1309601-26-0
Chemical Structure
TROX-1
- CAS No.: 1309601-26-0
- Formula:C22H16ClFN6O
- Molecular Weight:434.85
IUPAC Name: (R)-5-(3-chloro-4-fluorophenyl)-3-methyl-3-(pyrimidin-5-ylmethyl)-1-(1H-1,2,4-triazol-3-yl)indolin-2-one
InChIKey: OABSWPUPIHULMQ-JOCHJYFZSA-N
SMILES: O=C1N(C2=C([C@]1(CC3=CN=CN=C3)C)C=C(C=C2)C4=CC=C(C(Cl)=C4)F)C5=NNC=N5
Biological Activity: TROX-1 is a selective, orally active and brain-penetrant N-type calcium channel (Cav2.2) inhibitor with an IC50 value of 0.11 μM. TROX-1 exerts state-dependent and use-dependent inhibition, preferentially targets open/inactivated channels, blocks depolarization-associated calcium influx, and fully blocks calcium influx in rat dorsal root ganglion neurons. TROX-1 reverses inflammatory-induced hyperalgesia, nerve injury-induced allodynia. TROX-1 can be used for the research of pain[1][2].
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TROX-1 | 99.55% | TROX-1 is a selective, orally active and brain-penetrant N-type calcium channel (Cav2.2) inhibitor with an IC50 value of 0.11 μM. TROX-1 exerts state-dependent and use-dependent inhibition, preferentially targets open/inactivated channels, blocks depolarization-associated calcium influx, and fully blocks calcium influx in rat dorsal root ganglion neurons. TROX-1 reverses inflammatory-induced hyperalgesia, nerve injury-induced allodynia. TROX-1 can be used for the research of pain. | ||||||||||||||||||||
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- [1]. Swensen AM, et al. Characterization of the substituted N-triazole oxindole TROX-1, a small-molecule, state-dependent inhibitor of Ca(V)2 calcium channels. Mol Pharmacol. 2012;81(3):488-497. [Content Brief]
- [2]. Abbadie C, et al. Analgesic effects of a substituted N-triazole oxindole (TROX-1), a state-dependent, voltage-gated calcium channel 2 blocker. J Pharmacol Exp Ther. 2010;334(2):545-555. [Content Brief]
Keywords
