| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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| Other Sizes |
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Purity: ≥98%
Eprinomectin (also known as MK-397) is an avermectin used as a veterinary topical endectocide with anthelmintic, insecticidal and miticidal activity. It is a mixture of two chemical compounds, eprinomectin B1a and B1b. It is a semi-synthetic GABA signaling potentiator used to inhibit bacterial infections and can cause neuromuscular paralysis in microbes and parasites.
| ln Vitro |
Eprinomectin (2.5-50 μM; 0-48 h) significantly inhibits DU145 cell viability (IC50: 12.5 μM), colony formation and migration ability, and induces G0/G1 phase cell cycle arrest [1].
Eprinomectin (10-50 μM; 48 h) induces apoptosis and autophagy, increases reactive oxygen species production and endoplasmic reticulum stress, and promotes β-catenin nucleocytoplasmic translocation in DU145 cells [1]. |
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| ln Vivo |
Eprinomectin (0.08-0.5 mg/kg; Local pipette delivery; 14 days) has insecticidal, insecticidal and acaricidal activities in cattle[2].
Pharmacokinetic Analysis in cattle[1]
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| Cell Assay |
Cell Viability Assay[1]
Cell Line: DU145 cells Concentration: 2.5, 5, 10, 25 and 50 μM Incubation Time: 48 h Result: Significantly inhibited the cell viability. Western Blot Analysis[1] Cell Line: DU145 cells Concentration: 10, 25 and 50 μM Incubation Time: 48 h Result: Promotes the protein expression of pro-apoptotic marker BAD and DNA damage marker pH2AX and caspase-9 in a concentration-dependent manner. Inhibits DNA repair by reducing PARP-1. |
| Animal Protocol |
Animal Model: Infective nematode or chorioptes bovis treated male Jersey calves[2]
Dosage: 0.08, 0.16, 0.2, 0.24 and 0.5mg/kg Administration: Delivered topically from the tailhead to the withers at skin level via a pipette; 14 days Result:At the lowest dose (0.08 mg/kg), maximal or near-maximal efficacy was achieved against most adult endoparasites, with the exception of Capillaria serpiginosa (87%) and Capillaria cysticercus (88%). Control was ≥ 95% at all dose levels at day 14 post-treatment and was maintained at or near this efficacy level over the 6-week trial period. |
| References |
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| Molecular Formula |
C50H75NO14;C49H73NO14
|
|---|---|
| Molecular Weight |
914.13
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| CAS # |
123997-26-2
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| Related CAS # |
Eprinomectin-d3
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| Appearance |
White to off-white solid powder
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| Density |
1.23
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| Melting Point |
163-166 ºC
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| Flash Point |
2 °C
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| LogP |
5.469
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| SMILES |
C[C@H]1[C@@H](NC(C)=O)[C@@H](OC)C[C@H](O[C@@H]2[C@H](C)O[C@@H](O[C@@H](/C(C)=C/C[C@@H](C3)OC4(O[C@@H]([C@@H](CC)C)[C@H](C)C=C4)C[C@H]3OC5=O)[C@@H](/C=C/C=C6CO[C@@H]7[C@@]\6(O)[C@H]5C=C(C)[C@H]7O)C)C[C@@H]2OC)O1
|
| InChi Key |
WPNHOHPRXXCPRA-TVXIRPTOSA-N
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| InChi Code |
InChI=1S/C49H73NO14/c1-25(2)43-28(5)17-18-48(64-43)23-35-20-34(63-48)16-15-27(4)44(26(3)13-12-14-33-24-57-46-42(52)29(6)19-36(47(53)60-35)49(33,46)54)61-40-22-38(56-11)45(31(8)59-40)62-39-21-37(55-10)41(30(7)58-39)50-32(9)51/h12-15,17-19,25-26,28,30-31,34-46,52,54H,16,20-24H2,1-11H3,(H,50,51)/b13-12-,27-15-,33-14-/t26-,28-,30-,31-,34+,35-,36-,37+,38-,39-,40-,41+,42+,43+,44-,45+,46+,48+,49+/m0/s1
|
| Chemical Name |
Avermectin B1, 4''-(acetylamino)-4''-deoxy-, (4''R)-
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| Synonyms |
MK 397; MK-397; MK397; Eprinex; 4'-epi-acetylamino-4'-deoxy-avermectin B1a
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : 100~125 mg/mL (~136.74 )
Ethanol :~ 100 mg/mL |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (2.73 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (2.73 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (2.73 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 10% DMSO+40% PEG300+5% Tween-80+45% Saline: ≥ 2.5 mg/mL (2.73 mM) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.0939 mL | 5.4697 mL | 10.9394 mL | |
| 5 mM | 0.2188 mL | 1.0939 mL | 2.1879 mL | |
| 10 mM | 0.1094 mL | 0.5470 mL | 1.0939 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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