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Drug

D1393 | Clodronate

Molecular Formula CH4Cl2O6P2
Molecular Weight 244.89
Structure
State solid
Protein binding 2%-36%
Half life Approximately 13 hours.
Absorption After oral administration, absorption is estimated at 1–3% of the ingested dose because of the low uptake from the gastrointestinal tract.

M

M05BA02 Clodronic acid


[M05BA] Bisphosphonates


[M05B] DRUGS AFFECTING BONE STRUCTURE AND MINERALIZATION


[M05] DRUGS FOR TREATMENT OF BONE DISEASES


[M] Musculoskeletal system

Toxicity Dose Time Species Model Method Action Positive criterion Reference
MEMBRANE POTENTIAL > 400 µM 30 mins mouse liver mitochondria Rh123 fluorescence (excitation 485 nm, emission 535 nm) are recorded using a fluorescence multi-well plate reader (mCICCP (20 µM) treatments was considered as the 100% baseline for ΔΨm loss) decrease EC20 36
RESPIRATION > 400 µM 60 mins mouse liver mitochondria Oxygen consumption was monitored with 50nM MitoXpress ( an oxygen-sensitive phosphorescent dye) using a spectrofluorimeter (Tecan Infinite 200; λExcitation 380nm; λEmission 650nm). Rotenone (2µM) was used as 100% baseline for complex I inhibition. decrease EC20 36
RESPIRATION 227.2 µM 60 mins mouse liver mitochondria Oxygen consumption was monitored with 50nM MitoXpress ( an oxygen-sensitive phosphorescent dye) using a spectrofluorimeter (Tecan Infinite 200; λExcitation 380nm; λEmission 650nm). Oligomycin A (1µM) was used as 100% baseline for complex II inhibition. decrease EC20 36
SWELLING > 400 µM 30 mins mouse liver mitochondria swelling assay: Absorbance at 545 nm using a fluorescence multi-well plate reader (CaCl2 (50 µM) was considered as the 100% baseline for the swelling ) increase EC20 36

Target Dose Time Species Model Method Action Positive criterion Reference
NADH:ubiquinone reductase > 400 µM 60 mins mouse liver mitochondria Oxygen consumption was monitored with 50nM MitoXpress ( an oxygen-sensitive phosphorescent dye) using a spectrofluorimeter (Tecan Infinite 200; λExcitation 380nm; λEmission 650nm). Rotenone (2µM) was used as 100% baseline for complex I inhibition. inhibit EC20 36
Succinate dehydrogenase 227.2 µM 60 mins mouse liver mitochondria Oxygen consumption was monitored with 50nM MitoXpress ( an oxygen-sensitive phosphorescent dye) using a spectrofluorimeter (Tecan Infinite 200; λExcitation 380nm; λEmission 650nm). Oligomycin A (1µM) was used as 100% baseline for complex II inhibition. inhibit EC20 36
Cytochrome c > 400 µM 30 mins mouse liver mitochondria Cytochrome c release was evaluated using ELISA kit ( 20 µg/ml Alamethicin was used as 100% baseline) release EC20 36

Organism Test type Route Dose (normalized dose) Effect Source
rat LDLo subcutaneous 1600mg/kg (1600mg/kg) Journal of Pharmacology and Experimental Therapeutics. Vol. 266, Pg. 1691, 1993.
rat LDLo oral 2500mg/kg (2500mg/kg) Journal of Pharmacology and Experimental Therapeutics. Vol. 266, Pg. 1691, 1993.


  • DrugBank DB00720
    CAS Number 10596-23-3, 22560-50-5
    PubChem Compound 25419