2. Immunology/Inflammation Protein Tyrosine Kinase/RTK NF-κB Metabolic Enzyme/Protease
  3. Glycoprotein VI Src Interleukin Related Reactive Oxygen Species (ROS) NOD-like Receptor (NLR) Mitochondrial Metabolism
  4. 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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Convulxin

Convulxin Chemical Structure

CAS No. : 37206-04-5

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Convulxin Related Antibodies

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Description

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[3].

IC50 & Target[1]

IL-10

 

IL-1β

 

In Vitro

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.

Convulxin Related Antibodies

Cell Viability Assay[1]

Cell Line: human PBMCs
Concentration: 0.3; 0.625; 1.25; 2.5; 5; 10; 20 μg/mL
Incubation Time: 12; 24; 48; 72 h
Result: Showed no effect on the viability of the PBMCs.

ELISA Assay[1]

Cell Line: human PBMCs
Concentration: 5; 10 μg/mL
Incubation Time: 12; 24 h
Result: Did not produce IL-2 at both times.
Stimulated PBMCs to produce a significant amount of IL-10 at both times.

Western Blot Analysis[1]

Cell Line: human PBMCs
Concentration: 5; 10 μg/mL
Incubation Time: 3 h
Result: Activated the NLRP3 inflammasome complex.
Led to IL-1β secretion via NF-κB, caspase-1, NLRP3, and ROS-dependent pathways.
In Vivo

Convulxin (5-200 µg/animal; 180-524 µg/kg; i.v.; i.p.; single dose) induces dose-dependent respiratory distress and convulsions in mice[3].
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.

Animal Model: Albino mice (17-21 g)[3]
Dosage: 5; 10; 200 µg
Administration: i.v.; single dose
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.
Animal Model: Cats (700-1360 g)[3]
Dosage: 80; 100 µg/kg
Administration: i.v.; single dose
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.
Animal Model: Mongrel dogs (5-10 kg)[3]
Dosage: 100; 125; 250 µg/kg; 0.2 mg/kg
Administration: i.v.; single dose
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.
Animal Model: Guinea pigs[3]
Dosage: 1000; 2000 µg/kg
Administration: i.p.; single dose
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.
Animal Model: Rabbits[3]
Dosage: 125; 250; 500 µg
Administration: s.c.; single dose
Result: Did not affect capillary permeability at any tested dose.
CAS No.
SMILES

[Convulxin]
Structure Classification
Initial Source

Crotalus durissus terrificus
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References
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Convulxin Related Classifications

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Keywords:

Convulxin37206-04-5Glycoprotein VISrcInterleukin RelatedReactive Oxygen Species (ROS)NOD-like Receptor (NLR)Mitochondrial MetabolismGPVIILhuman washed plateletsp72SYKSrc family kinaseperipheral blood mononuclear cellsglycoprotein VINLRP3 inflammasomeCD14+ monocytesFc receptor γ chainDectin-2rabbit plateletsInhibitorinhibitorinhibit

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