Vapendavir - CAS 439085-51-5
Catalog number: 439085-51-5
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C21H26N4O3
Molecular Weight:
382.46
COA:
Inquire
Targets:
Rhinovirus
Description:
Vapendavir is an orally active capsid-binding inhibitor as a capsid binderwith potent anti-rhinoviral activity and broad serotype coverage.
Purity:
≥95%
Appearance:
White Solid
Synonyms:
Vapendavir; BTA-798; BTA798; BTA 7983-Ethoxy-6-[2-[1-(6-methyl-3-pyridazinyl)-4-piperidinyl]ethoxy]-1,2-benzisoxazole;
Solubility:
Soluble in DMSO
Storage:
Store at -20 °C
MSDS:
Inquire
Application:
Rhinovirus replication inhibitor
Quality Standard:
Enterprise standard
Shelf Life:
As supplied, 2 years from the QC date provided on the Certificate of Analysis, when stored properly.
Quantity:
Milligrams-Grams
InChIKey:
DKSVBVKHUICELN-UHFFFAOYSA-N
InChI:
1S/C21H26N4O3/c1-3-26-21-18-6-5-17(14-19(18)28-24-21)27-13-10-16-8-11-25(12-9-16)20-7-4-15(2)22-23-20/h4-7,14,16H,3,8-13H2,1-2H3
Canonical SMILES:
CCOc1c2ccc(cc2on1)OCCC3CCN(CC3)c4ccc(nn4)C
Current Developer:
Biota Holdings
1.The capsid binder Vapendavir and the novel protease inhibitor SG85 inhibit enterovirus 71 replication.
Tijsma A;Franco D;Tucker S;Hilgenfeld R;Froeyen M;Leyssen P;Neyts J Antimicrob Agents Chemother. 2014 Nov;58(11):6990-2. doi: 10.1128/AAC.03328-14. Epub 2014 Sep 8.
Antivirals against enterovirus 71 (EV71) are urgently needed. We demonstrate that the novel enteroviral protease inhibitor (PI) SG85 and capsid binder (CB) vapendavir efficiently inhibit the in vitro replication of 21 EV71 strains/isolates that are representative of the different genogroups A, B, and C. The PI rupintrivir, the CB pirodavir, and the host-targeting compound enviroxime, which were included as reference compounds, also inhibited the replication of all isolates. Remarkably, the CB compound pleconaril was devoid of any anti-EV71 activity. An in silico docking study revealed that pleconaril-unlike vapendavir and pirodavir-lacks essential binding interactions with the viral capsid. Vapendavir and SG85 (or analogues) should be further explored for the treatment of EV71 infections. The data presented here may serve as a reference when developing yet-novel inhibitors.
2.Antiviral Activity of Broad-Spectrum and Enterovirus-Specific Inhibitors against Clinical Isolates of Enterovirus D68.
Sun L;Meijer A;Froeyen M;Zhang L;Thibaut HJ;Baggen J;George S;Vernachio J;van Kuppeveld FJ;Leyssen P;Hilgenfeld R;Neyts J;Delang L Antimicrob Agents Chemother. 2015 Dec;59(12):7782-5. doi: 10.1128/AAC.01375-15. Epub 2015 Sep 14.
We investigated the susceptibility of 10 enterovirus D68 (EV-D68) isolates (belonging to clusters A, B, and C) to (entero)virus inhibitors with different mechanisms of action. The 3C-protease inhibitors proved to be more efficient than enviroxime and pleconaril, which in turn were more effective than vapendavir and pirodavir. Favipiravir proved to be a weak inhibitor. Resistance to pleconaril maps to V69A in the VP1 protein, and resistance to rupintrivir maps to V104I in the 3C protease. A structural explanation of why both substitutions may cause resistance is provided.
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