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Type HazMat fee for 500 gram (Estimated)
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Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Chemical Structure| 720710-69-0 Chemical Structure| 720710-69-0

Structure of 720710-69-0

Chemical Structure| 720710-69-0

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Product Citations

Product Citations

le Roux, Anandie ; Cloete, Stephanus J ; Petzer, Jacobus P ; Petzer, Anél ;

Abstract: Snakebite envenoming causes more than 130,000 deaths and more than 400,000 disabilities per year and has been classified as a priority Neglected Tropical Disease by the World Health Organization (WHO). While antivenom therapy remains the mainstay of snakebite treatment, small molecule therapeutics (SMTs) have been proposed as potential adjuncts to antivenom, particularly as oral treatment in the prehospital setting. Several SMTs have demonstrated efficacy in preclinical models of snakebite envenoming, with varespladib, a secreted phospholipase A2 (sPLA2) inhibitor, being granted orphan drug status for its potential to treat snakebite. The present study investigated the potential of four SMTs (e.g., varespladib, marimastat, nafamostat and dimercaprol) to neutralise toxic components present in the venom of southern African snake species. In vitro experimentation found that varespladib potently inhibited snake venom phospholipase A2 (svPLA2) activity in Bitis arietans (IC50 = 0.221 μM) and B. gabonica (IC50 = 0.276 μM). Marimastat exhibited potent inhibition of snake venom metalloproteinase (svMP) in several snake species with IC50 values ranging from 0.0042 to 3.06 μM, while dimercaprol, a metal chelator, was a lower potency svMP inhibitor with IC50 values ranging from 5.01 to 79.8 μM. Nafamostat proved to be an inhibitor of snake venom serine protease (svSP) in B. arietans (IC50 = 3.72 μM), B. gabonica (IC50 = 3.80 μM) and Causus rhombeatus (IC50 = 0.261 μM). These data demonstrate that SMTs are effective inhibitors of the relevant enzymes in several snake species and support the proposal that SMTs could be developed for therapeutic intervention in snakebite envenoming.

Keywords: Snakebite ; Varespladib ; Marimastat ; Nafamostat ; Dimercaprol ; Inhibition

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Alternative Products

Product Details of Mca-Lys-Pro-Leu-Gly-Leu-Dap(Dnp)-Ala-Arg-NH2

CAS No. :720710-69-0
Formula : C55H80N16O16
M.W : 1221.32
SMILES Code : O=C([C@H]1N(C([C@H](CCCCN)NC(CC(C2=C(O3)C=C(OC)C=C2)=CC3=O)=O)=O)CCC1)N[C@@H](CC(C)C)C(NCC(N[C@@H](CC(C)C)C(N[C@@H](CNC4=CC=C([N+]([O-])=O)C=C4[N+]([O-])=O)C(N[C@@H](C)C(N[C@@H](CCCNC(N)=N)C(N)=O)=O)=O)=O)=O)=O
MDL No. :MFCD07368601

Safety of Mca-Lys-Pro-Leu-Gly-Leu-Dap(Dnp)-Ala-Arg-NH2

GHS Pictogram:
Signal Word:Danger
Hazard Statements:H228-H315-H319
Precautionary Statements:P240-P210-P241-P264-P280-P302+P352-P370+P378-P337+P313-P305+P351+P338-P362+P364-P332+P313
Class:4.1
UN#:1325
Packing Group:

Isoform Comparison

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

0.82mL

0.16mL

0.08mL

4.09mL

0.82mL

0.41mL

8.19mL

1.64mL

0.82mL

 

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