Name | Zoledronic acid hydrate |
Synonyms | Zoledronic acid hydrate zoledronic acid hydrate ZoledronicacidforInjection ZOLEDRONIC ACID MONOHYDRATE (1-hydroxy-2-imidazol-1-ylethylidene)diphosphonic acid monohydrate (1-hydroxy-2-imidazol-1-yl-1-phosphono-ethyl)phosphonic acid hydrate [1-HYDROXY-(1H-IMIDAZOL-1-YL)-PHOSPHONOETHYL] PHOSPHONIC ACID MONOHYDRATE PHOSPHONIC ACID, [1-HYDROXY-2-(1H-IMIDAZOL-1-YL)ETHYLIDENE]BIS-, MONOHYDRATE [1-hydroxy-2-(1H-imidazol-1-yl)ethane-1,1-diyl]bis(phosphonic acid) monohydrate |
CAS | 165800-06-6 |
InChI | InChI=1/C5H10N2O7P2.H2O/c8-5(15(9,10)11,16(12,13)14)3-7-2-1-6-4-7;/h1-2,4,8H,3H2,(H2,9,10,11)(H2,12,13,14);1H2 |
InChIKey | FUXFIVRTGHOMSO-UHFFFAOYSA-N |
Molecular Formula | C5H12N2O8P2 |
Molar Mass | 290.1 |
Melting Point | 245 °C(dec.) |
Boling Point | 764°C at 760 mmHg |
Flash Point | 415.8°C |
Solubility | H2O: ≥2mg/mL |
Vapor Presure | 1.53E-24mmHg at 25°C |
Appearance | White-like crystal |
Color | white to beige |
Merck | 14,10187 |
Storage Condition | 2-8°C |
Hazard Symbols | Xi - Irritant![]() |
Risk Codes | 36/37/38 - Irritating to eyes, respiratory system and skin. |
Safety Description | 26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. |
WGK Germany | 3 |
RTECS | SZ8562450 |
HS Code | 29332900 |
Biological activity | Zoledronic acid (Zoledronate, CGP-4244) monohydrate is a monohydrate of Zoledronic acid (zoledronic acid), which is an effective osteoclast Inhibitor can induce osteoclast apoptosis by inhibiting enzymes of the mevale dihydroxyacid pathway and preventing isoprene of small GTP-binding proteins such as Ras and Rho. |
Target | Value |
Cell Line: | MC3T3-E1 cells MC3T3-E1 cells MC3T3-E1 cells |
Concentration: | 0.02 µM , 0.1 µM, 1 µM, 10 µM, 100 µM 0.02 µM , 0.1 µM, 1 µM, 10 µM, 100 µM 0.02 µM , 0.1 µM, 1 µM, 10 µM, 100 µM |
Incubation Time: | 1 day, 3 days, 5 days, 7 days 1 days, 4 days, 7 days 4 days |
Result: | Reduced cells viability at 10 µM and 100 µM. Increased the number of early apoptotic cells and late apoptotic or necrotic cells at dose-dependent and time-dependent (high concentrations). Down-regulated the protein level of inactive caspase-3 and up-regulated the protein level of active caspase-3 at the concentrations of 10 and 100 µM. Inhibited both osteoclast and osteoblasts function and bone remodeling at 0.5 mg/kg and 1 mg/kg. |
Animal Model: | Five-week-old C57BL6 mice |
Dosage: | 0.05 mg/kg, 0.5 mg/kg, 1 mg/kg |
Administration: | Intraperitoneal injection, weekly, for 3 weeks |