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商品详细Smartox/N型钙通道选择性阻滞剂/08CON013-00100/0.1mg
Smartox/N型钙通道选择性阻滞剂/08CON013-00100/0.1mg
Smartox/N型钙通道选择性阻滞剂/08CON013-00100/0.1mg
商品编号: 08CON013-00100
品牌: smartox-biotech
市场价: ¥2496.00
美元价: 1920.00
产地: 美国(厂家直采)
公司:
产品分类: 酸碱缓冲液
公司分类: acid_base_buffer_solution
联系Q Q: 3392242852
电话号码: 4000-520-616
电子邮箱: info@ebiomall.com
商品介绍

ω-conotoxin SO-3 is a selective blocker of N-type voltage-sensitive calcium channels. EC50 for ω-conotoxin SO-3 is 0.16 µM (similar to ω-conotoxin MVIIA) on HVA calcium currents. ω-conotoxin SO-3 did not show any inhibiting effects on L-type, P/Q-type and R-type currents at 3 µM concentration. ω-conotoxin SO-3 has no effect on voltage-sensitive sodium currents, delayed rectifier potassium currents and transient outward potassium currents. At 3 µM, the inhibition amounts of HVA ICa was very similar between ω-conotoxin SO-3 and ω-conotoxin MVIIA (~ 32%). Their inhibitory effects are almost fully reversible but their half-time for recovery are different (~ 7.5 min for ω-conotoxin SO-3 and  ~ 4.14 min for ω-conotoxin MVIIA). ω-conotoxin SO-3 displays an analgesic potency similar to ω-conotoxin MVIIA in a range of acute and chronic pain models in rodents, but has less adverse effects compared with identical dosages of ω-conotoxin MVIIAinjected intrathecally.


Description:

Product code: 08CON013. Categories: Calcium channels, High voltage-gated Ca2+ channels. Tags: Cav2.2, N-type.

AA sequence: Cys1-Lys-Ala-Ala-Gly-Lys-Pro-Cys8-Ser-Arg-Ile-Ala-Tyr-Asn-Cys15-Cys16-Thr-Gly-Ser-Cys20-Arg-Ser-Gly-Lys-Cys25-NH2
Disulfide bonds: Cys1-Cys16, Cys8-Cys20 and Cys15-Cys25
Length (aa): 25
Formula: C100H166N36O31S6
Molecular Weight: 2561.00 Da
Appearance: White lyophilized solid
Solubility: water and saline buffer
CAS number:
Source: Synthetic
Purity rate: > 97 %

Reference:

SO-3, a new O-superfamily conopeptide derived from Conus striatus, selectively inhibits N-type calcium currents in cultured hippocampal neurons
Whole-cell currents in cultured hippocampal neurons were recorded to investigate the effects of SO-3, a new O-superfamily conopeptide derived from Conus striatus, on voltage-sensitive channels. SO-3 had no effect on voltage-sensitive sodium currents, delayed rectifier potassium currents, and transient outward potassium currents. Similar to the selective N-type calcium channel blocker omega-conotoxin MVIIA (MVIIA), SO-3 could concentration-dependently inhibit the high voltage-activated (HVA) calcium currents (I(Ca)). MVIIA(3 microM), 10 microM nimodipine, and 0.5 microM omega-agatoxin IVA (Aga) could selectively block the N-, L-, and P/Q-type I(Ca), which contributed approximately 32, approximately 38, and approximately 21% of the HVA currents in hippocampal neurons, respectively. About 31% of the total HVA currents were inhibited by 3 microM SO-3. SO-3 (3 microM) and 3 microM MVIIA inhibited the overlapping components of HVA currents, whereas no overlapping component was inhibited by 3 microM SO-3 and 10 microM nimodipine, or by 3 microM SO-3 and 0.5 microM Aga. Also, 3 microM SO-3 had no effect on R-type currents. SO-3 had less inhibitory effects on non-N-type HVA currents than MVIIA at higher concentrations (30 and 100 microM). The inhibitory effects of SO-3 and MVIIA on HVA currents were almost fully reversible. However, the recovery from block by MVIIA was more rapid than recovery from block by SO-3. It is concluded that SO-3 is a new omega-conotoxin selectively targeting N-type voltage-sensitive calcium channels. Considering the significance of N-type calcium channels for pain transduction, SO-3 may have therapeutic potential as a novel analgesic agent.

Wen, L., et al. (2005) SO-3, a new O-superfamily conopeptide derived from Conus striatus, selectively inhibits N-type calcium currents in cultured hippocampal neurons, Br J Pharmacol. PMID: 15880145
Effect of new O-superfamily conotoxin SO3 on sodium and potassium currents of cultured hippocampal neurons
The effects of a new O-superfamily conotoxin SO3 on sodium and potassium currents were examined in cultured rat hippocampal neurons using the whole-cell patch clamp technique. SO3 caused a concentration-dependent, rapidly developing and reversible inhibition of sodium currents (I(Na)). The IC(50) value for the blockage of I(Na) was calculated to be 0.49 and the Hill coefficient was 1.7. Using electrophysiological and pharmacological protocols, transient A-type potassium currents (I(A)) and delayed rectifiers potassium currents (I(K)) were isolated. SO3 caused a concentration-dependent, and reversible inhibition of I(K). The IC(50) value for the blockage of I(K) was calculated to be 1.6 and the Hill coefficient was 0.6, with no significant effect on I(A). These results indicate that SO3 can selectively inhibit neuronal sodium and potassium currents.Li, Z., et al. (2003) Effect of new O-superfamily conotoxin SO3 on sodium and potassium currents of cultured hippocampal neurons, Brain Res. PMID: 12591132
品牌介绍
Smartox Biotechnology 是全球唯一一家专门生产动物毒液多肽毒素,用于细胞离子通道功能研究的生物医药公司。多肽毒素在生物制药领域具有重要的使用价值。Smartox Biotechnology 于 2009 年由来自 Grenoble 神经科学研究所 (Grenoble Institute of Neuroscience) 的 Michel de waard 博士创立, Smartox Biotechnology 专门研究动物毒液,制作合成多种毒液中的多肽成分(常称为毒素)。 De Waard 博士研究离子通道与毒素多肽的关系,尤其是鉴定、开发毒素多肽作为治疗性分子或细胞穿透肽 (cell penetrating peptides, CPP) 。其研究团队在毒液分离,药理性活性肽鉴定、富半胱氨酸肽定性、制作和优化等方面具有独特、丰富的经验。 2010 年, Smartox Biotechnolgy 被法国研究部 (Ministry of Research) 授予“新兴企业 OSEO 奖 (OSEO prize for emerging businesses) ”。