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| 10mg |
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Ablukast (Ro 23-3544) is a novel and potent leuktriene receptor antagonist with anti-asthmatic effects. It successfully lessens bronchoconstriction brought on by LTC4 and antigens.
| Targets |
LTD4
Peptidoleukotriene receptor antagonist (specifically antagonizes peptidoleukotrienes such as LTC4 and LTD4) [1] |
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|---|---|---|
| ln Vitro |
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| ln Vivo |
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| Animal Protocol |
Female BALB/c mice
Concentrations of 0.1 , 0.5 , 1.0 and 5.0 % of Ablukast Applied to one of the pretreated ears 1 h after elicitation and at 24 h intervals on the following 4 days; three times daily Female BALB/c mice were used. Allergic contact dermatitis was induced by sensitizing twice with 15 μl of 0.5% DNFB in acetone/olive oil (4:1) on the shaved abdomen. Two days later, dermatitis was elicited by painting both ears with 20 μl of 0.3% DNFB. Irritant contact dermatitis was induced by a single application of 0.5% croton oil in acetone/olive oil (4:1). Ablukast (Ro23-3544) was dissolved in polyethylene glycol (PEG) 400, and in some experiments in acetone/olive oil (4:1). Concentrations of 0.1%, 0.5%, 1.0%, and 5.0% of the antagonist were applied to one of the treated ears. Treatment started 1 hour after dermatitis elicitation and then at 24-hour intervals for the following 4 days (once daily). Another schedule was application of 5.0% three times daily. In pre-treatment experiments, ears were treated with 5.0% once daily for one week before dermatitis elicitation, with no additional treatment thereafter. After each treatment, ears were dried with a hair dryer. Ear thickness was measured with a spring-loaded micrometer prior to treatment and at 24 hours after each treatment for up to 5 days. Results were based on groups of 4 to 10 mice each. Statistical analysis used unpaired Student's t-test to compare experimental measurements with respective controls measured on the same day [1]. |
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| References | ||
| Additional Infomation |
Ablukast is an aromatic ketone.
Ablukast (Ro23-3544) is a specific peptidoleukotriene receptor antagonist. It effectively reduces LTC4- and antigen-induced bronchoconstriction in guinea pigs, but does not affect histamine- or platelet activating factor (PAF)-induced bronchoconstriction, indicating specificity for peptidoleukotrienes. The antagonist has some in vitro antichemotactic effects at high concentrations, but these are probably not significant in vivo. The drug is well tolerated in animal airways and human skin. In the murine contact dermatitis model, the antagonist suppressed allergic contact dermatitis during the early days of elicitation (first 3 days), with optimal effects when skin was pre-treated for several days before elicitation. No inhibitory effect was observed in irritant contact dermatitis; instead, an increase in ear swelling was noted. This suggests that peptidoleukotrienes play a role in the early stages of murine allergic contact dermatitis but not in irritant contact dermatitis [1]. |
| Molecular Formula |
C28H34O8
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|---|---|
| Molecular Weight |
498.57
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| Exact Mass |
498.225
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| Elemental Analysis |
C, 67.45; H, 6.87; O, 25.67
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| CAS # |
96566-25-5
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| Related CAS # |
96686-71-4 (S-isomer); 96686-73-6 (R-isomer); 96565-55-8 (sodium); 96566-25-5 (free acid)
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| PubChem CID |
57109
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| Appearance |
White to off-white solid powder
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| Density |
1.219g/cm3
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| Boiling Point |
730.8ºC at 760mmHg
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| Flash Point |
240.9ºC
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| Index of Refraction |
1.567
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| LogP |
5.156
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
13
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| Heavy Atom Count |
36
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| Complexity |
739
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(C1CCC2=CC(C(C)=O)=C(OCCCCCOC3=CC=C(C(C)=O)C(O)=C3CCC)C=C2O1)O
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| InChi Key |
FGGYJWZYDAROFF-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C28H34O8/c1-4-8-21-23(12-10-20(17(2)29)27(21)31)34-13-6-5-7-14-35-26-16-25-19(15-22(26)18(3)30)9-11-24(36-25)28(32)33/h10,12,15-16,24,31H,4-9,11,13-14H2,1-3H3,(H,32,33)
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| Chemical Name |
6-acetyl-7-[5-(4-acetyl-3-hydroxy-2-propylphenoxy)pentoxy]-3,4-dihydro-2H-chromene-2-carboxylic acid
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| Synonyms |
Ro-23-3544; Ro23-3544; Ablukast; Ro 23-3544/000; Ro 23-3544; Ro 233544; Ro-233544; Ro233544
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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 (~200.6 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (5.01 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.01 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0057 mL | 10.0287 mL | 20.0574 mL | |
| 5 mM | 0.4011 mL | 2.0057 mL | 4.0115 mL | |
| 10 mM | 0.2006 mL | 1.0029 mL | 2.0057 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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