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TROX-1

Cat. No. M42166
TROX-1 Structure
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Biological Activity

TROX-1 is an N-type calcium channel (CaV2.2) inhibitor with an IC50 value of 0.11 μM.

Chemical Information
Molecular Weight 434.85
Formula C22H16ClFN6O
CAS Number 1309601-26-0
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

References

[1] W Rahman et al. Neuroscience. Electrophysiological evidence for voltage-gated calcium channel 2 (Cav2) modulation of mechano- and thermosensitive spinal neuronal responses in a rat model of osteoarthritis

[2] R Patel et al. Neuroscience. Electrophysiological characterization of activation state-dependent Ca(v)2 channel antagonist TROX-1 in spinal nerve injured rats

[3] Andrew M Swensen et al. Mol Pharmacol. Characterization of the substituted N-triazole oxindole TROX-1, a small-molecule, state-dependent inhibitor of Ca(V)2 calcium channels

[4] Catherine Abbadie et al. J Pharmacol Exp Ther. Analgesic effects of a substituted N-triazole oxindole (TROX-1), a state-dependent, voltage-gated calcium channel 2 blocker

[5] Deborah Gater et al. IDrugs. American Chemical Society--238th National Meeting & Exposition. Developments in medicinal chemistry: part 1. 16-20 August 2009, Washington DC, USA

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  Catalog
Abmole Inhibitor Catalog




Keywords: TROX-1 supplier, Calcium Channel, inhibitors, activators


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