LTA4H-IN-1 |
Catalog No.GC63435
One-Click Copy Product Info
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LTA4H-IN-1 is a potent and highly selective leukotriene A4 hydrolase (LTA4H) inhibitor (IC50=2nM).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1799681-85-8
Sample solution is provided at 25 µL, 10mM.
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LTA4H-IN-1 is a potent and highly selective leukotriene A4 hydrolase (LTA4H) inhibitor (IC50=2nM). LTA4H-IN-1 can be used in research related to ulcerative colitis and non-alcoholic steatohepatitis[1-4].
In vitro, LTA4H-IN-1 (3.7nM) was used to pre-treat human peripheral blood mononuclear cells (PBMCs) for 4 hours, followed by stimulation with calcium ionophore. LTA4H-IN-1 inhibited LTB4 generation in the cells and reduced the inflammatory response[5].
In vivo, the day before modeling, LTA4H-IN-1 (LYS006) (3, 10, or 30mg/kg; twice a day; with 10h and 14h intervals) was orally administered to C57BL/6 mice with induced passive transfer arthritis for 7 consecutive days. LTA4H-IN-1 reduced the mice's combined paw swelling scores in a dose-dependent manner and significantly decreased inflammatory cell infiltration, tissue damage, and neutrophil infiltration in the joint tissues[5]. LTA4H-IN-1 (3mg/kg; once daily) was orally administered to fasted, approximately 2-year-old male beagle dogs for 5 consecutive days. LTA4H-IN-1 significantly inhibited LTB4 production in ex vivo stimulated blood[6].
References:
[1] Zhou X, Wang S, Yang X, et al. Optical Control of Leukotriene A4 Hydrolase Using Photoswitchable Inhibitors. J Med Chem. 2025 Oct 23;68(20):21520-21533.
[2] Frias J, Schmouder R, Lawitz E, et al. Clinical trial: A Phase 2 Randomised Platform Study to Assess Monotherapy and Combination Treatment Regimens in Metabolic Dysfunction-Associated Steatohepatitis. Aliment Pharmacol Ther. 2026 Mar;63(5):637-647.
[3] Poller B, Pearson D, Leuthold LA, et al. Human Pharmacokinetics of LYS006, an Oral Leukotriene A4 Hydrolase Inhibitor Displaying Target-Mediated Drug Disposition. Drug Metab Dispos. 2022 Dec;50(12):1472-1482.
[4] Loesche C, Picard D, Van Hoorick B, et al. LTA4H inhibitor LYS006: Clinical PK/PD and safety in a randomized phase I clinical trial. Clin Transl Sci. 2024 Feb;17(2):e13724.
[5] Thoma G, Markert C, Lueoend R, et al. Discovery of Amino Alcohols as Highly Potent, Selective, and Orally Efficacious Inhibitors of Leukotriene A4 Hydrolase. J Med Chem. 2023 Dec 14;66(23):16410-16425.
[6] Loesche C, Picard D, Van Hoorick B, et al. LTA4H inhibitor LYS006: Clinical PK/PD and safety in a randomized phase I clinical trial. Clin Transl Sci. 2024 Feb;17(2):e13724.
| Cell experiment [1]: | |
Cell lines | Human peripheral blood mononuclear cells (PBMCs) |
Preparation Method | PBMCs were stimulated with LTA4H-IN-1 for 4 hours, and treated with calcium ionophore to determine LTB4 production. |
Reaction Conditions | 3.7nM; 4h |
Applications | LTA4H-IN-1 significantly inhibited LTB4 generation in both PBMCs and whole blood. LTA4H-IN-1 elevated LXA4 biosynthesis in PBMCs via pathway shunting. |
| Animal experiment [1]: | |
Animal models | C57BL/6 mice (KRN serum passive transfer arthritis model) |
Preparation Method | On day 0, mice were intraperitoneally injected with arthritogenic KRN serum to induce passive transfer (antibody-mediated) arthritis. LTA4H-IN-1 was orally administered by gavage at 3, 10, or 30mg/kg twice daily (morning and evening doses spaced 10h and 14h apart, respectively), beginning on day −1 (one day before serum transfer) and continuing until day 6. |
Dosage form | 3, 10, or 30mg/kg; p.o.; twice daily of 7 days |
Applications | LTA4H-IN-1 dose-dependently reduced the composite claw swelling score. LTA4H-IN-1 significantly reduced inflammatory cell infiltrates, joint tissue destruction, and neutrophil infiltration within the arthritic paw/joint tissues compared with vehicle-treated arthritic controls. |
References: | |
| Cas No. | 1799681-85-8 | SDF | |
| Formula | C16H14ClFN6O3 | M.Wt | 392.77 |
| Solubility | DMSO : 250 mg/mL (636.50 mM; Need ultrasonic) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.546 mL | 12.7301 mL | 25.4602 mL |
| 5 mM | 509.2 μL | 2.546 mL | 5.092 mL |
| 10 mM | 254.6 μL | 1.273 mL | 2.546 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 34 reference(s) in Google Scholar.)