| Size | Price | Stock | Qty |
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| 1mg |
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| Targets |
BIIL-260 hydrochloride targets the leukotriene B4 (LTB4) receptor (BLT1), a key mediator of inflammatory responses. The compound exhibits high affinity for the LTB4 receptor on isolated human neutrophil membranes with a Ki value of 1.7 nM. It acts as a potent antagonist, interacting with the receptor in a saturable, reversible, and competitive manner. By blocking the LTB4 receptor, BIIL-260 hydrochloride inhibits LTB4-induced intracellular calcium release in human neutrophils with an IC50 of 0.82 nM, thereby modulating inflammatory responses.
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| ln Vitro |
BIIL-260 hydrochloride significantly suppresses LTB4-induced intracellular Ca2+ release in human neutrophils with an IC50 value of 0.82 nM.
In vitro, BIIL-260 hydrochloride binds to the LTB4 receptor on isolated human neutrophil membranes with high affinity, exhibiting a Ki value of 1.7 nM. The compound potently inhibits LTB4-induced intracellular Ca2+ release in human neutrophils with an IC50 of 0.82 nM. It interacts with the LTB4 receptor in a saturable, reversible, and competitive manner. These in vitro data demonstrate the compound's potent antagonism of the LTB4 receptor and its ability to block LTB4-mediated signaling in immune cells. |
| ln Vivo |
In vivo, BIIL-260 hydrochloride exhibits oral activity and anti-inflammatory properties. As a potent LTB4 receptor antagonist, the compound has been studied in animal models of inflammation. In monkey models, BIIL-260 hydrochloride has demonstrated efficacy in blocking LTB4-mediated inflammatory responses. The compound's oral bioavailability and potent antagonism of the LTB4 receptor make it a valuable tool for studying the role of LTB4 in inflammatory diseases. Detailed in vivo efficacy data are available in the scientific literature.
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| Enzyme Assay |
Receptor binding assays for BIIL-260 hydrochloride are performed using isolated human neutrophil membranes or membranes from cells expressing recombinant LTB4 receptors. Radioligand binding experiments are conducted using [3H]LTB4 as the tracer. Membranes are incubated with varying concentrations of BIIL-260 hydrochloride and a fixed concentration of [3H]LTB4 in binding buffer at room temperature or 4degC for a defined incubation period. Nonspecific binding is determined in the presence of excess unlabeled LTB4. Bound and free radioligands are separated by filtration, and radioactivity is measured by scintillation counting to calculate Ki values.
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| Cell Assay |
Cellular assays for BIIL-260 hydrochloride are performed using human neutrophils or other leukocytes. Cells are isolated from human blood and cultured in appropriate media. Cells are pre-treated with BIIL-260 hydrochloride at varying concentrations, then stimulated with LTB4. Intracellular calcium mobilization is measured using fluorescent calcium indicators such as Fura-2 or Fluo-4, and fluorescence is monitored using a plate reader or flow cytometry. The IC50 for inhibition of LTB4-induced calcium release is calculated from concentration-response curves.
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| Animal Protocol |
In vivo studies with BIIL-260 hydrochloride are conducted in rodent or monkey models of inflammation. The compound is administered via oral or intraperitoneal routes at defined doses. Inflammatory responses are induced by LTB4 administration or by other inflammatory stimuli. The compound's ability to block LTB4-mediated inflammation is assessed by measuring inflammatory markers, leukocyte infiltration, and tissue damage. Pharmacokinetic parameters are determined from plasma samples collected at various time points.
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| ADME/Pharmacokinetics |
BIIL-260 hydrochloride has a molecular weight of 503.03 and a molecular formula of C30H31ClN2O3. The compound is orally active and exhibits potent LTB4 receptor antagonism with a Ki of 1.7 nM. The compound is the bioactive metabolite of the prodrug BIIL. Detailed pharmacokinetic parameters, including oral bioavailability and half-life, are documented in the scientific literature. The compound is intended for research use and is not approved for clinical use.
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| Toxicity/Toxicokinetics |
Comprehensive toxicology data for BIIL-260 hydrochloride are not extensively documented in publicly available sources. The compound is intended for research use only and is not approved for human therapeutic applications. Standard laboratory safety practices should be followed when handling this compound, including the use of appropriate personal protective equipment and adherence to institutional biosafety and chemical hygiene guidelines. The compound has a purity of ≥98%.
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| References | |
| Additional Infomation |
BIIL-260 hydrochloride is a potent and orally active leukotriene B4 (LTB4) receptor antagonist with anti-inflammatory activity. It binds to the LTB4 receptor on human neutrophil membranes with a Ki of 1.7 nM and inhibits LTB4-induced intracellular Ca2+ release with an IC50 of 0.82 nM. The compound interacts with the receptor in a saturable, reversible, and competitive manner. BIIL-260 hydrochloride is a valuable tool for investigating leukotriene pathways and immune-mediated diseases. It is for research purposes only.
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| Molecular Formula |
C30H31CLN2O3
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|---|---|
| Molecular Weight |
503.0317
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| Exact Mass |
502.202
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| CAS # |
192581-24-1
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| Related CAS # |
204974-93-6;192581-24-1 (HCl);
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| PubChem CID |
23292598
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
36
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| Complexity |
644
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| Defined Atom Stereocenter Count |
0
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| SMILES |
Cl[H].O(C([H])([H])C1=C([H])C([H])=C([H])C(C([H])([H])OC2C([H])=C([H])C(/C(=N/[H])/N([H])[H])=C([H])C=2[H])=C1[H])C1C([H])=C([H])C(=C([H])C=1[H])C(C([H])([H])[H])(C([H])([H])[H])C1C([H])=C([H])C(=C([H])C=1[H])O[H]
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| InChi Key |
KYFHIWXKXUSXKB-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C30H30N2O3.ClH/c1-30(2,24-8-12-26(33)13-9-24)25-10-16-28(17-11-25)35-20-22-5-3-4-21(18-22)19-34-27-14-6-23(7-15-27)29(31)32;/h3-18,33H,19-20H2,1-2H3,(H3,31,32);1H
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| Chemical Name |
4-[[3-[[4-[2-(4-hydroxyphenyl)propan-2-yl]phenoxy]methyl]phenyl]methoxy]benzenecarboximidamide;hydrochloride
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~125 mg/mL (~248.49 mM)
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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 | 1.9880 mL | 9.9398 mL | 19.8795 mL | |
| 5 mM | 0.3976 mL | 1.9880 mL | 3.9759 mL | |
| 10 mM | 0.1988 mL | 0.9940 mL | 1.9880 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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