165800-06-6 Usage
Description
Zoledronic acid hydrate, also known as Zoledronic acid monohydrate, is a highly potent bisphosphonate and activator of PKC. It is a pharmaceutical secondary standard used for quality control in pharmaceutical laboratories and manufacturing. It is known for its strong anti-resorptive properties and its ability to activate protein kinase C (PKC), making it a valuable compound in various medical and environmental applications.
Uses
Used in Pharmaceutical Industry:
Zoledronic acid hydrate is used as a pharmaceutical compound for its anti-resorptive properties and activation of PKC. It is particularly effective in the treatment of cancer bone metastasis, where it helps to slow down the resorption of bone tissue and reduce the risk of skeletal-related events.
Used in Cancer Treatment:
Zoledronic acid hydrate is used as an anti-resorptive agent for cancer bone metastasis. It helps to prevent the breakdown of bone tissue, which is a common issue in patients with metastatic cancer. By inhibiting bone resorption, it can help to reduce pain and improve the quality of life for cancer patients.
Used in Environmental Risk Assessment:
Zoledronic acid hydrate is also used in studies for the environmental risk assessment of drugs. It is studied from the perspective of excretion forms to the environment, helping to understand the potential impact of pharmaceutical compounds on the environment and develop strategies to minimize their ecological footprint.
Used in Quality Control:
As a pharmaceutical secondary standard, Zoledronic acid hydrate is used in quality control processes in pharmaceutical laboratories and manufacturing. It provides a convenient and cost-effective alternative to the preparation of in-house working standards, ensuring the quality and consistency of pharmaceutical products.
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.
Check Digit Verification of cas no
The CAS Registry Mumber 165800-06-6 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,6,5,8,0 and 0 respectively; the second part has 2 digits, 0 and 6 respectively.
Calculate Digit Verification of CAS Registry Number 165800-06:
(8*1)+(7*6)+(6*5)+(5*8)+(4*0)+(3*0)+(2*0)+(1*6)=126
126 % 10 = 6
So 165800-06-6 is a valid CAS Registry Number.
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
165800-06-6Relevant articles and documents
Crystalline forms of zoledronic acid
-
Page/Page column 14, (2008/12/05)
The invention relates to new crystalline forms of low water soluble salts of zoledronic acid, the process for preparation of these crystalline forms, compositions containing these crystalline forms, and the use of these crystalline forms in diagnostic methods or therapeutic treatment of warm-blooded animals, especially humans. The invention relates to the crystalline form of the free acid monohydrate of zoledronic acid, the process for preparation of the crystalline form of the free acid monohydrate of zoledronic acid, compositions containing the crystalline form of the free acid monohydrate of zoledronic acid, and the use of crystalline form of the free acid monohydrate of zoledronic acid in diagnostic methods or therapeutic treatment of warm-blooded animals, especially humans.
CRYSTALLINE TRIHYDRATE OF ZOLEDRONIC ACID
-
Page/Page column 15, (2008/06/13)
Zoledronic acid trihydrate, processes for its preparation, and conversion into zoledronic acid monohydrate.
