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HomeProduct name listZoledronic acid hydrate

Zoledronic acid hydrate

Synonym(s):[1-hydroxy-2-(1H-imidazol-1-yl)ethane-1,1-diyl]bis(phosphonic acid) monohydrate;P,P′-[1-Hydroxy-2-(1H-imidazol-1-yl)ethylidene]bisphosphonic acid monohydrate;Zoledronate monohydrate

Zoledronic acid hydrate Structural

What is Zoledronic acid hydrate?

The Uses of Zoledronic acid hydrate

A highly potent bisphosphonate and activator of PKC.

The Uses of Zoledronic acid hydrate

Zoledronic acid monohydrate is an anti-resorptive agent for cancer bone metasis, also used on studies in the environmental risk asseessment of drugs from view of excretion form to environment.

What are the applications of Application

Zoledronic acid monohydrate is a highly potent bisphosphonate and activator of PKC

brand name

Zometa (Novartis).

General Description

Pharmaceutical secondary standards for application in quality control provide pharma laboratories and manufacturers with a convenient and cost-effective alternative to the preparation of in-house working standards

Biological Activity

Zoledronic acid (Zoledronate, CGP-4244) monohydrate is the monohydrate of Zoledronic acid (Zoledronic acid), a potent osteoclast inhibitor that inhibits small GTP-binding proteins by inhibiting enzymes of the mevalonate pathway Such as the prenylation of Ras and Rho to induce osteoclast apoptosis.

Biochem/physiol Actions

Zoledronic acid (zoledronate) is a bisphosphonate bone resorption inhibitor, an inhibitor of farnesyl diphosphate (FPP) synthase which results in downstream inhibition of osteoclast activity and reduced bone resorption and turnover. It has been used to treat postmenopausal osteoporosis, Paget′s disease, hypercalcemia, and along with cancer chemotherapy to treat bone damage caused by cancer that has spread to the bones.

in vitro

Zoledronic Acid monohydrate (0.1-1 μM; 48 hours) increases receptor activator of nuclear factor kB ligand (RANKL) and sclerostin mRNA expressions in osteocyte-like MLO-Y4 cells.Zoledronic Acid monohydrate increases the expression of osteoclastogenesis supporting factor from MLO-Y4 cells.Zoledronic Acid monohydrate enhances the RANKL expression via IL-6/ JAK2/STAT3 pathway in MLO-Y4 cells.Zoledronic Acid monohydrate inhibits osteoclast differentiation and function through the regulation of NF-κB and JNK signalling pathways.Zoledronic Acid monohydrate (10-100 μM; 1-7 days) markedly reduces the viability of MC3T3-E1 cells.Zoledronic Acid monohydrate (10-100 μM; 1-7 days) induces apoptosis in MC3T3-E1 cells.Zoledronic Acid monohydrate (10-100 μM; 4 days) inhibits cell viability due to the induction of apoptosis.Zoledronic Acid monohydrate exerts inhibitory effects on the differentiation and maturation of MC3T3-E1 cells at concentrations <1 μM.

in vivo

Zoledronic Acid monohydrate (0.05 mg/kg; i.p.; weekly; for 3 weeks) increases bone mineral density and content.Zoledronic Acid monohydrate (0.5-1 mg/kg; i.p.; weekly; for 3 weeks) inhibits both osteoclast and osteoblasts function and bone remodeling in vivo interfering with bone mechanical properties.

Properties of Zoledronic acid hydrate

Melting point: 245 °C(dec.)
storage temp.  2-8°C
solubility  H2O: ≥2mg/mL
form  powder
color  white to beige
Merck  14,10187
CAS DataBase Reference 165800-06-6(CAS DataBase Reference)

Safety information for Zoledronic acid hydrate

Signal word Warning
Pictogram(s)
ghs
Exclamation Mark
Irritant
GHS07
GHS Hazard Statements H315:Skin corrosion/irritation
H319:Serious eye damage/eye irritation
H335:Specific target organ toxicity, single exposure;Respiratory tract irritation
Precautionary Statement Codes P261:Avoid breathing dust/fume/gas/mist/vapours/spray.
P264:Wash hands thoroughly after handling.
P264:Wash skin thouroughly after handling.
P271:Use only outdoors or in a well-ventilated area.
P280:Wear protective gloves/protective clothing/eye protection/face protection.
P302+P352:IF ON SKIN: wash with plenty of soap and water.
P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

Computed Descriptors for Zoledronic acid hydrate

InChIKey FUXFIVRTGHOMSO-UHFFFAOYSA-N

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