Mildronate

Names

[ Name ]:
Mildronate

[Synonym ]:
Diazanium, 2-(2-carboxyethyl)-1,1,1-trimethyl-, inner salt
MET88
Meldonium
3-(2,2,2-Trimethyldiazan-2-ium-1-yl)propanoate
MFCD00876389
Quaterin
Mildronate
UNII-73H7UDN6EC

Biological Activity

[Description]:

Mildronate (Meldonium) functions as a cardioprotective drug by cpmpetetively inhibiting BBOX1 and OCTN2. Mildronate (Meldonium) exhibits IC50 values of 34-62 μM for human recombinant BBOX and an EC50 of 21 μM for human OCTN2. Mildronate (Meldonium) treatment-induced redirection of long-chain FA metabolism from mitochondria to peroxisomes[1].

[Related Catalog]:

Research Areas >> Cardiovascular Disease

Signaling Pathways >> Others >> Others

Research Areas >> Metabolic Disease

[Target]

IC50: 34-62 μM (human recombinant BBOX). EC50: 21 μM (human OCTN2).

[References]

[1]. Dambrova M, et al. Pharmacological effects of meldonium: Biochemical mechanisms and biomarkers of cardiometabolic activity. Pharmacol Res. 2016 Nov;113(Pt B):771-780.

[2]. Schobersberger W, et al. Story behind meldonium-from pharmacology to performance enhancement: a narrative review. Br J Sports Med. 2017 Jan;51(1):22-25.

Chemical & Physical Properties

[ Melting Point ]:
85-90ºC

[ Molecular Formula ]:
C₆H₁₄N₂O₂

[ Molecular Weight ]:
146.188

[ Exact Mass ]:
146.105530

[ PSA ]:
52.16000

[ Index of Refraction ]:
1.598

[ Storage condition ]:
Refrigerator

[ Stability ]:
Hygroscopic

Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :: MW0333620

CHEMICAL NAME :: Hydrazinium, 2-(2-carboxyethyl)-1,1,1-trimethyl-, hydroxide, inner salt

CAS REGISTRY NUMBER :: 76144-81-5

LAST UPDATED :: 199703

DATA ITEMS CITED :: 7

MOLECULAR FORMULA :: C6-H14-N2-O2

MOLECULAR WEIGHT :: 146.22

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >20 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: EKFMA7 Eksperimental'naya i Klinicheskaya Farmakoterapiya. (Izdatel'stvo Zinantne, Riga, USSR) No.1- 1970- Volume(issue)/page/year: 19,67,1991

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 12 gm/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Lungs, Thorax, or Respiration - respiratory stimulation

REFERENCE :: EKFMA7 Eksperimental'naya i Klinicheskaya Farmakoterapiya. (Izdatel'stvo Zinantne, Riga, USSR) No.1- 1970- Volume(issue)/page/year: 19,67,1991

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 18500 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: EKFMA7 Eksperimental'naya i Klinicheskaya Farmakoterapiya. (Izdatel'stvo Zinantne, Riga, USSR) No.1- 1970- Volume(issue)/page/year: 19,67,1991

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 7850 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: BAXXDU British UK Patent Application. (U.S. Patent and Trademark Office, Foreign Patents, Washington, DC 20231) Volume(issue)/page/year: #2105992

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 4430 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: BAXXDU British UK Patent Application. (U.S. Patent and Trademark Office, Foreign Patents, Washington, DC 20231) Volume(issue)/page/year: #2105992

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Mammal - cat

DOSE/DURATION :: >4 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: EKFMA7 Eksperimental'naya i Klinicheskaya Farmakoterapiya. (Izdatel'stvo Zinantne, Riga, USSR) No.1- 1970- Volume(issue)/page/year: 19,67,1991

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 8 gm/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Lungs, Thorax, or Respiration - respiratory depression Lungs, Thorax, or Respiration - other changes

REFERENCE :: EKFMA7 Eksperimental'naya i Klinicheskaya Farmakoterapiya. (Izdatel'stvo Zinantne, Riga, USSR) No.1- 1970- Volume(issue)/page/year: 19,67,1991

Safety Information

[ HS Code ]:
2928000090

Precursor & DownStream

Precursor

DownStream

Customs

[ HS Code ]: 2928000090

[ Summary ]:
2928000090 other organic derivatives of hydrazine or of hydroxylamine VAT:17.0% Tax rebate rate:9.0% Supervision conditions:none MFN tariff:6.5% General tariff:20.0%