Convulxin
Convulxin is a toxin found in a tropical rattlesnake. Convulxin stimulates platelet aggregation, and clusters GPVI to trigger Src family kinase activation, Fc receptor γ chain phosphorylation, and p72SYK signaling. Convulxin interacts with Dectin-2 to induce IL-10 production, activates monocytes to generate ROS and NLRP3 inflammasome-mediated IL-1β secretion, and induces mitochondrial ROS. Convulxin causes transient arterial blood pressure changes in dogs. Convulxin can be used for research related to coagulation.
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- CAS No.: 37206-04-5
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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IL-10 |
IL-1β |
Convulxin (0.3-20 μg/mL; 12-96 h) is non-toxic to human peripheral blood mononuclear cells[1].
Convulxin (5-10 μg/mL; 72 h) does not stimulate proliferation of human peripheral blood mononuclear cells[1].
Convulxin (5-10 μg/mL; 12-24 h) does not induce IL-2 secretion but stimulates IL-10 secretion via interaction with Dectin-2 in human peripheral blood mononuclear cells[1].
Convulxin (5-10 μg/mL; 24-72 h) does not stimulate nitric oxide production in human peripheral blood mononuclear cells[1].
Convulxin (5-10 μg/mL; 2-3 h) stimulates mitochondrial and intracellular ROS production in human CD14+ monocytes[1].
Convulxin (5-10 μg/mL; 3 h) activates the NLRP3 inflammasome complex in human peripheral blood mononuclear cells, leading to IL-1β secretion via NF-κB, caspase-1, NLRP3, and ROS-dependent pathways[1].
Convulxin (3-10 ng/mL) potently induces maximal aggregation of isolated human washed platelets, acting independently of the GPIb and α2β1 platelet receptors[2].
Convulxin (1 μg/mL; 3 h) specifically binds to the p62/GPVI collagen receptor on human platelet membranes[2].
Convulxin (30 ng/mL; 0-4 min) induces rapid, intense tyrosine phosphorylation of Fc receptor γ chain, p36-38, p725ʸᴷ, PI3K, c-Cbl, and PLCγ2 in isolated human washed platelets, signaling through p62/GPVI without direct involvement of α2β1-dependent early pp125FAK phosphorylation[2].
Convulxin (0.2-200 μg) exhibits no coagulant activity in dog or rabbit plasma[3].
Convulxin (20 pM-5 nM; 28 h) binds to washed rabbit platelets with high affinity (Kd = 30 pM) at 1000 specific sites per cell, with additional lower-affinity binding sites present[4].
Convulxin specifically competes for its own binding sites on washed rabbit platelets (IC50 = 8 nM), while common platelet agonists and antagonists do not interfere with this binding[4].
Convulxin (0.5-5 nM; 24-96 h) binds to washed rabbit platelets with a rapid association rate and extremely slow dissociation, resulting in a high-affinity interaction (kinetic Kd = 7 pM)[4].
Convulxin (300 μg/mL) does not exhibit haemagglutination activity against intact or trypsinized erythrocytes from rabbit, rat, mouse, hamster, guinea-pig, or human (O-type)[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human PBMCs
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Concentration:0.3; 0.625; 1.25; 2.5; 5; 10; 20 μg/mL
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Incubation Time:12; 24; 48; 72 h
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Result:Showed no effect on the viability of the PBMCs.
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Cell Line:human PBMCs
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Concentration:5; 10 μg/mL
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Incubation Time:12; 24 h
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Result:Did not produce IL-2 at both times.
Stimulated PBMCs to produce a significant amount of IL-10 at both times.
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Cell Line:human PBMCs
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Concentration:5; 10 μg/mL
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Incubation Time:3 h
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Result:Activated the NLRP3 inflammasome complex.
Led to IL-1β secretion via NF-κB, caspase-1, NLRP3, and ROS-dependent pathways.
Convulxin (80-100 µg/kg; i.v.; single dose) induces dose-dependent neurological and respiratory effects in Felis catus, with an ED50 of 80 µg/kg for convulsions, and most animals recover within 30 minutes[3].
Convulxin (100 µg/kg-0.2 mg/kg; i.v.; single dose) induces immediate neurological, respiratory, and cardiovascular effects in dogs, causing transient hypotension, pressor effects, apnea, and delayed convulsions in some animals, with minimal impact on haematocrit values[3].
Convulxin (1000-2000 µg/kg; i.p.; single dose) induces dose-dependent neurological and respiratory effects leading to respiratory failure in guinea pigs[3].
Convulxin (125-500 µg; s.c.; single dose) does not alter capillary permeability in rabbits[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Albino mice (17-21 g)[3]
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Dosage:5; 10; 200 µg
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Administration:i.v.; single dose
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Result:Caused tachypnea followed by brief apnea within 20 seconds.
Caused intense convulsive crises, usually leading to death.
Was ineffective at doses up to 200 µg/animal.
Reached an LD50 of 524 µg/kg.
Reached an ED50 of 522 µg/kg for convulsions.
Reached an ED50 of 180 µg/kg for brief apnea.
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Animal Model:Cats (700-1360 g)[3]
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Dosage:80; 100 µg/kg
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Administration:i.v.; single dose
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Result:Caused immediate respiratory disturbances (tachypnea leading to intense dyspnea), miosis, salivation, abdominal cramps, nystagmus, loss of equilibrium, convulsions, and sometimes brief hypotonia.
Reached an ED50 of 80 µg/kg for convulsions.
Allowed most animals to recover within 30 minutes.
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Animal Model:Mongrel dogs (5-10 kg)[3]
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Dosage:100; 125; 250 µg/kg; 0.2 mg/kg
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Administration:i.v.; single dose
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Result:Caused immediate excitation, barking, loss of equilibrium, respiratory disturbances, nystagmus, urination, defecation, and vomiting; after apparent recovery, 2/5 dogs developed intermittent clonic convulsions with 24-hour latency, while 3/5 had alternating agitation and torpor.
Caused an abrupt, transient fall in arterial blood pressure within 10 seconds, followed by a short-duration pressor effect; late hypotension was absent or slight.
Caused immediate increases in respiratory frequency and amplitude, followed by apnea lasting at least 0.5 minutes; 3/5 dogs died from persistent apnea, while 1 required 24 minutes of artificial respiration.
Caused a mean haematocrit change of 10%, with no significant alteration from baseline.
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Animal Model:Guinea pigs[3]
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Dosage:1000; 2000 µg/kg
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Administration:i.p.; single dose
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Result:Caused tremors and convulsive movements within the first hour, followed by dyspnea and apnea 4-10 hours post-injection.
Led to death from respiratory failure, with muscular tone retained.
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Animal Model:Rabbits[3]
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Dosage:125; 250; 500 µg
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Administration:s.c.; single dose
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Result:Did not affect capillary permeability at any tested dose.
Chemical Information
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CAS No. 37206-04-5
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SMILES
[Convulxin]
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Structure Classification
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Initial Source
Crotalus durissus terrificus
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Rego CMA, Francisco AF, Boeno CN, et al.. Inflammasome NLRP3 activation induced by Convulxin, a C-type lectin-like isolated from Crotalus durissus terrificus snake venom. Scientific reports. 2022 Mar 18;12(1):4706. [Content Brief]
[2]. Polgár J, Clemetson JM, Kehrel BE, et al.. Platelet activation and signal transduction by convulxin, a C-type lectin from Crotalus durissus terrificus (tropical rattlesnake) venom via the p62/GPVI collagen receptor. The Journal of biological chemistry. 1997 May 23;272(21):13576-83. [Content Brief]
[3]. Prado-Franceschi J, et al. Convulxin, a new toxin from the venom of the South American rattlesnake Crotalus durissus terrificus. Toxicon. 1981;19(6):875-87. [Content Brief]
[4]. Francischetti IM, Saliou B, Leduc M, et al.. Convulxin, a potent platelet-aggregating protein from Crotalus durissus terrificus venom, specifically binds to platelets. Toxicon : official journal of the International Society on Toxinology. 1997 Aug;35(8):1217-28. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Convulxin Related Classifications
HY-117123 Related Classifications
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- Convulxin
- 37206-04-5
- Glycoprotein VI
- Src
- Interleukin Related
- Reactive Oxygen Species (ROS)
- NOD-like Receptor (NLR)
- Mitochondrial Metabolism
- human washed platelets
- p72SYK
- Src family kinase
- peripheral blood mononuclear cells
- glycoprotein VI
- NLRP3 inflammasome
- CD14+ monocytes
- Fc receptor γ chain
- Dectin-2
- rabbit platelets
- Inhibitor
- inhibitor
- inhibit