Purotoxin 1

Potent P2X3 modulator CAS# 1396322-38-5

Purotoxin 1

Catalog No. BCC6333----Order now to get a substantial discount!

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Chemical structure

Purotoxin 1

3D structure

Chemical Properties of Purotoxin 1

Cas No. 1396322-38-5 SDF Download SDF
PubChem ID 90488991 Appearance Powder
Formula C155H249N51O47S8 M.Wt 3835.47
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble to 1 mg/ml in water
Sequence GYCAEKGIRCDDIHCCTGLKCKCNASGYNCVCRKK

(Modifications: Disulfide bridge: 3-16,10-21,15-32, 23-30)

(Modifications: Lys-35 = C-terminal amide)

SMILES CCC(C)C1C(=O)NC(C(=O)NC2CSSCC3C(=O)NC(C(=O)NC4CSSCC(C(=O)NC(C(=O)NC(CSSCC(C(=O)NC(CSSCC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NCC(=O)N1)CCCCN)CCC(=O)O)C)NC(=O)C(CC5=CC=C(C=C5)O)NC(=O)CN)C(=O)NC(C(=O)NCC(=O)NC(C(=O)NC(C(=O)N3)CCCCN)CC(C)C)C(C)O)NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC2=O)CC(=O)O)CC(=O)O)C(C)CC)CC6=CNC=N6)C(=O)NC(CCCNC(=N)N)C(=O)NC(CCCCN)C(=O)NC(CCCCN)C(=O)N)C(C)C)NC(=O)C(NC(=O)C(NC(=O)CNC(=O)C(NC(=O)C(NC(=O)C(NC4=O)CC(=O)N)C)CO)CC7=CC=C(C=C7)O)CC(=O)N)CCCCN)CCCNC(=N)N
Standard InChIKey KECTXGMVIXOQAO-UHFFFAOYSA-N
Standard InChI InChI=1S/C155H249N51O47S8/c1-12-75(7)120-152(252)188-91(32-25-49-171-155(167)168)132(232)197-105-67-256-255-65-103-143(243)186-89(30-18-23-47-160)131(231)196-104-66-257-260-70-108(200-139(239)98(55-111(163)212)189-136(236)95(52-81-35-39-84(210)40-36-81)180-113(214)60-173-127(227)101(63-207)194-125(225)78(10)176-134(234)97(54-110(162)211)190-145(104)245)148(248)204-119(74(5)6)151(251)202-107(144(244)187-90(31-24-48-170-154(165)166)129(229)184-87(28-16-21-45-158)128(228)181-85(123(164)223)26-14-19-43-156)69-259-258-68-106(199-138(238)96(53-82-59-169-72-175-82)193-153(253)121(76(8)13-2)205-141(241)100(57-118(221)222)191-140(240)99(56-117(219)220)192-146(105)246)147(247)201-109(149(249)206-122(79(11)208)150(250)174-61-114(215)179-93(50-73(3)4)135(235)185-88(130(230)195-103)29-17-22-46-159)71-261-254-64-102(198-137(237)94(178-112(213)58-161)51-80-33-37-83(209)38-34-80)142(242)177-77(9)124(224)182-92(41-42-116(217)218)133(233)183-86(27-15-20-44-157)126(226)172-62-115(216)203-120/h33-40,59,72-79,85-109,119-122,207-210H,12-32,41-58,60-71,156-161H2,1-11H3,(H2,162,211)(H2,163,212)(H2,164,223)(H,169,175)(H,172,226)(H,173,227)(H,174,250)(H,176,234)(H,177,242)(H,178,213)(H,179,215)(H,180,214)(H,181,228)(H,182,224)(H,183,233)(H,184,229)(H,185,235)(H,186,243)(H,187,244)(H,188,252)(H,189,236)(H,190,245)(H,191,240)(H,192,246)(H,193,253)(H,194,225)(H,195,230)(H,196,231)(H,197,232)(H,198,237)(H,199,238)(H,200,239)(H,201,247)(H,202,251)(H,203,216)(H,204,248)(H,205,241)(H,206,249)(H,217,218)(H,219,220)(H,221,222)(H4,165,166,170)(H4,167,168,171)
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of Purotoxin 1

DescriptionPotent P2X3 receptor modulator (IC50 = 12 nM). Exhibits negligible effects on P2X2 and P2X2/3. Demonstrates antinociceptive properties in an animal model of inflammatory pain.

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References on Purotoxin 1

Modulation of P2X3 receptors by spider toxins.[Pubmed:22842000]

Biochim Biophys Acta. 2012 Nov;1818(11):2868-75.

Recently, the novel peptide named purotoxin-1 (PT1) has been identified in the venom of the spider Geolycosa sp. and shown to exert marked modulatory effects on P2X3 receptors in rat sensory neurons. Here we studied another polypeptide from the same spider venom, purotoxin-2 (PT2), and demonstrated that it also affected activity of mammalian P2X3 receptors. The murine and human P2X3 receptors were heterologously expressed in cells of the CHO line, and nucleotide-gated currents were stimulated by CTP and ATP, respectively. Both PT1 and PT2 negligibly affected P2X3-mediated currents elicited by brief pulses of the particular nucleotide. When subthreshold CTP or ATP was added to the bath to exert the high-affinity desensitization of P2X3 receptors, both spider toxins strongly enhanced the desensitizing action of the ambient nucleotides. At the concentration of 50nM, PT1 and PT2 elicited 3-4-fold decrease in the IC(50) dose of ambient CTP or ATP. In contrast, 100nM PT1 and PT2 negligibly affected nucleotide-gated currents mediated by mP2X2 receptors or mP2X2/mP2X3 heteromers. Altogether, our data point out that the PT1 and PT2 toxins specifically target the fast-desensitizing P2X3 receptor, thus representing a unique tool to manipulate its activity.

Novel peptide from spider venom inhibits P2X3 receptors and inflammatory pain.[Pubmed:20437566]

Ann Neurol. 2010 May;67(5):680-3.

P2X3 purinoreceptors expressed in mammalian sensory neurons play a key role in several processes, including pain perception. From the venom of the Central Asian spider Geolycosa sp., we have isolated a novel peptide, named purotoxin-1 (PT1), which is to our knowledge the first natural molecule exerting powerful and selective inhibitory action on P2X3 receptors. PT1 dramatically slows down the removal of desensitization of these receptors. The peptide demonstrates potent antinociceptive properties in animal models of inflammatory pain.

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