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Clodronate sodium

Alias: clodronic acid disodium salt; Dichloromethylenediphosphonic acid disodium salt; Clodronate sodium; disodium dichloromethylene diphosphonate; Foreign brand names: Bonefos; Clasteon; Difosfonal; Loron; Mebonat; Ossiten. Code name: CL2MDP; DMDP.
Cat No.:V7106 Purity: ≥98%
Clodronic acid (Clodronate) disodium salt, a first-generation bisphosphonate, is an orally bioactive inhibitor of osteoclastic bone resorption.
Clodronate sodium
Clodronate sodium Chemical Structure CAS No.: 22560-50-5
Product category: New1
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
250mg
Other Sizes

Other Forms of Clodronate sodium:

  • Clodronate disodium tetrahydrate
  • Clodronic acid
Official Supplier of:
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Top Publications Citing lnvivochem Products
Product Description
Clodronic acid (Clodronate) disodium salt, a first-generation bisphosphonate, is an orally bioactive inhibitor of osteoclastic bone resorption. Clodronic acid disodium salt may be utilized in high bone turnover states, Paget's disease and osteolytic bone metastases.
Biological Activity I Assay Protocols (From Reference)
ln Vitro
Osteoclasts are induced to function swiftly by clodronate disodium salt, which blocks the absorption, internalization, and translocation of ADP into the mitochondria. Consequently, the inhibition of ATP generation causes the release of cytochrome C into the cytoplasm, which causes cellular fluorescence [2].
ln Vivo
At doses of 12.5 and 25 mg/kg, clodronate disodium salt (6.25–25 mg/kg; lateral; once daily for 28 days) somewhat reduced hindlimb edema [3].
Animal Protocol
Animal/Disease Models: Male Lewis rat, 7 years of age [3]
Doses: 6.25, 12.5, and 25 mg/kg
Route of Administration: Oral; one time/day for 28 days
Experimental Results: 25 mg/kg on days 21 and 28 Hind paw swelling was Dramatically less in the adjuvant arthritis (AA) control group (87% and 88% of the AA control group, respectively) and on day 28 in the 12.5 mg/kg dose group.
References

[1]. Clodronate (dichloromethylene bisphosphonate) inhibits LPS-stimulated IL-6 and TNF production by RAW 264 cells. Life Sci. 1994;54(14):PL229‐PL234.

[2]. Clodronic acid in the treatment of postmenopausal osteoporosis. Clin Drug Investig. 2007;27(6):419‐433.

[3]. Effects of clodronate and alendronate on local and systemic changes in bone metabolism in rats with adjuvant arthritis. Inflammation. 2004;28(1):15‐21.

Additional Infomation
Clodronic acid disodium salt is the disodium salt of clodronic acid. It inhibits bone resorption and soft tissue calcification, and is used (generally as the tetrahydrate) as an adjunct in the treatment of severe hypercalcaemia associated with malignancy, and in the management of osteolytic lesions and bone pain associated with skeletal metastases. It has a role as a bone density conservation agent. It is an organic sodium salt and a one-carbon compound. It contains a clondronate(2-).
Clodronate Disodium is the disodium salt of a nitrogen-free bisphosphonate analog of naturally occurring pyrophosphate. Clodronate binds to calcium and inhibits osteoclastic bone resorption and hydroxyapatite crystal formation and dissolution, resulting in a reduction of bone turnover. This agent may control malignancy-associated hypercalcemia, inhibit osteolytic bone metastasis and decrease pain.
A diphosphonate which affects calcium metabolism. It inhibits bone resorption and soft tissue calcification.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
CH2CL2NA2O6P2
Molecular Weight
288.86
Exact Mass
287.849
CAS #
22560-50-5
Related CAS #
Clodronate disodium tetrahydrate;88416-50-6;Clodronic acid;10596-23-3
PubChem CID
31195
Appearance
White to off-white solid powder
Density
2.306g/cm3
Boiling Point
474.7ºC at 760mmHg
Melting Point
>330ºC
Flash Point
240.9ºC
Vapour Pressure
2.55E-10mmHg at 25°C
LogP
1.307
Hydrogen Bond Donor Count
2
Hydrogen Bond Acceptor Count
6
Rotatable Bond Count
2
Heavy Atom Count
13
Complexity
206
Defined Atom Stereocenter Count
0
InChi Key
HJKBJIYDJLVSAO-UHFFFAOYSA-L
InChi Code
InChI=1S/CH4Cl2O6P2.2Na/c2-1(3,10(4,5)6)11(7,8)9;;/h(H2,4,5,6)(H2,7,8,9);;/q;2*+1/p-2
Chemical Name
disodium;[dichloro-[hydroxy(oxido)phosphoryl]methyl]-hydroxyphosphinate
Synonyms
clodronic acid disodium salt; Dichloromethylenediphosphonic acid disodium salt; Clodronate sodium; disodium dichloromethylene diphosphonate; Foreign brand names: Bonefos; Clasteon; Difosfonal; Loron; Mebonat; Ossiten. Code name: CL2MDP; DMDP.
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.
Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
H2O : ~100 mg/mL (~346.19 mM)
DMSO :< 1 mg/mL
Solubility (In Vivo)
Solubility in Formulation 1: 100 mg/mL (346.19 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 3.4619 mL 17.3094 mL 34.6188 mL
5 mM 0.6924 mL 3.4619 mL 6.9238 mL
10 mM 0.3462 mL 1.7309 mL 3.4619 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

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What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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g/mol

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

Clinical Trial Information
S0307 Phase III Trial of Bisphosphonates as Adjuvant Therapy for Primary Breast Cancer.
CTID: NCT00127205
Phase: Phase 3    Status: Completed
Date: 2021-07-02
Combination Chemotherapy in Treating Pain in Hormone Refractory Metastatic Prostate Cancer
CTID: NCT00003232
Phase: Phase 3    Status: Completed
Date: 2020-04-03
S0307A, Long-Term Bone Quality in Women With Breast Cancer Enrolled on Clinical Trial SWOG-S0307
CTID: NCT00873808
Phase:    Status: Withdrawn
Date: 2013-04-10
Bonefos and the Consumption of Analgesics
CTID: NCT00909142
Phase:    Status: Completed
Date: 2012-04-06
Effects of Continuous Combined Hormone Replacement Therapy and Clodronate
Multicenter, randomized, parallel group open study to compare, in patients with postmenopausal osteoporosis, the effects of clodronate (Difosfonal) administered either intramuscularly at a dose of 100 mg 1 weekly, intramuscularly at a dose of 200 mg once every 2 weeks or orally at a dose of 800 mg daily (400 mg x 2), on BMD and markers of bone metabolism.
CTID: null
Phase: Phase 3    Status: Prematurely Ended
Date: 2010-05-10
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Bisfosfonatbehandling av bentransplantat vid höftrevisionhöftplastikrevision utvärderat med radiostereofotogrametri. En randomiserad, dubbel-blind studie hos patienter opererade för osteolys och aseptisk lossning.
CTID: null
Phase: Phase 2    Status: Completed
Date: 2007-04-25

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