Bioactivity | 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]. |
Target | vesicular ATP release |
Invitro | 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: |
Name | Clodronate disodium tetrahydrate |
CAS | 88416-50-6 |
Formula | CH12Cl2Na2O10P2 |
Molar Mass | 362.93 |
Appearance | Solid |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
Reference | [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. |