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Zoledronic Acid 118072-93-8

Product Description

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Molecular Weight:

272.09 Zoledronic acid induces Apoptosis in osteoclasts by inhibiting enzymes of the mevalonate pathway and preventing the isoprenylation of small GTP-binding Proteins such as Ras and Rho.


Biological Activity


Zoledronic acid (10 µM and 100 µM) causes a significant reduction in the
proportions of MCF-7 cells (49.54% and 23.55% of control, respectively)
(P Zoledronic acid enhances OPG gene expression and protein secretion
by human osteoblasts (hOB) in a dose-dependent fashion with a maximum
effect at 10 nM after 72 hours, consistent with the higher biological
potency of Zoledronic acid.


Zoledronic acid prevents the inhibitory
effects of the glucocorticoid dexamethasone on OPG mRNA and protein
production in human osteoblasts. Zoledronic acid induces type I collagen
secretion and alkaline phosphatase activity by 2- and 4-fold,
respectively, in human osteoblasts.


Zoledronic acid (120 mg/kg, s.c.) prevents the formation of lesions,
prevents cancellous bone loss and loss of bone mineral density, and
reduces osteoclast perimeter in 5T2MM-bearing mice. Zoledronic acid (120
mg/kg, s.c.) also decreases paraprotein concentration, decreases tumor
burden, and reduces Angiogenesis in 5T2MM-bearing mice.


Protocol(Only for Reference)


Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)


Species Baboon Dog Monkey Rabbit Guinea pig Rat Hamster Mouse
Weight (kg) 12 10 3 1.8 0.4 0.15 0.08 0.02
Body Surface Area (m2) 0.6 0.5 0.24 0.15 0.05 0.025 0.02 0.007
Km factor 20 20 12 12 8 6 5 3

Animal A (mg/kg) = Animal B (mg/kg) multiplied by Animal B Km
Animal A Km



For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) × mouse Km(3) = 11.2 mg/kg
rat Km(6)










Chemical Information

Download Zoledronic Acid SDF



Molecular Weight (MW) 272.09
Formula

C5H10N2O7P2

CAS No. 118072-93-8

Storage 3 years -20℃Powder
6 months-80℃in solvent (DMSO, water, etc.)
Synonyms Zoledronate, CGP-4244



Solubility (25°C) * In vitro DMSO 0.004 mg/mL (
Water <1 mg/mL (
Ethanol <1 mg/mL (
In vivo 30% PEG400/0.5% Tween80/5% propylene glycol 10 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.




Chemical Name Phosphonic acid, P,P'-[1-hydroxy-2-(1H-imidazol-1-yl)ethylidene]bis-







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