For research use only. Not for therapeutic Use.
<p style=/line-height:25px/>Monepantel is organic anthelmintic, and acts as a positive allosteric modulator of a nematode-specific clade of nicotinic acetylcholine receptor (nAChR) subunits.<br>IC50﹠Target:<br>In Vitro: Monepantel (25 μM) induces accumulation of acidic vacuoles. Ovarian cancer cell lines are highly sensitive to Monepantel with IC50 values of 7.2 ± 0.2 μM (OVCAR-3) and 10.5 ± 0.4 μM (A2780). Monepantel (0, 10 and 25 μM) induces autophagosome formation in these cancer cell lines. Monepantel (0, 10 and 25 μM) exhibits a markedly reduced level of punctate staining indicating the suppression of phosphorylated mTOR at Ser2448. Monepantel also decreases the expression of phosphorylated Raptor at Ser792, which is one of the mTORC1 coMonepantelex members[2].<br>In Vivo:</p>
| Catalog Number | I005321 |
| CAS Number | 887148-69-8 |
| Molecular Formula | C20H13F6N3O2S |
| Purity | ≥95% |
| Solubility | 10 mM in DMSO |
| Storage | Store at -20°C |
| InChI | InChI=1S/C20H13F6N3O2S/c1-18(10-28,11-31-16-8-12(9-27)2-7-15(16)19(21,22)23)29-17(30)13-3-5-14(6-4-13)32-20(24,25)26/h2-8H,11H2,1H3,(H,29,30)/t18-/m0/s1 |
| InChIKey | WTERNLDOAPYGJD-SFHVURJKSA-N |
| SMILES | O=C(N[C@@](C)(C#N)COC1=CC(C#N)=CC=C1C(F)(F)F)C2=CC=C(SC(F)(F)F)C=C2 |
| Reference | </br>1:Mutations in the Hco-mptl-1 gene in a field-derived monepantel-resistant isolate of Haemonchus contortus. Bagnall NH, Ruffell A, Raza A, Elliott TP, Lamb J, Hunt PW, Kotze AC.Int J Parasitol Drugs Drug Resist. 2017 May 4;7(2):236-240. doi: 10.1016/j.ijpddr.2017.05.001. [Epub ahead of print] PMID: 28501715 Free Article</br>2:Reclassification of monepantel. [No authors listed]Vet Rec. 2017 Apr 8;180(14):361-362. doi: 10.1136/vr.j1704. No abstract available. PMID: 28385756 </br>3:Reclassification of monepantel. [No authors listed]Vet Rec. 2017 Apr 1;180(13):334. doi: 10.1136/vr.j1566. No abstract available. PMID: 28364082 </br>4:Organometallic Derivatization of the Nematocidal Drug Monepantel Leads to Promising Antiparasitic Drug Candidates. Hess J, Patra M, Rangasamy L, Konatschnig S, Blacque O, Jabbar A, Mac P, Jorgensen EM, Gasser RB, Gasser G.Chemistry. 2016 Nov 7;22(46):16602-16612. doi: 10.1002/chem.201602851. Epub 2016 Oct 5. PMID: 27706843 </br>5:Assessment of the nematocidal activity of metallocenyl analogues of monepantel. Hess J, Patra M, Jabbar A, Pierroz V, Konatschnig S, Spingler B, Ferrari S, Gasser RB, Gasser G.Dalton Trans. 2016 Nov 28;45(44):17662-17671. Epub 2016 Oct 17. PMID: 27748782 </br>6:Resistance of Haemonchus sp. to monepantel and reduced efficacy of a derquantel / abamectin combination confirmed in sheep in NSW, Australia. Sales N, Love S.Vet Parasitol. 2016 Sep 15;228:193-196. doi: 10.1016/j.vetpar.2016.08.016. Epub 2016 Aug 23. PMID: 27692326 </br>7:Increased expression of ATP binding cassette transporter genes following exposure of Haemonchus contortus larvae to a high concentration of monepantel in vitro. Raza A, Bagnall NH, Jabbar A, Kopp SR, Kotze AC.Parasit Vectors. 2016 Sep 29;9(1):522. PMID: 27682865 Free PMC Article</br>8:Phenotypic assessment of the ovicidal activity of monepantel and monepantel sulfone on gastro-intestinal nematode eggs. Bartley DJ, Meslé M, Donegan H, Devin L, Morrison AA.Vet Parasitol. 2016 Apr 15;220:87-92. doi: 10.1016/j.vetpar.2016.02.022. Epub 2016 Feb 23. PMID: 26995727 </br>9:Larval development assays reveal the presence of sub-populations showing high- and low-level resistance in a monepantel (Zolvix®)-resistant isolate of Haemonchus contortus. Raza A, Lamb J, Chambers M, Hunt PW, Kotze AC.Vet Parasitol. 2016 Apr 15;220:77-82. doi: 10.1016/j.vetpar.2016.02.031. Epub 2016 Mar 3. PMID: 26995725 </br>10:Hepatic biotransformation pathways and ruminal metabolic stability of the novel anthelmintic monepantel in sheep and cattle. Ballent M, Virkel G, Maté L, Viviani P, Lanusse C, Lifschitz A.J Vet Pharmacol Ther. 2016 Oct;39(5):488-96. doi: 10.1111/jvp.12296. Epub 2016 Feb 29. PMID: 26923886 |
