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Clodronate disodium tetrahydrate

Names

[ CAS No. ]:
88416-50-6

[ Name ]:
Clodronate disodium tetrahydrate

[Synonym ]:
Sodium (dichloromethylene)bis[hydrogen (phosphonate)] hydrate (2:1:4)
Phosphonic acid, (dichloromethylene)bis-, sodium salt, hydrate (1:2:4)
Disodium clodronate tetrahydrate
clodronate disodium tetrahydrate
Clodronate Disodium

Biological Activity

[Description]:

Clodronate disodium tetrahydrate (Disodium clodronate tetrahydrate) is first-generation bisphosphonate, with anti-osteoporotic, anti-inflammatory and analgesic effects. Clodronate disodium tetrahydrate is a selective, potent, reversible and Cl- competitive vesicular nucleotide transporter (VNUT) inhibitor, with an IC50 of 15.6 nM. Clodronate disodium tetrahydrate inhibits vesicular ATP release from neurons and reduces chronic neuropathic and inflammatory pain[1][2].

[Related Catalog]:

Signaling Pathways >> Others >> Others
Research Areas >> Inflammation/Immunology
Research Areas >> Neurological Disease

[Target]

vesicular ATP release[1]


[In Vitro]

Clodronate disodium tetrahydrate, a first-generation bisphosphonate, significantly attenuates neuropathic and inflammatory pain unrelated to bone abnormalities via inhibition of VNUT, a key molecule for the initiation of purinergic chemical transmission [1]. Clodronate disodium tetrahydrate is an allosteric modulator of VNUT Cl- dependence [1]. Clodronate disodium tetrahydrate acts as antiresorptive in osteoporosis[2].

[In Vivo]

Clodronate disodium tetrahydrate (10 mg/kg; i.v.) attenuates inflammatory pain via VNUT inhibition[1]. Clodronate disodium tetrahydrate attenuates inflammation via VNUT inhibition [1]. Animal Model: C57BL/6 mice (22-30 g)[1] Dosage: 10 mg/kg Administration: Intravenous injection Result: Attenuated carrageenan- or complete Freund’s adjuvant (CFA)-evoked inflammatory pain.

[References]

[1]. Kato Y, et al. Identification of a vesicular ATP release inhibitor for the treatment of neuropathic and inflammatory pain. Proc Natl Acad Sci U S A. 2017 Aug 1;114(31):E6297-E6305.

[2]. Moriyama Y, et al. Clodronate: A Vesicular ATP Release Blocker. Trends Pharmacol Sci. 2018 Jan;39(1):13-23.

Chemical & Physical Properties

[ Molecular Formula ]:
CH12Cl2Na2O10P2

[ Molecular Weight ]:
360.917

[ Exact Mass ]:
359.892151

[ PSA ]:
177.26000

[ LogP ]:
1.04990

Related Compounds