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| | L-Cysteinamide, L-cysteinyl-L-lysylglycyl-L-lysylglycyl-L-alanyl-L-lysyl-L-cysteinyl-L-seryl-L-arginyl-L-leucyl-L-methionyl-L-tyrosyl-L-α-aspartyl-L-cysteinyl-L-cysteinyl-L-threonylglycyl-L-seryl-L-cysteinyl-L-arginyl-L-serylglycyl-L-lysyl-, cyclic (1→16),(8→20),(15→25)-tris(disulfide), 2,2,2-trifluoroacetate (1:?) Basic information |
| Product Name: | L-Cysteinamide, L-cysteinyl-L-lysylglycyl-L-lysylglycyl-L-alanyl-L-lysyl-L-cysteinyl-L-seryl-L-arginyl-L-leucyl-L-methionyl-L-tyrosyl-L-α-aspartyl-L-cysteinyl-L-cysteinyl-L-threonylglycyl-L-seryl-L-cysteinyl-L-arginyl-L-serylglycyl-L-lysyl-, cyclic (1→16),(8→20),(15→25)-tris(disulfide), 2,2,2-trifluoroacetate (1:?) | | Synonyms: | L-Cysteinamide, L-cysteinyl-L-lysylglycyl-L-lysylglycyl-L-alanyl-L-lysyl-L-cysteinyl-L-seryl-L-arginyl-L-leucyl-L-methionyl-L-tyrosyl-L-α-aspartyl-L-cysteinyl-L-cysteinyl-L-threonylglycyl-L-seryl-L-cysteinyl-L-arginyl-L-serylglycyl-L-lysyl-, cyclic (1→16),(8→20),(15→25)-tris(disulfide), 2,2,2-trifluoroacetate (1:);L-cysteinyl-L-lysylglycyl-L-lysylglycyl-L-alanyl-L-lysyl-L-cysteinyl-L-seryl-L-arginyl-L-leucyl-L-methionyl-L-tyrosyl-L-α-aspartyl-L-cysteinyl-L-cysteinyl-L-threonylglycyl-L-seryl-L-cysteinyl-L-arginyl-L-serylglycyl-L-lysyl-L-cysteinamide,cyclic(1→16),(8→20),(15→25)-tris(disulfide),trifluoroacetatesalt | | CAS: | 1660960-77-9 | | MF: | C104H173F3N36O34S7 | | MW: | 2753.16 | | EINECS: | | | Product Categories: | | | Mol File: | 1660960-77-9.mol |  |
| | L-Cysteinamide, L-cysteinyl-L-lysylglycyl-L-lysylglycyl-L-alanyl-L-lysyl-L-cysteinyl-L-seryl-L-arginyl-L-leucyl-L-methionyl-L-tyrosyl-L-α-aspartyl-L-cysteinyl-L-cysteinyl-L-threonylglycyl-L-seryl-L-cysteinyl-L-arginyl-L-serylglycyl-L-lysyl-, cyclic (1→16),(8→20),(15→25)-tris(disulfide), 2,2,2-trifluoroacetate (1:?) Chemical Properties |
| solubility | Water: 1 mg/ml | | form | A lyophilized powder |
| | L-Cysteinamide, L-cysteinyl-L-lysylglycyl-L-lysylglycyl-L-alanyl-L-lysyl-L-cysteinyl-L-seryl-L-arginyl-L-leucyl-L-methionyl-L-tyrosyl-L-α-aspartyl-L-cysteinyl-L-cysteinyl-L-threonylglycyl-L-seryl-L-cysteinyl-L-arginyl-L-serylglycyl-L-lysyl-, cyclic (1→16),(8→20),(15→25)-tris(disulfide), 2,2,2-trifluoroacetate (1:?) Usage And Synthesis |
| Description | Ziconotide is a synthetic version of ω-conopeptide MVIIA, a peptide toxin originally found in the venom of the fish-eating marine snail C. magus, that blocks N-type calcium channels in rat brain membranes (Kds = 1.1-18 pM; IC50s = 2-55 pM).1,2 It blocks high-voltage-activated calcium currents in rat superior cervical ganglion neurons (IC50 = 32 nM) as well as depolarization-induced norepinephrine release by rat peripheral sympathetic efferent neurons and in rat hippocampus (IC50s = 1.2 and 5.5 nM, respectively).1 Intrathecal administration of ziconotide inhibits formalin-induced flinch responses and increases the paw withdrawal threshold in the paw pressure test in rats (ED50s = 0.11 and 0.60 μg, respectively), indicating antinociceptive effects.3 It decreases latency to tail withdrawal in a hot plate test in a rat model of sciatic chronic constriction injury.1 Ziconotide also reduces infarct volume post ischemia in a rat model of transient focal ischemia.4 | | References | 1. McGivern, J.G. Ziconotide: A review of its pharmacology and use in the treatment of pain Neurophyschiatr. Dis. Treat. 3(1),69-85(2007). 2. Olivera, B.M., Cruz, L.J., de Santos, V., et al. Neuronal calcium channel antagonists. Discrimination between calcium channel subtypes using ω-conotoxin from Conus magus venom Biochemistry 26(8),2086-2090(1987). 3. Wang, Y.X., Gao, D., Pettus, M., et al. Interactions of intrathecally administered ziconotide, a selective blocker of neuronal N-type voltage-sensitive calcium channels, with morphine on nociception in rats Pain 84(2-3),271-281(2000). 4. Zhao, Q., Smith, M.L., and Siesj, B.K. The omega-conopeptide SNX-111, an N-type calcium channel blocker, dramatically ameliorates brain damage due to transient focal ischaemia Acta. Physiol. Scand. 150(4),459-461(1994). |
| | L-Cysteinamide, L-cysteinyl-L-lysylglycyl-L-lysylglycyl-L-alanyl-L-lysyl-L-cysteinyl-L-seryl-L-arginyl-L-leucyl-L-methionyl-L-tyrosyl-L-α-aspartyl-L-cysteinyl-L-cysteinyl-L-threonylglycyl-L-seryl-L-cysteinyl-L-arginyl-L-serylglycyl-L-lysyl-, cyclic (1→16),(8→20),(15→25)-tris(disulfide), 2,2,2-trifluoroacetate (1:?) Preparation Products And Raw materials |
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