Alendronate 121268-17-5

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Alendronate

Alendronate Chemical Structure

Molecular Weight: 326.13 Alendronate (Fosamax) is a farnesyl diphosphate synthase inhibitor with IC50 of 460 nM.


Biological Activity


Alendronate (Fosamax) is a farnesyl diphosphate synthase inhibitor with IC50 of 460 nM. It is a nitrogen-containing bisphosphate that acts as a robust inhibitor of bone resorption and induces Apoptosis in osteoclasts. It causes disruption of the ruffled border and actin cytoskeleton of osteoclasts and induces in vitro apoptosis of osteoclasts and macrophages by inhibiting farnesyl diphosphate synthase (IC50 = 460 nM). It efficiently chelates metal ions and functions as a broad-spectrum MMP Inhibitor (IC50 ~ 40 - 70 µM). And it also displays antimetastatic, anti-invasive and cell-adhesion-promoting properties (IC50 ~ 1 pM, in vitro invasion of prostate cancer cells).


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

Molecular Weight (MW)	326.13
Formula	C4H13NO7P2.3H2O.Na
CAS No.	121268-17-5

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

Solubility (25°C) *	In vitro	DMSO	<1 mg/mL (
		Water	<1 mg/mL (
		Ethanol	<1 mg/mL (

Chemical Name	P,P'-(4-amino-1-hydroxybutylidene)bis-phosphonic acid, sodium salt, hydrate (1:1:3)

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