Smartox/Discriminates between α9α10 and α7 nAChRs/13CON017-50100/5x0.1mg,Smartox,,Smartox,smartox-biotech,+,,Array.Array.Array蚂蚁淘厂家直采.

产品名称：Smartox/Discriminates between α9α10 and α7 nAChRs/13CON017-50100/5x0.1mg

产品编号：13CON017-50100

市场价：¥2620.80

场地：美国(厂家直采)

产品分类：生化试剂>缓冲液>酸碱缓冲液>

联系QQ：1570468124

电话号码：4000-520-616

邮箱： info@ebiomall.com

美元价：$252.00

品牌： Smartox

公司：Smartox

公司分类：

商品介绍

α-conotoxin PeIA is a conotoxin that has been isolated from the venom of Conus pergrandis. α-conotoxin PeIA discriminates between α9α10 and α7 nicotinic acetylcholine receptors (AChRs) with IC₅₀ values of 7-50 nM (depending of the authors) and 1.8 µM, respectively. The toxin is also known to block α3β2 nicotinic AChRs (with an IC₅₀ of 97 nM) and block voltage-gated N-type Ca²⁺ channels in rat DRG neurons with an IC₅₀ of 1.1 nM. No significant inhibition of ACh-evoked currents for nicotinic α4β2 and muscle αβγδ AChRs by 1 µM α-conotoxin PeIA was observed. The action of α-conotoxin PeIA is fully reversible after washout of the peptide in the extracellular medium.

Description:

Product code: 13CON017. Category: Nicotinic Acetylcholine Receptor. Tags: bungarotoxin, nachr, nicotinic.

AA sequence: Gly-Cys²-Cys³-Ser-His-Pro-Ala-Cys⁸-Ser-Val-Asn-His-Pro-Glu-Leu-Cys¹⁶-NH₂ Disulfide bonds: Cys²-Cys⁸, Cys³-Cys¹⁶
Length (aa): 16
Formula: C₆₅H₉₈N₂₂O₂₁S₄
Molecular Weight: 1651.9 Da
Appearance: White lyophilized solid
Solubility: water or saline buffer
CAS number: not available
Source: Synthetic
Purity rate: > 99 %

Reference:

Structure and Activity of α-Conotoxin PeIA at Nicotinic Acetylcholine Receptor Subtypes and GABAB Receptor-coupled N-type Calcium Channels

α-Conotoxins are peptides from cone snails that target the nicotinic acetylcholine receptor (nAChR). RgIA and Vc1.1 have analgesic activity in animal pain models. Both peptides target the α9α10 nAChR and inhibit N-type calcium channels via GABA(B) receptor activation, but the mechanism of action of analgesic activity is unknown. PeIA has previously been shown to inhibit the α9α10 and α3β2 nAChRs. In this study, we have determined the structure of PeIA and shown that it is also a potent inhibitor of N-type calcium channels via GABA(B) receptor activation. The characteristic α-conotoxin fold is present in PeIA, but it has a different distribution of surface-exposed hydrophobic and charged residues compared with Vc1.1. Thus, the surface residue distribution, rather than the overall fold, appears to be responsible for the 50-fold increase in selectivity at the α3β2 nAChR by PeIA relative to Vc1.1. In contrast to their difference in potency at the nAChR, the equipotent activity of PeIA and Vc1.1 at the GABA(B) receptor suggests that the GABA(B) receptor is more tolerant to changes in surface residues than is the nAChR. The conserved Asp-Pro-Arg motif of Vc1.1 and RgIA, which is crucial for potency at the α9α10 nAChR, is not required for activity at GABA(B) receptor/N-type calcium channels because PeIA has a His-Pro-Ala motif in the equivalent position. This study shows that different structure-activity relationships are associated with the targeting of the GABA(B) receptor versus nAChRs. Furthermore, there is probably a much more diverse range of conotoxins that target the GABA(B) receptor than currently realized.

Day N., et al. (2011) Structure and Activity of α-Conotoxin PeIA at Nicotinic Acetylcholine Receptor Subtypes and GABAB Receptor-coupled N-type Calcium Channels. JBC. PMID: 21252227

A novel α-conotoxin, PeIA, cloned from Conus Pergrandis, discriminates between rat α9α10 and α7 nicotinic cholinergic receptor

The alpha9 and alpha10 nicotinic cholinergic subunits assemble to form the receptor believed to mediate synaptic transmission between efferent olivocochlear fibers and hair cells of the cochlea, one of the few examples of postsynaptic function for a non-muscle nicotinic acetylcholine receptor (nAChR). However, it has been suggested that the expression profile of alpha9 and alpha10 overlaps with that of alpha7 in the cochlea and in sites such as dorsal root ganglion neurons, peripheral blood lymphocytes, developing thymocytes, and skin. We now report the cloning, total synthesis, and characterization of a novel toxin alpha-conotoxin PeIA that discriminates between alpha9alpha10 and alpha7 nAChRs. This is the first toxin to be identified from Conus pergrandis, a species found in deep waters of the Western Pacific. Alpha-conotoxin PeIA displayed a 260-fold higher selectivity for alpha-bungarotoxin-sensitive alpha9alpha10 nAChRs compared with alpha-bungarotoxin-sensitive alpha7 receptors. The IC50 of the toxin was 6.9 +/- 0.5 nM and 4.4 +/- 0.5 nM for recombinant alpha9alpha10 and wild-type hair cell nAChRs, respectively. Alpha-conotoxin PeIA bears high resemblance to alpha-conotoxins MII and GIC isolated from Conus magus and Conus geographus, respectively. However, neither alpha-conotoxin MII nor alpha-conotoxin GIC at concentrations of 10 microM blocked acetylcholine responses elicited in Xenopus oocytes injected with the alpha9 and alpha10 subunits. Among neuronal non-alpha-bungarotoxin-sensitive receptors, alpha-conotoxin PeIA was also active at alpha3beta2 receptors and chimeric alpha6/alpha3beta2beta3 receptors. Alpha-conotoxin PeIA represents a novel probe to differentiate responses mediated either through alpha9alpha10 or alpha7 nAChRs in those tissues where both receptors are expressed.

McIntosh M., et al. (2005) A novel α-conotoxin, PeIA, cloned from Conus Pergrandis, discriminates between rat α9α10 and α7 nicotinic cholinergic receptor. JBC. PMID: 15983035

品牌介绍

Smartox Biotechnolgy的多肽毒素产品如下：

1. 作用于钠离子通道(Sodium channel)的毒素

Toxin name	Catalog #	Target
Phrixotoxin-3	13PHX003	Selective blocker of Nav1.2
µ-conotoxin GIIIB	CON020	Selective blocker of Nav1.4
µ-conotoxin CnIIIC	CON021	Selective blocker of Nav1.4
μ-conotoxin PIIIA	08CON006	Selective blocker of Nav1.4
Jingzhaotoxin-III	12JZH003	Selective blocker of Nav1.5
ProTx-II	07PTX002	Selective blocker of Nav1.7
ProTx-II Biotin	12PTB002	Selective blocker of Nav1.7
ProTx-I	12PTX001	Blocker of Nav1.8, Nav1.2, Nav1.5, Nav1.7
Huwentoxin-I	07HWT001	Blocker of TTX-S
Huwentoxin-IV	08HWT002	Blocker of TTX-S
Hainantoxin-III	13HTX003	Blocker of TTX-S
Hainantoxin-IV	12HTX001	Blocker of TTX-S
GsAF-I	12GSF001	Blocker of TTX-S
GsAF-II	12GSF002	Blocker of TTX-S

2. 作用于钾离子通道(Potassium channel)的毒素

Toxin name	Catalog #	Target
K_Ca channels
Apamin 蜜蜂神经毒素	08APA001	SK1, SK2, SK3
Charybdotoxin 蝎毒素	11CHA001	KCa1.1, KCa3.1 - Kv1.2, Kv1.3, Kv1.6
Iberiotoxin	12IBX001	KCa1.1
Leiurotoxin 1 (Scyllatoxin)	10LEI001	SK1, SK2, SK3
Tamapin	10TAM001	SK1, SK2, SK3
Kaliotoxin-1	08KTX002	BK, Kv1.1, Kv1.2, Kv1.3
Kv channels
ShK	08SHK001	Kv1.3, Kv1.1, Kv1.4, Kv1.6
TMR-ShK	SAT001	Kv1.3, Kv1.1
Margatoxin	08MAG001	Kv1.3
(Dap22)-ShK	13SHD001	Kv1.3
ADWX-1	13ADW001	Kv1.3
HsTx1	08NEU001	Kv1.3, Kv1.2
Agitoxin-2	13AGI002	Kv1.3, Kv1.1
Maurotoxin	08MAR001	Kv1.2, KCa3.1
Guangxitoxin 1E	11GUA002	Kv2.1, Kv2.2
Stromatoxin 1 NEW	SCT01	Kv2.1, Kv2.2
Kaliotoxin-1	08KTX002	BK, Kv1.1, Kv1.2, Kv1.3
Charybdotoxin	11CHA001	KCa1.1, KCa3.1 - Kv1.2, Kv1.3, Kv1.6
Phrixotoxin-2	PHX002	Kv4.2, Kv4.3
AmmTx3 NEW	AMX001	A-type potassium channels
Inwardly rectifying potassium channels
TertiapinQ	08TER001	Kir1.1, Kir3.1/3.4, Kir3.1/3.2-KCa1.1
hERG/Kv11.1
BeKm-1	13BEK001	ERG1

3. 作用于钙离子通道(Calcium channel)的毒素

Toxin name	Catalog #	Target
High voltage-gated Ca²⁺ channels
ω-agatoxin IVA	11AGA001	P/Qtype
ω-Conotoxin MVIIC	08CON002	P/Qtype, N-type
ω-Conotoxin MVIIA	08CON001	N-type
ω-Conotoxin GVIA	08CON003	N-type
ω-Conotoxin SO3	08CON013	N-type
Huwentoxin I	07HWT001	N-type
ProTx-II	07PTX002	T-type, L-type
Intermediate voltage-gated Ca²⁺ channels
SNX482	08SNX002	R-type
Low voltage-gated Ca²⁺ channels
ProTx-I	12PTX001	T-type
ProTx-II	07PTX002	T-type, L-type
Ryanodine receptors
Maurocalcine	07PAU001	Ryr1

4. 作用于氯离子通道(Chloride channel)的毒素

Toxin name	Catalog #	Target
Chlorotoxin	08CHL001	Blocker of small conductance Cl- channels
GaTx1	13GTX001	Selective blocker of CFTR channel
GaTx2	10GTX002	Selective blocker of ClC-2 channel

5. 作用于乙酰胆碱受体(Acetylcholine receptor)的毒素

Toxin name	Catalog #	Target
α-conotoxin PeIA	13CON017	α9α10, α3β2 subunits
α-Conotoxin PrXA	13CON016	α1/β1/ε/δ, α1/β1/γ/δ subunits
Waglerin-1	12WAG001	MusclenAChR
α-conotoxin MI	08CON012	α1/δsubunits
α-conotoxin GI	08CON005	α/δsite
α-conotoxin IMI	08CON011	α7 homomeric nAChR
α-conotoxin GID	CON019	Blocker of α3β2, α7 and α4β2 nAChRs

6. 含N-甲基-D-天冬氨酸NR2B

(NMDA, NR2B containing N-methyl-D-aspartate)

Conantokin-G

选择性、特异性抑制含NR2B的NMDAR。Conantokin-G能剂量依赖性抑制Ca2+内流，抑制NMDA诱导的兴奋性中毒效应。研究表明，在小鼠皮层神经元，Conantokin-G阻滞NMDA引发的电流信号的IC50值为480 nM。

7. 作用于酸敏感离子通道(ASIC channel, Acid-Sensing Ion Channel)的毒素

Toxin name	Catalog #	Target
APETx2	07APE002	Selective blocker of ASIC3
Psalmotoxin1/PcTx1	13PCT001	Selective blocker of ASIC1a
Ugr9-1	13UGR001	Blocker of ASIC3

8. 作用于瞬时受体电位(TRP channel, transient receptor potential)的毒素

Toxin name	Catalog #	Target
GsMTx4	08GSM001	TRPC, TRPA
Vanillotoxin3	10VAN003	Activator of TRPV1
ProTx-I	12PTX001	Antagonist of TRPA1

9. 作用于嘌呤能通道(Purinergic channel)的毒素

Purotoxin-1

选择性抑制P2X3受体。100 nM Purotoxin-1 (PT-1)选择性抑制P2X3受体通道，在大鼠DRG神经元上，使用膜片钳实验表明：PT-1对电压门控通道和TRPV1均无抑制效应。10 µM ATP和100 µM α,β Methylene-ATP浓度下Purotoxin-1对P2X3受体有选择性作用，在该ATP浓度下Purotoxin-1对P2X2和杂化二聚体P2X2/3并无激动作用。Purotoxin-1对疼痛的潜在治疗作用。

10. 作用于其它膜受体通道(Others)的毒素

Smartox Biotechnology还提供其他类型的膜受体抑制剂：

Toxin name	Catalog #	Target
Morphiceptin	011CAS001	Agonist of µ-opoid receptors
Lys-conopressin G	11CON14	Vasopressin-like peptide
GsMTx4	08GSM001	Mechano sensitive ion channels
Obtustatin	10OBT001	Blocks the binding of α1β1 integrin to collagen IV
Rho-Conotoxin TIA	CON022	Blocks α1-adrenergic receptor

公司简介

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)”。

总之，Smartox Biotechnolgy提供一系列高质量、具开创价值的多肽毒素。这些化合物在离子通道研究中具有高的亲和性和选择性，是相应领域科学研究理想的生物毒素提供商和贴心的合作伙伴。

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