| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
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| ln Vitro |
Amelubant is a prodrug of the active metabolites BIIL 260 and BIIL 315, which have Kis values of 1.4, 1.1 nM and 1.7, 1.9 nM in living cells and cell membranes, respectively. These metabolites are competitive and reversible LTB4 receptor antagonists [1].
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| References | |
| Additional Infomation |
Drug Indication
Investigated for use/treatment in asthma, chronic obstructive pulmonary disease (COPD), cystic fibrosis, and rheumatoid arthritis. Mechanism of Action Amelubant is a long-acting oral Leukotriene B4 (LTB4) receptor antagonist. Amelubant is a prodrug which is metabolized by ubiquitous esterases to BIIL 260 and its glucuronidated metabolite BIIL 315.14. BIIL 260 and BIIL 315.14 interact directly with the LTB4 receptors. LTB4 is a chemotactic factor for immune cells and potentiates the immune response. The G-protein coupled receptors BLT1, (high affinity for LTB4, expressed in most leukocytes) and BLT2 (low affinity for LTB4) are responsible for mediating LTB4's effects. |
| Molecular Formula |
C33H34N2O5
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|---|---|
| Molecular Weight |
538.644
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| Exact Mass |
568.294
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| CAS # |
346735-24-8
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| PubChem CID |
135564996
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| Appearance |
White to off-white solid powder
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| LogP |
8.512
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
12
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| Heavy Atom Count |
40
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| Complexity |
780
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
SBVYURPQULDJTI-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C33H34N2O5/c1-4-38-32(37)35-31(34)25-8-16-29(17-9-25)39-21-23-6-5-7-24(20-23)22-40-30-18-12-27(13-19-30)33(2,3)26-10-14-28(36)15-11-26/h5-20,36H,4,21-22H2,1-3H3,(H2,34,35,37)
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| Chemical Name |
ethyl N-[4-[[3-[[4-[2-(4-hydroxyphenyl)propan-2-yl]phenoxy]methyl]phenyl]methoxy]benzenecarboximidoyl]carbamate
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| Synonyms |
Amelubant BIIL-284-BS BIIL-284
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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 |
| 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 : ~100 mg/mL (~185.66 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 | 1.8565 mL | 9.2826 mL | 18.5653 mL | |
| 5 mM | 0.3713 mL | 1.8565 mL | 3.7131 mL | |
| 10 mM | 0.1857 mL | 0.9283 mL | 1.8565 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT02265653 | COMPLETED | Drug: BIIL 284 BS tablet C Drug: BIIL 284 BS tablet D Drug: BIIL 284 BS WIF tablet |
Healthy | Boehringer Ingelheim | 1999-11 | Phase 1 |
| NCT02265627 | COMPLETED | Drug: BIIL 284 BS | Hepatic Insufficiency | Boehringer Ingelheim | 2000-03 | Phase 1 |
| NCT02266550 | COMPLETED | Drug: [14C] BILL 284 BS | Healthy | Boehringer Ingelheim | 1999-10 | Phase 1 |
| NCT02265640 | COMPLETED | Drug: BIIL 284 BS boli Drug: BIIL 284 BS tablet C Other: standard breakfast |
Healthy | Boehringer Ingelheim | 2000-10 | Phase 1 |
| NCT02268149 | COMPLETED | Drug: BIIL 284 BS Drug: Prednisone Drug: Placebo |
Healthy | Boehringer Ingelheim | 2000-04 | Phase 1 |
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