Shaanxi BLOOM Tech Co., Ltd. is one of the most experienced manufacturers and suppliers of lotilaner powder in China. Welcome to wholesale bulk high quality lotilaner powder for sale here from our factory. Good service and reasonable price are available.
Lotilaner powder is a chemically well‑defined compound with a CAS number of 1369852-71-0, a molecular formula of C₂₀H₁₄Cl₃F₆N₃O₃S, and an accurately calculated molecular weight of 596.76. It presents as a white to off‑white solid at room temperature and exhibits a series of distinct physicochemical properties that support its research and developmental applications.
The compound has a predicted density of 1.66 ± 0.1 g/cm³ and a pKa value of 12.52 ± 0.46, reflecting its specific acid‑base behavior in solution. In terms of solubility, lotilaner shows excellent dissolution in dimethyl sulfoxide (DMSO), with solubility reaching ≥ 100 mg/mL (167.57 mM), which greatly facilitates its use in laboratory testing, in vitro studies, and early pharmaceutical formulation development.
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To maintain its structural integrity and biological activity, long‑term storage at −20 °C is strongly recommended. This article provides a comprehensive analysis of metronidazole injection 100 mL, a cornerstone clinical antimicrobial agent typically formulated at a concentration of 500 mg per 100 mL. It systematically examines the drug's pharmacological mechanisms, evidence‑based clinical indications, standardized administration procedures, common and rare adverse reactions, and key safety precautions necessary for rational clinical use. As a classic nitroimidazole derivative with potent activity against anaerobic bacteria and protozoa.
It is widely applied in inpatient wards, intensive care units, and surgical settings to manage severe and refractory infections, offering valuable guidance for standardized and safe clinical practice.The clinical manifestations of anaerobic bacterial infections differ considerably based on the infected tissue or organ, the species of pathogenic anaerobes involved, and the patient's underlying health condition. In most cases,however, they present a combination of localized inflammatory symptoms, systemic inflammatory responses, and characteristic diagnostic signs, which are elaborated in detail below:
Clinical application: from single deworming to comprehensive prevention and control
1.1 Prevention and control of external parasites
Flea prevention and control:
Killing adult insects: The killing rate is>99% within 8 hours after administration and reaches 100% within 24 hours.
Blocking reproduction: Inhibiting the development of eggs and larvae, cutting off the life cycle of fleas.
Clinical case: Field studies in the United States have shown that after continuous use for 3 months, the number of fleas in the home environment decreases by 99.5% -100%, and pet skin symptoms (erythema, desquamation) significantly improve.
Quick onset: Killing begins 4 hours after administration, with a killing rate of ≥ 97% within 48 hours.
Disease prevention: By blocking tick bites, reduce the risk of tick borne diseases such as Lyme disease and Babesia.
1.2 Prevention and control of internal parasites (compound preparation)
Taking Credelio Quattro (compound of Lopinal/Moxibustin/Praziquantel/Thiamethoxam) as an example:
Heartworm prevention: 100% prevention of canine heartworm disease, blocking the development of L3 stage larvae.
2.Special Scenario Applications
2.1 Protection of puppies and elderly dogs
Suitable age: Puppies over 8 weeks old can use lotilaner powder, with a minimum weight of 1.5kg.
Elderly dog safety: No risk of liver and kidney toxicity accumulation, suitable for pets with chronic disease comorbidities.
2.2 Breeding period management
Pregnancy: Although safety has not been formally evaluated, no teratogenic effects have been found in clinical monitoring.
Breastfeeding period: The amount of medication secreted through breast milk is extremely low and does not affect the health of the offspring.
2.3 Prevention and Control of Multi Pet Families
Cross protection: Reduce cross infection among pets through environmental pest control.
Collaborative medication: can be used in combination with vaccines, antibiotics, etc., without significant drug interactions.
3.Product portfolio: Upgrades from individual items to solutions
3.1 Unilateral formulations (Credelio series)
Credelio CAT: Oral flea/tick medication and beef flavored chewable tablets for cats to improve palatability.
Credelio DOG: a single agent for dogs, focusing on the prevention and control of external parasites.
3.2 Compound preparation (Credelio Quattro)
Four effects in one:
Lothilana: Quickly kills fleas/ticks.
Moxibustin: Prevent heartworms and control mites.
Praziquantel: broad-spectrum anti tapeworm.
Thiamethoxam: Quickly kills roundworms/hookworms.
Clinical advantages:
Reduce medication frequency: Replace multiple medications once a month.
Improve compliance: Beef flavored chewable tablets have a palatability of 92%.
Reduce the risk of drug resistance: multi-target action delays parasite drug resistance.
In the existing technology, PCT patents WO2022020585A1 and WO2014090918A1 disclose a synthetic route for lotilaner powder. Specifically, before the formation of the imidazole ring, halogen or carboxyl groups are introduced into the thiophene ring in advance, and then side chains are introduced to obtain lotilan. However, the inventor found through research that in the synthesis method of lotilana in the aforementioned patent, the method of introducing halogens or carboxyl groups on the thiophene ring before the formation of the imidazole ring, and then introducing side chains, is difficult to obtain raw materials, expensive, and has the disadvantage of reducing molecular polarity.
At the same time, in the post-processing of the subsequent cyclization reaction, there are many impurities in the finished product that are difficult to purify. Impurities are easily introduced into the finished product, making it more difficult to refine. Multiple purification treatments are required, making production difficult, energy consuming, and costly, making it difficult to achieve industrial production. Therefore, overcoming the obvious shortcomings in the synthesis process of lotilana in existing technologies and developing a synthesis route suitable for industrial scale production is particularly important for achieving the industrialization of lotilana.
Synthetic method
1. Add 140g (1.0mol) of 2-acetyl-4-methylthiophene and 277g (1.0mol) of 2,2,2-trifluoro-1- (3,4,5-trichlorophenyl) acetophenone, each containing 700mL of methyl tert butyl ether, to a three necked flask. After stirring and dissolving, add 50g of triethylamine and react at 50 ℃ for 2 hours to obtain the reaction solution. After cooling the reaction solution to below 5 ℃, slowly add 50g of thionyl chloride and heat it up to 40 ℃ for 3 hours. After cooling, extract with 200mL of saturated sodium bicarbonate solution and 200mL of purified water respectively. Extract the aqueous phase twice with 100mL of methyl tert butyl ether, combine the organic phases and wash once with 200mL of purified water. Dry with anhydrous sodium sulfate, filter, and concentrate the filtrate under reduced pressure at 50 ℃ to obtain a concentrate. The concentrate is recrystallized from an ethanol/water (volume ratio 1:1) solution to obtain 351g of intermediate I with a yield of 87.8%.
2. Add 350g of intermediate I (0.876mol) and 1000mL of ethanol into a reaction flask, stir to dissolve, cool to below 5 ℃, then add 60.9g of hydroxylamine hydrochloride (0.876mol), slowly add 116g of 30wt% sodium hydroxide solution, and react at 20 ℃ for 3 hours; Then add 1000mL of deionized water, stir for 2 hours, filter, wash the filter cake with deionized water, dry until there is no change in weight, and obtain 313g of intermediate II with a yield of 86.2%.
3. Add 50g (0.12mol) of intermediate II and 100mL of LDMF into a reaction flask. Add phosphorus oxychloride (24.5, 0.16mol) dropwise at 0 ℃. After the dropwise addition is complete, react at 0 ℃ for 10 hours. After the reaction is complete, pour the reaction solution into 1000mL of ice water, let it stand for 15 minutes, then dilute it further with 300mL of water and 100mL of saturated NaHCO3, and stir for 1 hour; Then extract three times with 50mL of ethyl acetate, combine the organic phases, dry with anhydrous sodium sulfate, filter, and concentrate the filtrate under reduced pressure at 50 ℃ until the total volume is reduced by about 1/3 to obtain a concentrate. Then, under stirring conditions, 500mL of n-hexane was added dropwise to the concentrate, and allowed to crystallize until there was no solid precipitation. The solid was filtered and dried until there was no change in weight, resulting in 48g of white crystalline intermediate III with a yield of 90.3%.
4. CuSO4 · 5H2O (1.25g, 5mmol), 2-amino-N - (2,2,2-trifluoroethyl) acetamide hydrochloride (19.3g, 0.1mol), triethylamine (20.2 g, 0.2mol), CaCO3 (11g, 0.11mol), and 200mL acetonitrile were added to a reaction flask. Intermediate III (44.3g, 0.1mol) and tert butanol hydroperoxide (70% aqueous solution, 16mL, 0.11mol) were added under nitrogen atmosphere. The reaction was stirred at 20-30 ℃ for 6 hours, and then concentrated under reduced pressure at 50 ℃ to obtain a concentrated solution. The concentrated solution was crystallized using n-hexane/ethyl acetate (volume ratio 1:5) to obtain 55.7g of lotilaner powder with a yield of. 93.3%, HPLC purity 99.90%.
In summary, Lotilaner powder presents well‑defined physicochemical properties, including stable solid form, favorable solubility in DMSO, and clear acid‑base characteristics, laying a reliable foundation for its research and pharmaceutical development. Strict storage at −20 °C is essential to maintain its structural integrity and biological activity. With its clear chemical profile and controllable physical and chemical stability, Lotilaner holds promising application prospects in veterinary and medical research, and provides a solid basis for subsequent formulation optimization and efficacy validation.
Frequently Asked Questions
- Is lotilaner the same as ivermectin?
Strikingly, our bioassays on human body lice demonstrated that the adulticide effect of lotilaner was higher than that of ivermectin and fipronil. Whereas 10 μM ivermectin treatment killed 100% of adult lice after 24h, we obtained the same result with 10 μM lotilaner in only 3 hours following exposure.
- Is lotilaner safe for humans?
Lotilaner was also safe and well tolerated, with no serious adverse events reported. For primary care providers, this study underscores the importance of recognizing collarettes as a key diagnostic marker for Demodex blepharitis during routine examinations.
- What class of drug is lotilaner?
Lotilaner belongs to the isoxazoline class of drugs and is a potent arthropod-selective gamma-aminobutyric acid-gated chloride ion channel inhibitor. Like several other drugs in the isoxazoline class, lotilaner has a long plasma half-life and high plasma protein binding of about 99.9%.
- What are the side effects of lotilaner?
Feeling like there is something in your eye;increased sensitivity of the eyes to light;swelling, redness, pain, or tenderness of the eyelid;tearing and irritation of the eye.
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