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011PUR001-Purotoxin-1
- 發(fā)布日期：
- 有效日期：
- 所 在 地：
- 產(chǎn) 地：
- 已獲點(diǎn)擊：
- 2024年10月13日
- 2025年4月13日
- 北京北京市
- 法國
- 90次
【產(chǎn)品簡介】
【詳細(xì)說明】
Purotoxin-1
Selective inhibitor of P2X3 receptors
ATP離子通道P2X3受體選擇性抑制劑
Therapeutic interest : painPurotoxin-1 (PT-1) is a peptide originally isolated from the Central Asian spider Geolycosa sp. Purotoxin-1 was shown to inhibit selectively P2X3 receptor channels at a 100 nM concentration. Studies were carried-out on cultured rat DRG neurons. Patch-clamp experiments did not show any inhibitory effect of PT-1 on voltage-gated channels (potentials range tested from -100 to 20 mV), neither on TRPV1 (after activation with 500 nM capsaicin). The selectivity of Purotoxin-1 for P2X3 was highlighted by activating this receptor with 10 µM ATP and 100 µM α, β Methylene-ATP. Indeed, unlike P2X3, P2X2 and heterodimer P2X2/3 are known to be not sensitive to such concentrations. Moreover, P2X3, P2X2, and P2X2/3 are the only known ATP-sensitive receptors expressed in plasma membranes of DRG neurons. So, the observed effect seems to be well related to a selective inhibition of P2X3. P2X3-mediated current was fully inhibited with 100 nMPurotoxin-1, making it the most potent and selective ligand for P2X3.
P2X3 receptors are known to be implicated in pain mechanisms. Behavioral experimentations carried-out on rat pain models using 0.5 nmol PT-1 injected intraplantar showed to reduce nociception. This anti-nociceptive effect is comparable to A-317491 compound (Abbott's drug) with an amount of almost 3 orders of magnitude lower.
Purotoxin-1 技術(shù)資料
氨基酸序列：
Gly-Tyr-Cys3-Ala-Glu-Lys-Gly-Ile-Arg-Cys10-Asp-Asp-Ile-His-Cys15-Cys16-Thr-Gly-Leu-Lys-Cys21-Lys-Cys23-Asn-Ala-Ser-Gly-Tyr-Asn-Cys30-Val-Cys32-Arg-Lys-Lys-NH2
二硫鍵：Cys3-Cys16; Cys10-Cys21; Cys15-Cys32; Cys23-Cys30
長度 (aa)： 35
分子式：C155H248N50O48S8
分子量： 3834.59 Da
外觀：White lyophilized solid
可溶性： water and saline buffer
CAS 號：not available
來源： Synthetic
純度： > 97 %
產(chǎn)品信息
011PUR001-00100 | Purotoxin 1 | 0.1mg |
011PUR001-00500 | Purotoxin 1 | 0.5mg |
011PUR001-01000 | Purotoxin 1 | 1mg |