1. Anti-infection
    Membrane Transporter/Ion Channel
  2. Parasite
    Chloride Channel
    P-glycoprotein
  3. Selamectin

Selamectin 

Cat. No.: HY-107212 Purity: 99.89%
Handling Instructions

Selamectin, a semi-synthetic macrocyclic lactone, is a potent parasiticide and anthelminthic. Selamectin activates glutamate-gated chloride channels in neurons and pharyngeal muscles to prevent heartworm, Lymphatic filariae, and nematode infection. Selamectin is also a potent P-glycoprotein substrate and a P-glycoprotein inhibitor with an IC50 of 120 nM.

For research use only. We do not sell to patients.

Selamectin Chemical Structure

Selamectin Chemical Structure

CAS No. : 220119-17-5

Size Price Stock Quantity
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Solution
10 mM * 1 mL in DMSO USD 163 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 163 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 120 In-stock
Estimated Time of Arrival: December 31
10 mg USD 192 In-stock
Estimated Time of Arrival: December 31
25 mg USD 348 In-stock
Estimated Time of Arrival: December 31
50 mg USD 552 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

Selamectin, a semi-synthetic macrocyclic lactone, is a potent parasiticide and anthelminthic. Selamectin activates glutamate-gated chloride channels in neurons and pharyngeal muscles to prevent heartworm, Lymphatic filariae, and nematode infection. Selamectin is also a potent P-glycoprotein substrate and a P-glycoprotein inhibitor with an IC50 of 120 nM[1][2].

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

769.96

Formula

C₄₃H₆₃NO₁₁

CAS No.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (129.88 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.2988 mL 6.4938 mL 12.9877 mL
5 mM 0.2598 mL 1.2988 mL 2.5975 mL
10 mM 0.1299 mL 0.6494 mL 1.2988 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (3.25 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.5 mg/mL (3.25 mM); Suspended solution; Need ultrasonic

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (3.25 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Animal Administration
[1]

The cats are weighed on Days-2, 29 and 58 to calculate the dosing. Cats in group 1 (control group) remain untreated. On Day 0, the cats in group 3 are treated with fluralaner at the minimum recommending label dose of 40.0 mg per kg body weight. On Days 0, 30 and 60, the cats in group 2 are treated with the new spot-on formulation at the minimum recommending label dose of 1.0 mg/kg sarolaner and 6.0 mg/kg Selamectin. The cats are observed at different time points after treatment for possible adverse reactions to treatment. On Day 0, administration site observations are performed on all cats 30 min (±5 min), 3 h (±15 min) and 24 h (±1 h) and again on Days 3 and 5 after treatment[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Product Name:
Selamectin
Cat. No.:
HY-107212
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