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

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.

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Selamectin Chemical Structure

Selamectin Chemical Structure

CAS No. : 220119-17-5

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Selamectin:

Selamectin Related Antibodies

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

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].

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

Selamectin Related Antibodies
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

769.96

Formula

C43H63NO11
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O[C@@]12[C@@]3([H])/C(C(C)=C[C@@]1([H])C(O[C@]4([H])C[C@]5(O[C@@](C/C=C(C)/[C@@H](O[C@@]6([H])C[C@@H]([C@@H](O)[C@H](C)O6)OC)[C@@H](C)/C=C/C=C2\CO3)([H])C4)O[C@H](C7CCCCC7)[C@@H](C)CC5)=O)=N\O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (129.88 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 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

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 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

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.2988 mL 6.4938 mL 12.9877 mL 32.4692 mL
5 mM 0.2598 mL 1.2988 mL 2.5975 mL 6.4938 mL
10 mM 0.1299 mL 0.6494 mL 1.2988 mL 3.2469 mL
15 mM 0.0866 mL 0.4329 mL 0.8658 mL 2.1646 mL
20 mM 0.0649 mL 0.3247 mL 0.6494 mL 1.6235 mL
25 mM 0.0520 mL 0.2598 mL 0.5195 mL 1.2988 mL
30 mM 0.0433 mL 0.2165 mL 0.4329 mL 1.0823 mL
40 mM 0.0325 mL 0.1623 mL 0.3247 mL 0.8117 mL
50 mM 0.0260 mL 0.1299 mL 0.2598 mL 0.6494 mL
60 mM 0.0216 mL 0.1082 mL 0.2165 mL 0.5412 mL
80 mM 0.0162 mL 0.0812 mL 0.1623 mL 0.4059 mL
100 mM 0.0130 mL 0.0649 mL 0.1299 mL 0.3247 mL
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Selamectin Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Selamectin220119-17-5ParasiteChloride ChannelP-glycoproteinBacterialCl− Channels P-gpPgpMultidrug resistance protein 1MDR1ATP-binding cassette sub-family B member 1ABCB1Cluster of differentiation 243CD243Inhibitorinhibitorinhibit

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