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Chemical Structure| 51037-30-0 Chemical Structure| 51037-30-0

Structure of Acipimox
CAS No.: 51037-30-0

Chemical Structure| 51037-30-0

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Acipimox is a niacin derivative used as a hypolipidemic agent.

Synonyms: K-9321

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Product Details of Acipimox

CAS No. :51037-30-0
Formula : C6H6N2O3
M.W : 154.12
SMILES Code : O=C(C1=C[N+]([O-])=C(C)C=N1)O
Synonyms :
K-9321
MDL No. :MFCD00865757
InChI Key :DJQOOSBJCLSSEY-UHFFFAOYSA-N
Pubchem ID :5310993

Safety of Acipimox

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H319
Precautionary Statements:P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
HEK-293 cells 100 pM to 10 μM 20 cycles To measure the effect of Acipimox on G-protein signaling and β-arrestin recruitment of GPR109A. Results showed that Acipimox behaved as a full agonist but with lower potency in G-protein dissociation, cAMP response, and βarr recruitment assay. PMC10908815

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Patients with non-insulin-dependent diabetes mellitus Human patients Oral 2×250 mg Single dose, experiment lasted approximately 6 hours To study the effect of Acipimox on glucose metabolism under basal and insulin-stimulated conditions. Results showed that Acipimox reduced NEFA levels in both basal and insulin-stimulated states, inhibited lipid oxidation, increased insulin-stimulated glucose disposal rate, and enhanced basal and insulin-stimulated muscle glycogen synthase activity. PMC295597
C57BL/6 mice High-methionine diet-induced hyperhomocysteinemia model Oral 0.08 g/kg Once daily for 8 weeks To evaluate the effect of Acipimox on Hcy-induced lipolysis and nonalcoholic fatty liver, results showed that Acipimox significantly reduced Hcy-induced lipolysis and hepatic lipid accumulation PMC7559542
LDLR null mice Atherosclerosis model Oral administration in drinking water 0.05% wt 14 weeks Evaluate the effect of Acipimox on ritonavir-induced atherosclerosis, results showed Acipimox reversed the adverse effects of ritonavir PMC2783673
C57BL6/J mice Intermittent hypoxia model Drinking water 0.5 mg/ml 14 days To investigate the effect of acipimox on glucose tolerance and insulin sensitivity in mice exposed to intermittent hypoxia, results showed that acipimox fully prevented IH-induced impairments in fasting glycemia, glucose tolerance, and insulin sensitivity. PMC4979366
Nude mice Prostate cancer xenograft model Oral gavage 50 mg/kg Single dose, 1 hour before tracer injection In PC3 xenografts, Acipimox significantly increased tumor uptake of 18F-FDG and improved tumor-to-background ratios; no significant effect was observed in CWR22R v1 xenografts. PMC3662867
C57BL/6J mice High-fat diet-induced obesity model Drinking water 0.05% 12 weeks To study the effects of acipimox on e-cigarette-induced cardiac dysfunction. Results showed that acipimox reversed the e-cigarette-induced decrease in cardiac systolic function, increased levels of inflammatory cytokines and free fatty acids (FFAs), oxidative stress, and DNA damage. PMC10600141

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT01299831 Healthy Not Applicable Completed - Denmark ... More >> Department of medical endocrinology, University Hospital of Aarhus Aarhus, Denmark, 8000 Less <<
NCT01752348 Systemic Inflammatory Response... More >> Syndrome Less << Not Applicable Completed - Denmark ... More >> Medical Research Laboratory, Department of Internal Medicine and Endocrinology Aarhus C, Denmark, 8000 Less <<
NCT00449423 Acute Heart Failure Phase 2 Terminated(due to slow recruit... More >>ment) Less << - Denmark ... More >> Aarhus University Hospital, Skejby Sygehus, Department of Cardiology Aarhus, Denmark, 8200 Less <<
NCT02792621 Impaired Mitochondrial Functio... More >>n, Muscle Performance Less << Not Applicable Recruiting December 8, 2018 United Kingdom ... More >> NIHR Exeter Clinical Research Facility Recruiting Exeter, Devon, United Kingdom, EX2 5DW Contact: Anna Steele, PhD    01392 408173    anna.steele@nhs.net    Contact: Kim Rownden    01392 408188    kim.rowden@nhs.net Less <<
NCT03325491 Impaired Mitochondrial Functio... More >>n, Muscle Performance Less << Not Applicable Recruiting December 31, 2018 United Kingdom ... More >> NIHR Exeter Clinical Research Facility Recruiting Exeter, Devon, United Kingdom, EX2 5DW Contact: Colleen Deane, PhD    01392722882    c.s.deane@exeter.ac.uk Less <<
NCT01209416 Metabolism In... More >>sulin Resistance Hypopituitarism Less << Not Applicable Completed - Denmark ... More >> University Hospital of Aarhus Aarhus, Denmark, 8000 Less <<
NCT00759291 Metabolic Syndrome Phase 2 Phase 3 Completed - United States, Massachusetts ... More >> Brigham and Women's Hospital Boston, Massachusetts, United States, 02115 Less <<
NCT02256722 Healthy Phase 1 Completed - -
NCT02782208 Hypopituitarism ... More >> Insulin Resistance Endocrine System Diseases Glucose Metabolism Disorders Metabolic Diseases Pituitary Diseases Brain Diseases Less << Not Applicable Unknown November 2018 Denmark ... More >> University Hospital of Aarhus Recruiting Aarhus, Denmark, 8000 Contact: Astrid J Hjelholt, MD    +4524800664    ajh@clin.au.dk Less <<
NCT00153179 Type 2 Diabetes Mellitus Phase 1 Phase 2 Completed - United States, Massachusetts ... More >> Brigham & Women's Hospital Boston, Massachusetts, United States, 02115 Less <<
NCT00153179 - Completed - -
NCT00246402 Insulin Resistance ... More >> Cardiovascular Diseases Heart Diseases HIV Infections Hypertriglyceridemia Hyperlipidemia Less << Not Applicable Completed - United States, Massachusetts ... More >> Massachusetts General Hospital Boston, Massachusetts, United States, 02114 Less <<
NCT00549614 Heart Failure Not Applicable Completed - Denmark ... More >> Department of Cardiology, Aarhus Universityhospital, Skejby Aarhus N, Denmark, 8200 Less <<
NCT01980524 Type 2 Diabetes Phase 2 Phase 3 Completed - Austria ... More >> Division of Endocrinology and Metabolism, Internal Medicine III, Medical University of Vienna Vienna, Austria, 1090 Less <<
NCT01980524 - Completed - -
NCT01260376 Diabetes Obes... More >>ity Less << Not Applicable Completed - Denmark ... More >> University Hospital of Aarhus, Norrebrogade Aarhus, Denmark, 8000 University Hospital of Aarhus, Norrebrogade Aarhus, Denmark, 8 Less <<
NCT01580813 Type 2 Diabetes Not Applicable Recruiting December 2018 United States, Colorado ... More >> University of Colorado Anschutz Medical Campus Recruiting Aurora, Colorado, United States, 80045 Principal Investigator: Irene Schauer, MD, PhD Less <<
NCT01488409 Abdominal Obesity ... More >> Insulin Resistance Hypertriglyceridemia Less << Phase 2 Completed - United States, Massachusetts ... More >> Massachusetts General Hospital Boston, Massachusetts, United States, 02114 Less <<
NCT01488409 - Completed - -
NCT01816165 Type 1 Diabetes Phase 3 Active, not recruiting September 2018 United States, Colorado ... More >> University of Colorado Denver Aurora, Colorado, United States, 80045 Less <<
NCT00943059 Diabetes Mellitus, Type 2 ... More >> Cardiomyopathy, Dilated Less << Not Applicable Completed - Netherlands ... More >> Maastricht University Medical Centre Maastricht, Netherlands, 6200MD Less <<
NCT03338387 Eating Disorder ... More >> Bulimia Nervosa Less << Phase 2 Enrolling by invitation August 1, 2018 -
NCT02796950 Diabetes Mellitus Type 2 Not Applicable Completed - Denmark ... More >> University Hospital of Aarhus Aarhus, Denmark, 8000 Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

6.49mL

1.30mL

0.65mL

32.44mL

6.49mL

3.24mL

64.88mL

12.98mL

6.49mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2
The prepared working fluid is recommended to be prepared now and used up as soon as possible in a short period of time. The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1

References

 

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