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Lotilaner (CAS 1369852-71-0, C₂₀H₁₄Cl₃F₆N₃O₃S, MW 596.76) is a chiral isoxazoline ectoparasiticide: white to off-white powder, practically water-insoluble, DMSO-soluble, stored dry/dark/cold. It selectively blocks arthropod GABA-gated chloride channels, killing fleas, ticks and mites while sparing mammals. Main uses: (1) vet API for monthly chewables (Credelio family) in dogs/cats; (2) human ophthalmic API in 0.25% eye drops (Xdemvy) for Demodex blepharitis; (3) pharmacology probe and LC-MS isotope internal standard. Selling points: dual market—recurring pet volume plus a growing human indication; only the (5S)-enantiomer is active (chiral-HPLC proof available); premium-priced isoxazoline class; impurity and D4-labeled standards supplied; cross-sell with fluralaner/afoxolaner/sarolaner intermediates. Note: H410 very toxic to aquatic life—contained handling and effluent control required; RUO/further-manufacturing use only; verify patent/FTO status by territory.
Specifications of Lotilaner CAS 1369852-71-0 COA:
Items | Specifications | Results |
Appearance | White to off-white crystalline powder | White crystalline powder |
Identification | HPLC retention time of main peak of sample solution should be identical with that of reference solution under the items of related substances. | Complies |
Water | NMT 1.0% | 0.05% |
Residue on ignition | NMT 0.1% | Less than 0.1% |
Related substances 1(HPLC) | A1025-50(S) NMT 0.15% | Not detected |
RRT about 0.83 NMT 0.15% | 0.08% | |
Other single impurities NMT 0.10% | 0.02% | |
Total impurities NMT 1.0% | 0.13% | |
Related substances 2(HPLC) | Enantiomer NMT 1.0% | 0.14% |
Residual solvents(GC) | 1,4-dioxane NMT 380ppm | Not detected |
Triethylamine NMT 5000ppm | 263ppm | |
Methyl tert butyl ether NMT 5000ppm | 716ppm | |
Ethanol NMT 5000ppm | 6ppm | |
Ethyl acetate NMT 5000ppm | 216ppm | |
Heptane NMT 5000ppm | 451ppm | |
2-butanol/Tetrahydrofuran NMT 720ppm | Not detected | |
Acetonitrile NMT 410ppm | Not detected | |
Toluene NMT 890ppm | Not detected | |
N-hexane NMT 290ppm | Not detected | |
Conclusion | The product conforms to the above specifications. | |
CAS:1369852-71-0
MF:
Melting point :
form:powder
color:White Crystalline
Uses:
| Item | Details |
|---|---|
| Chinese name | 洛替拉纳（也写作乐替拉纳） |
| English / INN | Lotilaner |
| CAS | 1369852-71-0（UNII: HEH4938D7K） |
| IUPAC | (S)-3-methyl-N-(2-oxo-2-((2,2,2-trifluoroethyl)amino)ethyl)-5-(5-(3,4,5-trichlorophenyl)-5-(trifluoromethyl)-4,5-dihydroisoxazol-3-yl)thiophene-2-carboxamide |
| Formula / MW | C₂₀H₁₄Cl₃F₆N₃O₃S / 596.76 |
| Appearance | White to off-white solid powder |
| Melting point | ~145–148 °C |
| Solubility | Practically insoluble in water; DMSO ≥100–150 mg/mL; soluble in organic solvents |
| Storage | Sealed, dry, dark; -20 °C long term (powder stable years); 2–8 °C short term |
| GHS | Warning: H400/H410 — very toxic to aquatic life with long lasting effects (P273/P391/P501) |
Lotilaner is a third-generation isoxazoline ectoparasiticide built on a 4,5-dihydroisoxazole (isoxazoline) core with a 3,4,5-trichlorophenyl + CF₃ quaternary center, a 3-methylthiophene-2-carboxamide, and a trifluoroethylamide tail. Only the (5S)-enantiomer is active. It acts as a potent non-competitive antagonist of arthropod GABA-gated chloride channels (and GluCl) — low-nM IC₅₀ at flea/tick receptors with >1000-fold selectivity over mammalian GABA_A receptors, so parasites hyperexcite, paralyze and die while the host is spared. PK features: high protein binding (>99%), large Vd, very slow elimination (half-life of weeks), and >80% oral bioavailability enhanced by food.
Commercially: CREDELIO / Credelio Plus / Credelio Quattro (Elanco) — monthly chewables for dogs and cats against fleas, ticks and mites; XDEMVY 0.25% ophthalmic solution (Tarsus, FDA-approved Jul 2023) — first-in-class treatment for Demodex blepharitis in humans.
2. Main uses
① Veterinary ectoparasiticide API (largest volume)
Oral chewable tablets for dogs/cats: kills Ctenocephalides felis (cat flea) and ticks (Rhipicephalus sanguineus, Ixodes ricinus, I. hexagonus, Dermacentor reticulatus, Amblyomma americanum), starts killing within hours and persists ~30 days/monthly dosing; also used against Demodex mange mites, and as part of flea-allergy dermatitis control programs. In Credelio Quattro it's combined with moxidectin, praziquantel and pyrantel for broad-spectrum coverage.
② Human ophthalmic API — Demodex blepharitis (fastest-growing, highest-value)
Xdemvy 0.25% eye drops, one drop in each eye twice daily for 6 weeks; first drug specifically targeting Demodex mites on eyelashes. Drives demand for ophthalmic-grade/low-impurity lotilaner, sterile-filtration-suitable material and tight genotoxic/elemental-impurity control.
③ Research reagent & pharmacology probe
Sold by MCE/MedKoo/TargetMol etc. as a GABA_Cl receptor antagonist reference (IC₅₀ ~24 nM DmS-GABA; active vs dieldrin/fipronil-resistant forms, Lepeophtheirus salmonis, Rhipicephalus microplus). Used in 10 mM DMSO solutions for in-vitro assays, resistance studies and comparative isoxazoline profiling.
④ Analytical standards & impurities
Lotilaner related substances/impurity standards, enantiomer reference, D4-lotilaner stable isotope internal standard for LC-MS/MS residue analysis in plasma, tissues, pet food and environmental matrices — small packs, very high margin.
⑤ Other arthropod-control R&D
Lead/scaffold for livestock ectoparasite, aquaculture sea-lice and vector-control programs; also a benchmark molecule in new isoxazoline design.
3. Selling points
A. Market-side
Two engines, one molecule: recurring pet-care volume (monthly chewables, global generics pipeline) + a novel human ophthalmic franchise with large addressable population (~tens of millions of Demodex blepharitis-suspect patients) → demand growth beyond the saturated vet-only story.
Patent cliff opportunity: core compound patents expiring around the end of this decade (formulation/method patents later) → generic API and intermediate interest rising; early-qualification customers want qualified sources now. (Verify FTO/patent status and territorial freedom before quoting.)
Premium price tier: isoxazoline APIs command far higher $ /kg than legacy pyrethroids/organophosphates; ophthalmic-grade commands an additional premium over technical grade.
B. Quality/technical levers buyers actually check
4. Chiral purity: only (5S) is active — offer enantiomeric excess/chiral HPLC control and a validated chiral method; this is your strongest technical differentiator vs. racemic or enriched material.
5. Spec discipline: assay ≥98.5–99.5% (HPLC), single unknown ≤0.10%, residual solvents (esp. halogenated), Pd/metal catalyst residues, heavy metals, water, ash; for ophthalmic grade add bacterial endotoxin/bioburden, elemental impurities (ICH Q3D), nitrosamine risk assessment and particle-size/PSD for dissolution.
6. Impurity & isotope portfolio: supply the impurity set (including the R-enantiomer) and D4-labeled IS — lets you be a one-stop source for both API and analytical departments.
7. Documentation pack: CoA, HPLC/GC chromatograms, NMR/IR/MS, chiral report, SDS, residual solvent, TSE/BSE-free, non-GMO, origin statement; for vet-API routes, support DMF/CEP-type filings and stability data/retest period.
8. Grade ladder: research/reference (mg–g) → technical/vet-intermediate → vet-API grade → ophthalmic-grade candidate; margin scales with documentation, not just tonnage.
C. Supply & service
9. Scalable route know-how: isoxazoline formation from the trichlorophenyl-CF₃ ketone + hydroxylamine-type cyclization, thiophene amide coupling, and chiral resolution/asymmetric step — ability to control the key quaternary stereocenter cost-effectively is the real moat; offer process-IP-clean, non-infringing routes.
10. Cross-sell the class: fluralaner, afoxolaner, sarolaner, esafoxolaner intermediates and the shared building blocks (3,4,5-trichlorobenzoyl derivatives, trifluoroethylamine, methylthiophene acids) — one inquiry becomes a program.
11. Handling/logistics: non-volatile solid, long shelf life when dry/dark/cold; small packs ship easily (note: not classified for transport in most cases but verify; always flag aquatic hazard).
4. Risks worth disclosing
Aquatic toxicity (H410): isoxazolines are highly toxic to aquatic life and persistent; manufacture needs contained handling, scrubbed effluent and no environmental release. This drives customer EHS audits and may limit where you can make it.
Neurotoxicity class label: FDA/EMA warn of tremors, ataxia, seizures; caution in MDR1/ABCB1-mutant dogs, epileptics, and with P-gp inhibitors. For API suppliers this means tight spec control and clean labeling — never dilute safety info.
Chirality risk: any R-enantiomer or epimerization during synthesis directly erodes potency and complicates registration; lock the asymmetric step and validate the chiral method.
Solubility/formulation limits: essentially water-insoluble → ophthalmic and chewable formulations need solubilizers/surfactants; your PSD and polymorph consistency affect their bioavailability and dissolution testing.
Commercial reality: dominated by Elanco/Tarsus with strong brands; the near-term API market is qualification-driven and lumpy, and Chinese/Indian competition on price is intense. Margin lives in chiral proof, ophthalmic-grade capability, impurity/isotope standards and filing support — not in commodity pricing.
Compliance boundary: RUO for research material; vet-API/pharma grades require appropriate filings. Do not make efficacy claims for the raw material; avoid asserting "patent-free" without a territory-specific FTO opinion.
Also, if you have any other questions, you can contact us
FAQ From Wuhan Fortuna Chemical Co.,Ltd
Q1: Can I get a sample for free ?
A: For small QTY and low value product, we can provide sample for free exclude shipping cost. For high value sample, we will charge the basic sample cost, but we can refund all the cost if customers place order after sample test.
Q2: How to confirm the product quality before placing orders ?
A: Most of our products confirm to international standards like USP/EP/BP/JP/CP. We will provide COA/TDS/MSDS for customers to confirm the specification before placing order.
Q3: What is the payment you accept?
A: For small and low value order, we accept CreditCard, MaterCard,VISA,Western Union and T/T.For large order, we can do T/T and L/C. Any pay on delivery or pay-after are not available for us.
Q4: What is your shipment way ?
A: For less than 100kg gross weight order will ship with courier like FedEx or UPS, we support customers to place courier orders remotely by their account, we will package the goods well and wait for pick up.For more than 100kg goods, we will transport by Air or Sea according to customers' requirement.
Q5: How long is your after-sales service?
A: We accept customer’s quality complaint in three month after customer received the goods. We provide tech.support for all-life if customer place order from our company.
Q6: How do you treat quality complaint ?
A: We support customer to provide our products to any rightful third party testing organization to test our products according to the COA specification, if the test result is confirm with COA, we will take all the loss for customers.
Name:Wuhan Fortuna Chemical Co.,Ltd
Category:Others
Trade Category: Trading Company
Employees: 11 - 50 People
Address: Room 2015, No.2 Building, Kaixin Mansion No.107
Company Information: Wuhan Fortuna Chemical Co.,Ltd established in 2006, is a big integrative chemical enterprise being engaged in Pharmaceutical and Intermediates, Food and Feed additives, Fine chemicals,Biochemical and Reagent, which is the members of Hubei E-commerce Chamber.
Our company has professional persons who major in chemical R&D and sicentific management, supply fine chemical products with high quality and close service, also supply custom-tailored products according to our clients' requirement.
We have a positive and self-motivated management work team with a common philosophy, caring and commitment through teamwork, our team strive to achieve success in delighting our clients and ourselves.
Since Wuhan Fortuna Chemical Co., Ltd founded, we continuously innovate our products and improve our service, sales network. Hence, we initiate the first sale mode on net in China, which is the retail trade of small package bring along wholesale of diversified management modes. Our products are exported widely to South Korea, Vietnam, Australia, Europe and South America, highly recommended by our clients.We insist on the management creed “Market is our compass, Quality is our life, Credit is our soul”. Clients’ trust is our forward power, their satisfaction is our struggling goal.
Wuhan Fortuna Chemical Co.,Ltd is a professional manufacturer which provide Lotilaner with good quality and best price, welcome to contact us to get COA/TDS/MSDS of Lotilaner.
1. Guaranteed purity;
2. Large quantity in stock;
3. Largest manufacturer;
4. Best service after shipment with email;
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