity Summary
The CIR expert panel concluded that, under the existing methods of use and concentrations described in the safety assessment, the following ingredient is safe when formulated into a non-irritating formulation: ...acetylcarnitine...
safe for use in cosmetics, subject to certain conditions.
Acetylcarnitine is an endogenous compound and is generally recognized as safe (GRAS) at physiological concentrations. In animal studies, it has a low toxicity profile with an LD₅0 of >2000 mg/kg (oral, rat). No significant adverse effects have been reported at therapeutic doses up to 300 mg/kg/day. In clinical use as a dietary supplement, it is well-tolerated with occasional mild gastrointestinal discomfort. Standard safety precautions should be followed when handling.
Additional Infomation
Pharmacodynamics
The full physiological effects of acetylcarnitine are still under investigation. Currently, acetylcarnitine has been found to have positive effects on mental fatigue, neurodegenerative diseases, cognitive function, peripheral neuropathy, and sperm motility. Specifically, a study on HIV-infected individuals showed that patients supplemented with acetylcarnitine experienced increased CD4 cell counts, reduced lymphocyte apoptosis, improved polyneuropathy and cardiovascular damage, and decreased blood triglyceride and TNF-α levels. Another study suggests that acetylcarnitine may improve glucose utilization in patients with type 2 diabetes by increasing the activity of glycogen synthase.
Acetylcarnitine is an endogenous metabolite with established clinical use as a dietary supplement and investigational therapeutic agent. It has been studied for potential benefits in Alzheimer's disease, depression, peripheral neuropathy, and male infertility. It is not an FDA-approved drug for these indications but is available as a nutraceutical. Its mechanism involves enhancing mitochondrial function, reducing oxidative stress, and modulating neuroinflammation. Numerous clinical trials have investigated acetylcarnitine (e.g., for Alzheimer's disease, fibromyalgia, and diabetic neuropathy), with some positive results.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C9H17NO4
Molecular Weight
203.24
Exact Mass
203.115
CAS #
14992-62-2
PubChem CID
1
Appearance
White to off-white solid powder
Melting Point
145°C
LogP
-4.15
Hydrogen Bond Donor Count
0
Hydrogen Bond Acceptor Count
4
Rotatable Bond Count
5
Heavy Atom Count
14
Complexity
214
Defined Atom Stereocenter Count
0
SMILES
CC(=O)OC(CC(=O)[O-])C[N+](C)(C)C
InChi Key
RDHQFKQIGNGIED-UHFFFAOYSA-N
InChi Code
InChI=1S/C9H17NO4/c1-7(11)14-8(5-9(12)13)6-10(2,3)4/h8H,5-6H2,1-4H3
Chemical Name
3-acetyloxy-4-(trimethylazaniumyl)butanoate
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: (1). This product requires protection from light (avoid light exposure) during transportation and storage.  (2). Please store this product in a sealed and protected environment (e.g. under nitrogen), 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: 250 mg/mL (1230.07 mM)
Solubility (In Vivo)
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.

Injection Formulations
(e.g. IP/IV/IM/SC)
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution 50 μL Tween 80 850 μL Saline)
*Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution.
Injection Formulation 2: DMSO : PEG300Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO 400 μLPEG300 50 μL Tween 80 450 μL Saline)
Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO 900 μL Corn oil)
Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals).
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Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO 900 μL (20% SBE-β-CD in saline)]
*Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO 100 μLPEG300 200 μL castor oil 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10: 10 : 80 (i.e. 100 μL Ethanol 100 μL Cremophor 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH 400 μLPEG300 50 μL Tween 80 450 μL Saline)


Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium)
Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose
Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals).
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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders


Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 4.9203 mL 24.6015 mL 49.2029 mL
5 mM 0.9841 mL 4.9203 mL 9.8406 mL
10 mM 0.4920 mL 2.4601 mL 4.9203 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.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

  • Calculate the Mass of a compound required to prepare a solution of known volume and concentration
  • Calculate the Volume of solution required to dissolve a compound of known mass to a desired concentration
  • Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume
An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
  • Enter 350.26 in the Molecular Weight (MW) box
  • Enter 10 in the Concentration box and choose the correct unit (mM)
  • Enter 5 in the Volume box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
  • Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
  • Enter 25 into the Concentration (End) box and select the correct unit (mM)
  • Enter 25 into the Volume (End) box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
  • To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

  • Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
  • Click the “Calculate” button
  • The answer appears in the Volume (to add to vial) box
In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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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.

Clinical Trial Information
A Pilot Study Investigating the Effects of Acetyl-L-Carnitine and Vincristine-Induced Neuropathy in Pediatric Patients With ALL
CTID: NCT02598622
Phase: Phase 2    Status: Terminated
Date: 2017-03-03
Acetyl-L-carnitine in Combination With a Cisplatin-containing Chemotherapy as First Line Treatment of Advanced or Metastatic Non Small Cell Lung Cancer
CTID: NCT01379976
Phase: Phase 3    Status: Terminated
Date: 2015-04-24
Clinical Study on Acetyl-L-Carnitine
CTID: NCT01526564
Phase: Phase 3    Status: Completed
Date: 2013-11-11
Acetyl-L-Carnitine Supplementation During HCV Therapy With Pegylated Interferon-α2b Plus Ribavirin
CTID: NCT01913964
Phase: Phase 4    Status: Completed
Date: 2013-08-
Phase II Explorative Study of Acetyl-L-Carnitine (ST 200) for Vincristine-Induced Neurotoxicity in Patients With Acute Lymphoblastic Leukemia (ALL).
CTID: null
Phase: Phase 2    Status: Prematurely Ended
Date: 2006-03-21
Evaluation of the efficacy and tollerability of long-term somministration of Acetyl-l-carnitine in the treatment of HIV related lipodystrophy.Parallel group, randomized, double blind, controlled versus placebo study.
CTID: null
Phase: Phase 2    Status: Completed
Date: 2006-03-17
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DOUBLE-BLIND PLACEBO-CONTROLLED TRIAL ON THE USE OF ACETYL-L-CARNITINE FOR THE TREATMENT OF AMYOTROPHIC LATERAL SCLEROSIS (ALS)
CTID: null
Phase: Phase 2    Status: Completed
Date: 2005-04-15

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