| 包装: | 100μg |
| 市场价: | 4322元 |
| 别名 | PcTx1; Psalmopoeus cambridgei toxin-1 |
| Canonical SMILES | CCC(C(/N=C(O)\C(/N=C(O)/C(/N=C(O)/C(N)CCC(O)=O)CC(O)=O)CSSCC1C(O)=NC(C(O)=NCC(O)=NC(C(O)=NC(C(O)=NC(/C(O)=N/C(/C(O)=N/C(/C(O)=N/C(/C(O)=N/C(/C(O)=N/C(/C(O)=N\C(/C(O)=N/C(/C(O)=N/C(/C(O)=N/C(/C(O)=N/2)C(C)C)CCC(O)=O)CC3=CC=CC=C3)CO)CCCNC(N)=N)CCCNC(N)=N)CC |
| 分子式 | C200H312N62O57S6 |
| 分子量 | 4689.39 |
| 溶解度 | Soluble to 2 mg/ml in Water |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
| 产品描述 | IC50: 0.9 nM Psalmotoxin 1 is a potent and selective acid-sensing ion channel 1a (ASIC1a) blocker. Several ASIC subunits described: ASIC1a, ASIC1b, ASIC2a, ASIC2b, and ASIC3 with different kinetics, tissue distribution, and external pH sensitivities. ASIC1a and ASIC1b both transform rapidly inactivating currents, following rapid and modestacidification of the external pH. In vitro: Psalmotoxin 1 (PcTx1) is the first potent and specific blocker of the ASIC1. PcTx1 has been successfully expressed to produce a spider toxin of the drosophila melanogaster S2 cell for the first time. Important structural elements involved in the binding of PcTx1 to ASIC1a channels was identified by surface characteristics of PcTx1. T [2]. To identify the binding site of PcTx1, an iodinated form of the toxin (125I-PcTx1YN) was produced, and a set of binding and electrophysiological experiments on several chimeras of ASIC1a and the PcTx1-insensitive channels ASIC1b and ASIC2a were developed. 125I-PcTx1YN binding specifically to ASIC1a at a single site (IC50 of 128 pM) distinct from the amiloride blocking site. Results obtained from chimeras indicate that PcTx1 binds principally on both cysteine-rich domains I and II (CRDI and CRDII) of the extracellular loop, rather than binding to ASIC1a transmembrane domains (M1 and M2) which involved in formation of the ion pore. The post-M1 and pre-M2 regions for the ability of PcTx1 to inhibit ASIC1a current are crucial, although not involved in the binding site. [3]. Psalmotoxin 1, a peptide isolated from the South American tarantula Psalmopoeus cambridgei, has very potent analgesic properties that inhibits thermal, mechanical, chemical, inflammatory and neuropathic pain in rodents. The blockade of acid-sensing ion channel 1a results in an activation of the endogenous encephalin pathway. [4]. In vivo: So far, no study in vivo has been conducted. Clinical trial: So far, no clinical study has been conducted. References: |
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