Selamectin

Selamectin is an avermectin derivative prepared by hydrolysis and oximation of doramectin Selamectin is a potent nematocide used for the treatment of parasites which selectively binds to parasite glutamate-gated chloride ion channels and disrupts neurotransmission

Product information

CAS Number: 220119-17-5

Molecular Weight: 769.96

Formula: C43H63NO11

Synonym:

UK-124114

Chemical Name: A name could not be generated for this structure.

Smiles: CO[C@@H]1C[C@@H](O[C@@H](C)[C@@H]1O)O[C@H]1[C@@H](C)C=CC=C2CO[C@@H]3/C(=N\O)/C(C)=C[C@@H](C(=O)O[C@H]4C[C@H](CC=C1C)O[C@]1(C4)CC[C@H](C)[C@H](O1)C1CCCCC1)[C@@]23O |c:17,t:15,36|

InChiKey: AFJYYKSVHJGXSN-VOMYPSQFSA-N

InChi: InChI=1S/C43H63NO11/c1-24-11-10-14-30-23-50-40-36(44-48)27(4)19-33(43(30,40)47)41(46)52-32-20-31(16-15-25(2)38(24)53-35-21-34(49-6)37(45)28(5)51-35)54-42(22-32)18-17-26(3)39(55-42)29-12-8-7-9-13-29/h10-11,14-15,19,24,26,28-29,31-35,37-40,45,47-48H,7-9,12-13,16-18,20-23H2,1-6H3/b11-10-,25-15-,30-14-,44-36-/t24-,26-,28-,31-,32-,33-,34+,35-,37-,38-,39-,40+,42+,43-/m0/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : ≥ 100 mg/mL (129.88 mM) H2O : < 0.1 mg/mL (insoluble)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

The transport of radiolabelled Selamectin through Caco-2 monolayers shows that Selamectin is P-glycoprotein (P-gp) substrates with a secretory/absorptive ratio of 4.7. Selamectin inhibits the efflux of Rh-123 from peripheral blood lymphocytes (PBL) and the concentration of inhibition is similar to that of Verapamil[2].

In Vivo:

A single administration of 6 mg/kg topical Selamectin given every two months could effectively prevent B. malayi infection in cats. Application of topical Selamectin twice a year could block circulating microfilariae[1].

References:

1. Patsharaporn T Sarasombath, et al. First study of topical selamectin efficacy for treating cats naturally infected with Brugia malayi and Brugia pahangi under field conditions. Parasitol Res. 2019 Apr;118(4):1289-1297.
2. J Griffin, et al. Selamectin is a potent substrate and inhibitor of human and canine P-glycoprotein. J Vet Pharmacol Ther. 2005 Jun;28(3):257-65.

Products are for research use only. Not for human use.