| Size | Price | Stock | Qty |
|---|---|---|---|
| 25mg |
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| Targets |
L-674573 targets 5-lipoxygenase-activating protein (FLAP), an integral membrane protein that is essential for the activity of 5-lipoxygenase (5-LO). FLAP facilitates the transfer of arachidonic acid to 5-LO, enabling the synthesis of leukotrienes. By binding to FLAP, L-674573 specifically inhibits its function, preventing the translocation of 5-LO to the nuclear membrane and thereby blocking the biosynthesis of leukotrienes. This mechanism is distinct from direct inhibition of the 5-LO enzyme itself.
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|---|---|
| ln Vitro |
In vitro, L-674573 is a potent inhibitor of leukotriene biosynthesis. It inhibits Calcimycin- and N-Formyl-Met-Leu-Phe-induced leukotriene production with IC₅₀ values of 100 nM and 50 nM, respectively. It specifically inhibits the labeling of an 18-kDa protein, identified as FLAP, in a concentration-dependent manner with an IC₅₀ of 70 nM. These in vitro activities confirm its mechanism as a FLAP inhibitor and its potent anti-leukotriene effects.
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| ln Vivo |
Detailed in vivo activity data for L-674573 are not extensively reported in the available literature. However, as a potent inhibitor of leukotriene biosynthesis, it is expected to have in vivo efficacy in models of inflammation and other leukotriene-driven diseases. Its applications include in vivo models of inflammation. Further in vivo studies would be required to fully characterize its therapeutic potential.
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| Enzyme Assay |
Non-cell-based assays for L-674573 include FLAP binding assays using membrane preparations from cells expressing FLAP. The compound is incubated with a radiolabeled FLAP ligand and varying concentrations of L-674573. Its binding affinity (IC₅₀) is determined by measuring the displacement of the radiolabeled ligand. The IC₅₀ for labeling the 18-kDa protein is 70 nM. Leukotriene synthesis inhibition can be assessed using cell-free systems with purified enzymes.
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| Cell Assay |
Cellular assays for L-674573 are performed using various cell types, such as leukocytes, to assess its effects on leukotriene production. Cells are stimulated with Calcimycin or N-Formyl-Met-Leu-Phe to induce leukotriene synthesis. The compound is added at various concentrations, and the levels of leukotrienes in the supernatant are measured by ELISA. Its ability to inhibit leukotriene production is quantified, with IC₅₀ values of 100 nM and 50 nM, respectively.
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| Animal Protocol |
In vivo animal models for L-674573 include models of inflammation, such as carrageenan-induced paw edema or models of asthma. The compound is administered via appropriate routes, and inflammatory markers, leukotriene levels, and other relevant endpoints are measured. These studies are crucial for evaluating the compound's in vivo efficacy. Detailed protocols are not extensively reported.
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| ADME/Pharmacokinetics |
L-674573 has a molecular weight of 457.58 g/mol and a molecular formula of C₂₈H₂₇NO₃S. Its CAS number is 127481-29-2. The compound is supplied as a solid with a purity of >99%. It is soluble in DMSO (10 mg/mL). Storage conditions: 4°C, protected from light. Detailed pharmacokinetic parameters such as half-life and bioavailability are not extensively reported.
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| Toxicity/Toxicokinetics |
Detailed toxicological data for L-674573 are not extensively reported in the available literature. As a research compound, its safety profile would need to be established through standard preclinical toxicity assessments. The compound is intended for research use only and is not for human consumption. Standard laboratory safety precautions should be followed when handling the compound.
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| References | |
| Additional Infomation |
L-674573 is a quinoline leukotriene synthesis inhibitor. It targets 5-lipoxygenase-activating protein (FLAP) and specifically inhibits the labeling of an 18-kDa protein with an IC₅₀ of 70 nM. It inhibits Calcimycin- and N-Formyl-Met-Leu-Phe-induced leukotriene production with IC₅₀ values of 100 nM and 50 nM, respectively. L-674573 is used in research on inflammatory pathways. Its CAS number is 127481-29-2.
|
| Molecular Formula |
C28H27NO3S
|
|---|---|
| Molecular Weight |
457.58
|
| Exact Mass |
457.171
|
| CAS # |
127481-29-2
|
| Related CAS # |
127481-29-2 (free);AZD-4769 sodium;
|
| PubChem CID |
124437
|
| Appearance |
White to off-white solid powder
|
| Density |
1.235g/cm3
|
| Boiling Point |
656ºC at 760 mmHg
|
| Flash Point |
350.5ºC
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| Vapour Pressure |
4.2E-18mmHg at 25°C
|
| Index of Refraction |
1.652
|
| LogP |
6.695
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
11
|
| Heavy Atom Count |
33
|
| Complexity |
574
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
JOIXGLLMSDPZDN-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C28H27NO3S/c30-28(31)20-33-27(12-6-9-21-7-2-1-3-8-21)23-14-17-25(18-15-23)32-19-24-16-13-22-10-4-5-11-26(22)29-24/h1-5,7-8,10-11,13-18,27H,6,9,12,19-20H2,(H,30,31)
|
| Chemical Name |
2-[4-phenyl-1-[4-(quinolin-2-ylmethoxy)phenyl]butyl]sulfanylacetic acid
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| Synonyms |
L674573 AZD4769 L-674573AZD-4769 AZD 4769L 674573
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| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1854 mL | 10.9271 mL | 21.8541 mL | |
| 5 mM | 0.4371 mL | 2.1854 mL | 4.3708 mL | |
| 10 mM | 0.2185 mL | 1.0927 mL | 2.1854 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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