GLPBio

Ivermectin

Catalog No.: GC12339Purity:>98.00%Synonyms: 22,23-dihydro Avermectin B1, L-640,471, MK-933
Ivermectin is a macrolide endectocide with activity against both endoparasites and ectoparasites.

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Ivermectin
Cas No.: 70288-86-7
10mM (in 1mL DMSO)In Stock
$44.00
1
500mgIn Stock
$40.00
1
1gIn Stock
$68.00
1
5gIn Stock
$134.00
1

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Description

Ivermectin is a macrolide endectocide with activity against both endoparasites and ectoparasites [1]. Ivermectin disrupts neurotransmission in nerve and muscle cells, causing hyperpolarisation of the neuronal membrane, inducing paralysis of somatic muscles, particularly the pharyngeal pump, killing the parasites [2]. Ivermectin has been widely used to inhibit parasitic infections and kill viruses[3].

In vitro, Ivermectin treatment for 48 hours significantly inhibited the proliferation of C6 cells and U251 cells, with IC50 values of 16.32µM and 14.58µM, respectively[4]. 2.5µM of Ivermectin treatment for 72 hours reduced the proliferation of Pseudorabies virus (PRV) in BHK-21 cells and inhibited the entry of PRV DNA polymerase auxiliary subunit UL42 into the cell nucleus[5].

In vivo, Ivermectin treatment via oral administration at a dose of 0.2mg/kg twice a week for 5 weeks significantly increased the expression level of Cyp 3a11 in the liver of mice and the mRNA level of Cyp 1a1 in the intestine [6]. Intraperitoneal injection of a 3mg/kg dose of Ivermectin every other day for 30 days, which significantly inhibited tumor growth in the ovarian cancer xenograft mouse model, without affecting the body weight of the mice[7].

References:
[1] Dourmishev, Assen L., Lyubomir A. Dourmishev, and Robert A. Schwartz. "Ivermectin: pharmacology and application in dermatology." International journal of dermatology 44.12 (2005): 981-988.
[2] Crump A. Ivermectin: enigmatic multifaceted ‘wonder’drug continues to surprise and exceed expectations[J]. The Journal of antibiotics, 2017, 70(5): 495-505.
[3] Johnson-Arbor K. Ivermectin: a mini-review[J]. Clinical Toxicology, 2022, 60(5): 571-575.
[4] Song D, Liang H, Qu B, et al. Ivermectin inhibits the growth of glioma cells by inducing cell cycle arrest and apoptosis in vitro and in vivo[J]. Journal of Cellular Biochemistry, 2019, 120(1): 622-633.
[5] Lv C, Liu W, Wang B, et al. Ivermectin inhibits DNA polymerase UL42 of pseudorabies virus entrance into the nucleus and proliferation of the virus in vitro and vivo[J]. Antiviral research, 2018, 159: 55-62.
[6] Albérich M, Ménez C, Sutra J F, et al. Ivermectin exposure leads to up-regulation of detoxification genes in vitro and in vivo in mice[J]. European journal of pharmacology, 2014, 740: 428-435.
[7] Zhang X, Qin T, Zhu Z, et al. Ivermectin augments the in vitro and in vivo efficacy of cisplatin in epithelial ovarian cancer by suppressing Akt/mTOR signaling[J]. The American journal of the medical sciences, 2020, 359(2): 123-129.

Protocol

Cell experiment [1]:

Cell lines

C6 cells

Preparation Method

C6 cells were seeded at a density of 8×103 cells/well in a 96-well plate and cultured in DMEM medium supplemented with 1% fetal bovine serum (FBS) and 1% penicillin and streptomycin for 24h. C6 cells were subsequently treated with different concentrations of Ivermectin (0, 5, 10, 15, and 20µM) for 48h. Cell viability was analyzed.

Reaction Conditions

0, 5, 10, 15, and 20µM; 48h

Applications

Ivermectin treatment significantly reduced the cell viability of C6 cells in a dose-dependent manner.
Animal experiment [2]:

Animal models

NOD/SCID mice

Preparation Method

Ten million PA-1 cells suspended in 100μl of PBS were injected subcutaneously into NOD/SCID mice. After the development of palpable tumors, the mice were randomized into 4 treatment groups (n=10 each group): vehicle control (80%/20% saline/DMSO), Ivermectin at 3mg/kg on alternating days via intraperitoneal injection, cisplatin at 1mg/kg twice per week via intraperitoneal injection. Mice were treated with the drugs for 30 days and then euthanized via CO2 inhalation. Tumor length and width were measured every 3 days, and tumor volume was calculated using the formula: width2×length /2.

Dosage form

3mg/kg; every other day for 30 days; i.p.

Applications

Ivermectin treatment significantly inhibited tumor growth in the PA-1 xenograft mouse model.

References:
[1] Song D, Liang H, Qu B, et al. Ivermectin inhibits the growth of glioma cells by inducing cell cycle arrest and apoptosis in vitro and in vivo[J]. Journal of Cellular Biochemistry, 2019, 120(1): 622-633.
[2] Zhang X, Qin T, Zhu Z, et al. Ivermectin augments the in vitro and in vivo efficacy of cisplatin in epithelial ovarian cancer by suppressing Akt/mTOR signaling[J]. The American journal of the medical sciences, 2020, 359(2): 123-129.

Product Documents

Purity:>98.00%Appearance:A solid

Chemical Properties

CAS No.
70288-86-7
Synonyms
22,23-dihydro Avermectin B1, L-640,471, MK-933
Chemical Name
Ro 5-2807
SMILES
C/C([C@@H](O[C@H]1C[C@H](OC)[C@@H](O[C@H]2C[C@H](OC)[C@@H](O)[C@H](C)O2)[C@H](C)O1)[C@@H](C)/C=C/C=C(CO3)/[C@@]([C@@]3([H])[C@H](O)C(C)=C4)(O)[C@@H]4C5=O)=C\C[C@@H]6C[C@H](O5)C[C@@]7(O[C@@]([C@@H](C)CC)([H])[C@@H](C)CC7)O6
Molecular Formula
C48H74O14
Molecular Weight
875.09
Solubility
≥ 43.7545mg/mL in DMSO
Storage
Store at 2-8°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.

CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility

g/mol

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