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TILUDRONIC ACID, DISODIUM SALT

Product Name
TILUDRONIC ACID, DISODIUM SALT
CAS No.
149845-07-8
Chemical Name
TILUDRONIC ACID, DISODIUM SALT
Synonyms
SKELID;SR-41319B;SR 41319G;Unii-bh6m93cia0;Tiludrote disodium;DisodiuM Tiludronate;DisodiumTiludronate>TILUDRONIC ACID, DISODIUM SALT;Disodium (4-chlorophenylthio)methylenediphosphonate;(((4-chlorophenyl)thio)methylene)diphosphonic acid, sodium salt
CBNumber
CB9288177
Molecular Formula
C7H10ClNaO6P2S
Formula Weight
342.6
MOL File
149845-07-8.mol
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TILUDRONIC ACID, DISODIUM SALT Property

Melting point:
>300°C
storage temp. 
-20°C Freezer
solubility 
Methanol (Slightly), Water (Slightly)
form 
Solid
color 
White to Off-White
Merck 
14,9441
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Safety

HS Code 
2931.39.0030
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Danger
Hazard statements

H302Harmful if swallowed

H318Causes serious eye damage

Precautionary statements

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P310Immediately call a POISON CENTER or doctor/physician.

P330Rinse mouth.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

TCI Chemical
Product number
D4167
Product name
Disodium Tiludronate
Purity
>98.0%(HPLC)
Packaging
25mg
Price
$290
Updated
2024/03/01
TRC
Product number
T441250
Product name
TiludronicAcidDisodiumSalt
Packaging
250mg
Price
$400
Updated
2021/12/16
Usbiological
Product number
T5468
Product name
Tiludronic Acid, Disodium Salt
Packaging
100mg
Price
$432
Updated
2021/12/16
Biosynth Carbosynth
Product number
FT28278
Product name
Tiludronic acid disodium salt
Packaging
250mg
Price
$625
Updated
2021/12/16
American Custom Chemicals Corporation
Product number
API0004187
Product name
TILUDRONIC ACID DISODIUM SALT
Purity
95.00%
Packaging
100MG
Price
$727.65
Updated
2021/12/16
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TILUDRONIC ACID, DISODIUM SALT Chemical Properties,Usage,Production

Description

Tiludronate disodium, the first of the third generation of bisphosphonates, was introduced to the market in Switzerland for the treatment of Paget‘s disease. Bisphosphonates have high affinity for bone. When given orally, they are not metabolized but are absorbed, stored, preferentially localized to the skeleton where they inhibit bone resorption and therefore are useful in the treatment of diseases of high bone turnover such as Paget’s disease and hypercalcemia of malignancy. Mechanistically, tiludronate disodium is suggested to be a specific inhibitor of functioning osteoclasts through selective incorporation into the polarized osteoclastlike multinucleated cells and direct interference with the maintenance of the cytoskeletal structure. Tiludronate disodium is reportedly in clinical trials for osteoporosis in post-menopausal women.

Chemical Properties

Fine White to Off-White Crystalline Powder

Originator

Sanofi (France)

Uses

A biphosphonate bone resorption inhibitor.

Manufacturing Process

The 50% strength suspension of sodium hydride in oil is added, a little at a time to a solution of tetraisopropyl methylene-diphosphonate in dimethylformamide. After all has been added, the mixture is stirred, the 1-(4- chlorphenyl) disulfide is then added and the whole is heated at 25°C for 6 h. The mixture is evaporated to dryness in vacuo and residue is taken up in hexane. The solution is washed with water and dried. The solvent is evaporated to dryness and the residue is chromatographed on silica column, elution being carried out with a 98:2 (v/v) mixture of methylene chloride/methanol. The obtained 1-(4-chlorphenylthio)tetraisopropyl methylene-diphosphonate is then hydrolyzed with 12 N HCl for 18 h to give the 1-(4-chlorphenylthio)methylene-diphosphonic acid.
The 1-(4-chlorphenylthio)methylene-diphosphonic acid are dissolved in water, containing sodium hydroxide. The solution is filtered, the methanol are then added and the mixture is left to crystallize. The precipitate is filtered off and washed with methanol and dried at 80°C in vacuo and the disodium salt of 1- (4-chlorphenylthio)methylene-diphosphonic acid is thus obtained.

brand name

Skelid

Therapeutic Function

Bone calcium regulator

Biological Activity

Tiludronate (Tiludronic Acid) disodium is an orally active bisphosphonate that acts as a bone modulating agent. Tiludronate disodium for the study of metabolic bone diseases. Tiludronate disodium is a potent inhibitor of osteoclast vacuolar H(+)-ATPase.

in vitro

The ability of Tiludronate to inhibit proton transport is 5-fold higher in kidney-derived vesicles (IC 50 =1.1 mM) and 10,000-fold higher in vesicles derived from osteoclasts (IC 50 =466 nM). Tiludronate also potently inhibits proton transport in yeast microsomal preparations (IC 50 =3.5 microM) and inhibits the activity of purified yeast V-ATPase. The inhibition of the osteoclast V-ATPase-mediated proton transport by Tiludronate is rapid, pH-dependent, and reversible.

in vivo

Tiludronate exerts a dose-dependent inhibitory activity on bone resorption. Tiludronate could act on mature osteoclasts by reducing their capacity to secrete proton into the resorption space and also by favoring their detachment from the bone matrix. Tiludronate is also tested in other models of osteoporosis. In the castrated male rat model, Tiludronate (5-200 mg/kg; p.o.) prevents the decrease in the skeletal mass, assessed physically by measuring the bone weight and density or chemically by determining the calcium and phosphate content.

TILUDRONIC ACID, DISODIUM SALT Preparation Products And Raw materials

Raw materials

Preparation Products

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149845-07-8, TILUDRONIC ACID, DISODIUM SALTRelated Search:


  • Disodium (4-chlorophenylthio)methylenediphosphonate
  • SR-41319B
  • SKELID
  • TILUDRONIC ACID, DISODIUM SALT
  • [[(4-CHLOROPHENYL)THIO]METHYLENE]BIPHOSPHONIC ACID, DISODIUM SALT
  • [[(4-Chlorophenyl)thio]methylene]biphosphonicAcid,DisodiumSalt,SR-41319B,Skelid
  • Unii-bh6m93cia0
  • DisodiuM Tiludronate
  • SR 41319G
  • DisodiumTiludronate&gt
  • Tiludrote disodium
  • Disodium [[(4-Chlorophenyl)thio]methylene]bis(hydrogenphosphonate)
  • (((4-chlorophenyl)thio)methylene)diphosphonic acid, sodium salt
  • 149845-07-8
  • C7H7ClNa2O6P2S
  • Intermediates & Fine Chemicals
  • Pharmaceuticals
  • Phosphorylating and Phosphitylating Agents