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Submit ReviewSNX 482 is a potent and selective, voltage-dependent R-type CaV2.3 calcium channel blocker (IC50 = 30 nM). Antinociceptive; inhibits nociceptive C-fibre and Aδ-fibre-evoked neuronal responses.
分子量 | 4495.01 |
公式 | C192H274N52O60S7 |
序列 |
GVDKAGCRYMFGGCSVNDDCCPRLGCHSLFSYCAWDLTFSD (Modifications: Disulfide bridge between 7 - 21, 14 - 26, 20 - 33) |
储存 | Desiccate at -20°C |
CAS Number | 203460-30-4 |
PubChem ID | 90488787 |
InChI Key | NSUPRLHDCFNOKD-UHFFFAOYSA-N |
Smiles | [H]NCC(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)NCC(=O)N[C@H]1CSSC[C@@H]2NC(=O)[C@@H]3CSSC[C@H](NC(=O)[C@H](CC4=CC=C(O)C=C4)NC(=O)[C@H](CO)NC(=O)[C@H](CC4=CC=CC=C4)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@H](CC4=CNC=N4)NC(=O)[C@H](CSSC[C@H](NC(=O)CNC(=O)CNC(=O)[C@H](CC4=CC=CC=C4)NC(=O)[C@H](CCSC)NC(=O)[C@H](CC4=CC=C(O)C=C4)NC(=O)[C@H](CCCNC(N)=N)NC1=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CC(O)=O)C(=O)N3)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@@H]1CCCN1C2=O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC1=CNC2=C1C=CC=C2)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CC1=CC=CC=C1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(O)=O)C(O)=O |
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Tocris products are intended for laboratory research use only, unless stated otherwise.
参考文献是支持产品生物活性的出版物。
Newcomb et al (1998) Selective peptide antagonist of the class E calcium channel from the venom of the Tarantula Hysterocrates gigas. Biochemistry 37 15353 PMID: 9799496
Bourinet et al (2001) Interaction of SNX482 with domains III and IV inhibits activation gating of α1E (CaV2.3) calcium channels. Biophys.J. 81 79 PMID: 11423396
Matthews et al (2007) The CaV2.3 calcium channel antagonist SNX-482 reduces dorsal horn neuronal responses in a rat model of chronic neuropathic pain. Eur.J.Neurosci. 25 3561 PMID: 17610575
关键词: SNX 482, SNX 482 supplier, Potent, selective, CaV23, blockers, R-type, Calcium, CaV, Channels, R-Type, voltage-gated, voltage-dependent, Ca2+, SNX482, venoms, Cav2.x, 2945, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 SNX 482 的部分引用包括:
Higley and Sabatini (2010) Competitive regulation of synaptic Ca2+ influx by D2 DA and A2A adenosine receptors. Nat Neurosci 13 958 PMID: 20601948
Smith et al (2018) Calcium Channel CaV2.3 Subunits Regulate Hepatic Glucose Production by Modulating Leptin-Induced Excitation of Arcuate Pro-opiomelanocortin Neurons. Cell Rep 25 278 PMID: 30304668
Pan et al (2014) σ-1 receptor antagonism restores injury-induced decrease of voltage-gated Ca2+ current in sensory neurons. Proc Natl Acad Sci U S A 350 290 PMID: 24891452
Hashiguchi (2017) Direct versus indirect actions of ghrelin on hypothalamic NPY neurons. PLoS One 12 e0184261 PMID: 28877214
Goswami et al (2012) Miniature IPSCs in hippocampal granule cells are triggered by voltage-gated Ca2+ channels via microdomain coupling. J Neurosci 32 14294 PMID: 23055500
Brennan et al (2013) Fetal calcium regulates branching morphogenesis in the developing human and mouse lung: involvement of voltage-gated calcium channels. PLoS One 8 e80294 PMID: 24282533
Grubb and Burrone (2010) Activity-dependent relocation of the axon initial segment fine-tunes neuronal excitability. J Pharmacol Exp Ther 465 1070 PMID: 20543823
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