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| 25mg |
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Purity: ≥98%
Alcaftadine (R89674; R-89674; trade name Lastacaft) is a potent H1 histamine receptor antagonist used as a topical medication to prevent eye irritation caused by allergic conjunctivitis. It was approved by FDA in 2010 under the trade name Lastacaft. Alcaftadine is an antagonist at three of the histamine receptors (1, 2 and 4). The main indication for Alcaftadine is for prevention of allergic conjunctivitis. By blocking these four receptors, Alcaftadine has been shown to significantly reduce the effects of allergens.
| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
Based on data following oral administration of alcaftadine, the carboxylic acid metabolite is primarily eliminated unchanged in the urine. Metabolism / Metabolites The metabolism of alcaftadine is mediated by non-CYP450 cytosolic enzymes to the active carboxylic acid metabolite. Biological Half-Life The elimination half-life of the carboxylic acid metabolite is approximately 2 hours following topical ocular administration. |
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| Toxicity/Toxicokinetics |
Protein Binding
The protein binding of alcaftadine and the active metabolite are 39.2% and 62.7% respectively. |
| References |
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| Additional Infomation |
Alcaftadine is an imidazobenzazepine that is 6,11-dihydro-5H-imidazo[2,1-b][3]benzazepine substituted at position 3 by a formyl group and at position 11 by a 1-methylpiperidin-4-ylidene group. An antihistamine used for treatment of allergic conjunctivitis. It has a role as a H1-receptor antagonist and an anti-allergic agent. It is an aldehyde, a member of piperidines, an imidazobenzazepine and a tertiary amino compound.
Alcaftadine is a H1 histamine receptor antagonist indicated for the prevention of itching associated with allergic conjunctivitis. This drug was approved in July 2010. Alcaftadine is a Histamine-1 Receptor Antagonist. The mechanism of action of alcaftadine is as a Histamine H1 Receptor Antagonist. Drug Indication For the prevention of itching associated with allergic conjunctivitis. FDA Label Mechanism of Action Alcaftadine is a H1 histamine receptor antagonist and inhibitor of the release of histamine from mast cells. Decreased chemotaxis and inhibition of eosinophil activation has also been demonstrated. Pharmacodynamics Following bilateral topical ocular administration of alcaftadine ophthalmic solution, 0.25%, the mean plasma Cmax of alcaftadine was approximately 60 pg/mL and the median Tmax occurred at 15 minutes. Plasma concentrations of alcaftadine were below the lower limit of quantification (10 pg/mL) by 3 hours after dosing. The mean Cmax of the active carboxylic acid metabolite was approximately 3 ng/mL and occurred at 1 hour after dosing. Plasma concentrations of the carboxylic acid metabolite were below the lower limit of quantification (100 pg/mL) by 12 hours after dosing. |
| Molecular Formula |
C19H21N3O
|
|---|---|
| Molecular Weight |
307.3895
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| Exact Mass |
307.168
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| CAS # |
147084-10-4
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| PubChem CID |
19371515
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
556.2±60.0 °C at 760 mmHg
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| Melting Point |
167 °C
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| Flash Point |
290.2±32.9 °C
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| Vapour Pressure |
0.0±1.5 mmHg at 25°C
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| Index of Refraction |
1.663
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| LogP |
3.2
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
23
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| Complexity |
479
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
MWTBKTRZPHJQLH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H21N3O/c1-21-9-6-15(7-10-21)18-17-5-3-2-4-14(17)8-11-22-16(13-23)12-20-19(18)22/h2-5,12-13H,6-11H2,1H3
|
| Chemical Name |
2-(1-Methylpiperidin-4-ylidene)-4,7-diazatricyclo[8.4.0.0(3,7)]tetradeca- 1(14),3,5,10,12-pentaene-6-carbaldehyde
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| Synonyms |
R-89674; R 89674; R89674; Alcaftadine; trade name: Lastacaft;
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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 : ≥ 40 mg/mL (~130.13 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 | 3.2532 mL | 16.2660 mL | 32.5320 mL | |
| 5 mM | 0.6506 mL | 3.2532 mL | 6.5064 mL | |
| 10 mM | 0.3253 mL | 1.6266 mL | 3.2532 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 |
| NCT01808768 | Unknown status | Drug: Alcaftadine | Allergic Conjunctivitis Rhinoconjunctivitis |
Starx Research Center, LLC | 2013-04 | Phase 4 |
| NCT02555761 | Completed | Drug: Alcaftadine | Allergic Conjunctivitis Rhinoconjunctivitis |
Starx Research Center, LLC | 2013-04 | Phase 4 |
| NCT02555761 | Completed | Drug: Alcaftadine Ophthalmic Solution 0.25% | Conjunctivitis, Allergic | Allergan | 2015-10-19 | |
| NCT00889330 | Completed | Drug: alcaftadine Drug: Placebo |
Allergic Conjunctivitis | Vistakon Pharmaceuticals | 2009-04 | Phase 3 |
| NCT01732757 | Completed | Drug: Alcaftadine 0.25% Drug: Olopatadine 0.2% Drug: dextran 70 0.1%/hydroxypropyl methylcellulose 0.3% |
Conjunctivitis, Allergic | Allergan | 2012-11 | Phase 4 |
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