Sarolaner API

Sarolaner API

CAS No.1398609-39-6
Therapeutic CategoryAnthelmintic
TechnologySynthetic
Dosage FormChewable tablets/Topical Solution
Innovator BrandSimparica、Simparica Trio
Stronghold Plus
Revolution Plus
Registration StatusR&D
PolymorphN/A
GMPFDA(USA)/NMPA(China)/MFDS(Korea) approved
EHSISO 14001 & 45001 certified

Product Description

  • Grade: Active Pharmaceutical Ingredient(API)
  • ChemicalName: 1‑(5’-((5S)-5-(3,5-Dichloro-4-fluorophenyl)-5-trifluoromethyl)-4,5-dihydroisoxazol-3-yl)-3’-H-spiro(azetidine-3,1’-(2)benzofuran)-1-yl)-2-(methylsulfonyl)ethanone
  • Molecular Formula: C23H18Cl2F4N2O5S
  • Molecular Weight: 581.36
  • Specification: Enterprise Standard established according to ChP/USP/EP
  • Appearance: Powder
  • Total impurities: not more than 2.0%
  • Purity: not less than 98%
  • Residual Solvents: fully comply with ICH Q3C
  • Mutagenic impurities: fully comply with ICH M8
  • Nitrosamine assessment: available
  • Particle size: regular grade or milling/sieving according to customer’s requirement.
  • Storage: Room temperature
  • Production capacity: To be defined
  • Standard Package: 1kg/bag or according to the customer’s requirement

Applications of Sarolaner

  • Sarolaner is a broad-spectrum antiparasitic active ingredient used in veterinary medicine in pets against external parasites (fleastickslicemites, etc.). It is not used against agricultural and household pests. It belongs to the chemical class of the isoxazolines.
  • Type: veterinary medicine
  • Chemical classISOXAZOLINES
  • Type of action: Broad-spectrum, systemic ectoparasiticide: insecticide, tickicide, acaricide.
  • Main veterinary parasites controlledfleas, (Ctenocephalides felisCtenocephalides canis), ticks (EU: Dermacentor reticulatusIxodes ricinusIxodes hexagonus, Rhipicephalus sanguineus) and mites (Sarcoptes scabiei), screwworms (Cochliomyia hominivorax).
  • Efficacy against a specific parasite depends on the delivery form and on the dose administered.
  • Sarolaner is an insecticide and acaricide with systemic mode of action that belongs to the chemical class of the isoxazolines, a pesticide class introduced in 2013. It is available for oral administration (chewable tablets) to dogs for the control of fleasticks and a few other external parasites. It is ineffective against any kind of parasitic worms.
  • After afoxolaner and fluralaner, sarolaner was the third active ingredient belonging to the isoxazolines introduced as a veterinary antiparasitic. Isoxazolines are a new class of insecticides discovered in the 2000s. Whereas afoxolaner and fluralaner were licensed from other companies by MERIAL and MERCK AH, respectively, sarolaner was an own discovery and development of ZOETIS, the patent holder, and was selected as the best candidate among several thousand analogues.
  • Sarolaner is available in the form of chewable tablets for oral administration to dogs (SIMPARICA), i.e. it has a systemic mode of action. Ingested sarolaner is rapidly absorbed into blood and distributed throughout the whole body of the treated dog. Blood-sucking parasites (mainly fleas and ticks) are killed during their blood meal.
  • But the systemic mode of action means also that for fleas and/or ticks to be killed, they have to bite the dog first and suck enough blood before the ingested active ingredient kills them.
  • As other isoxazolines with insecticidal and tickicidal efficacy, afoxolaner is a non-competitive GABA (gamma-aminobutyric acid) receptor antagonist, much more selective for GABA receptors in insects or ticks, than for those in mammals, including humans. It binds to chloride channels in nerve and muscle cells, which blocks the transmission of neuronal signals. Affected parasites are paralyzed and die.
  • Sarolaner is highly effective against several flea and tick species at very low doses. In studies in vitro it showed to be about 10x more potent than other isoxazolines, with an LD80 of 0.3 mcg/ml =0.3 ppm) against fleas. In the EU, indications for the chewable tablets include control and prevention of fleas, (Ctenocephalides felisCtenocephalides canis), ticks (Dermacentor reticulatusIxodes ricinusIxodes hexagonus, Rhipicephalus sanguineus) and mites (Sarcoptes scabiei) after monthly administration. Contol od Sarcoptes scabiei is quite unique for sarolaner: other isoxazolines do not include this indication. Administered orally to dogs at a dose of 5 mg/kg it provides 5 to 4 weeks days efficacy against fleas and ticks, respectively.

Why Choose Us as Your Sarolaner Supplier?

  • Qingmu is a Leading Sarolaner Manufacturer, which manufactured under cGMP and can be supported for registration worldwide.
  • Our factory is established according to ICH/USFDA/EU/JAPAN/China regulations and current GMP, totally complies with environmental law in China, no risk to remove factory.
  • Qingmu’s team has rich experience in patent challenges on crystalline form & synthesis processes, synthetic route development, scale-up & quality research.
  • Qingmu’s lab is equipped with HPLC, GC, ICP-MS, GC-MS, CAD, microbalance, Malvern particle analyzer, etc. Qingmu passed the site inspection from NMPA(China), FDA(USA) and MFDS(Korea) and also customer audits from Europe, USA , Japan, etc. We are committed to producing the best quality products.
  • As a reliable Sarolaner factory, Qingmu successfully exported products to more than 40 countries including Japan, USA, Germany, Spain, the Netherlands, Russia, South Korea, and Brazil.

FAQ

A1: Negotiate via email→ sign the contract →ship the good

A2: We usually ship the goods by courier, Air, or Sea.

A3: We use Bag, Drum, Carton Box, Alu Tin, etc

A4: We have compliant SOP as per GMP requirement and will be handled according to SOP.

A5: Yes, we’re able to enlarge the batch size if current batch size couldn’t meet your requirement.

A6: