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MedKoo Cat#: 314209 | Name: Alcaftadine
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Alcaftadine is used to prevent eye irritation brought on by allergic conjunctivitis. It is a H1 histamine receptor antagonist. It was approved by the U.S. Food and Drug Administration 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.

Chemical Structure

Alcaftadine
Alcaftadine
CAS#147084-10-4

Theoretical Analysis

MedKoo Cat#: 314209

Name: Alcaftadine

CAS#: 147084-10-4

Chemical Formula: C19H21N3O

Exact Mass: 307.1685

Molecular Weight: 307.39

Elemental Analysis: C, 74.24; H, 6.89; N, 13.67; O, 5.20

Price and Availability

Size Price Availability Quantity
25mg USD 350.00 2 Weeks
50mg USD 550.00 2 Weeks
100mg USD 850.00 2 Weeks
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Related CAS #
No Data
Synonym
R89674; R 89674; R-89674; Alcaftadine; trade name: Lastacaft;
IUPAC/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
InChi Key
MWTBKTRZPHJQLH-UHFFFAOYSA-N
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
SMILES Code
O=CC1=CN=C2/C(C3=CC=CC=C3CCN12)=C4CCN(C)CC/4
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO.
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info

Preparing Stock Solutions

The following data is based on the product molecular weight 307.39 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
1: Mahvan TD, Buckley WA, Hornecker JR. Alcaftadine for the prevention of itching associated with allergic conjunctivitis. Ann Pharmacother. 2012 Jul- Aug;46(7-8):1025-32. doi: 10.1345/aph.1Q755. Epub 2012 Jul 17. PMID: 22811343. 2: Ayyappanavar S, Sridhar S, Kumar K, Jayanthi CR, Gangasagara SB, Rathod BLS, Preethi B, Mittal P. Comparative analysis of safety and efficacy of Alcaftadine 0.25%, Olopatadine hydrochloride 0.2% and Bepotastine besilate 1.5% in allergic conjunctivitis. Indian J Ophthalmol. 2021 Feb;69(2):257-261. doi: 10.4103/ijo.IJO_2083_20. PMID: 33463568; PMCID: PMC7933849. 3: Namdar R, Valdez C. Alcaftadine: a topical antihistamine for use in allergic conjunctivitis. Drugs Today (Barc). 2011 Dec;47(12):883-90. doi: 10.1358/dot.2011.47.12.1709243. PMID: 22348913. 4: Drugs for allergic rhinitis and allergic conjunctivitis. Med Lett Drugs Ther. 2021 Apr 19;63(1622):57-64. PMID: 33848281. 5: Fujishima H, Hasunuma T, Kawakita T, Sekiya T, Gomes P, Hollander DA. Efficacy of Alcaftadine 0.25% (AGN-229666) for Once-daily Prevention of Cedar- Pollen Allergic Conjunctivitis: A Phase 3 Randomized Study. Ocul Immunol Inflamm. 2021 Nov 17;29(7-8):1621-1626. doi: 10.1080/09273948.2020.1760309. Epub 2020 Jun 5. PMID: 32501774. 6: Nakatani H, Gomes P, Bradford R, Guo Q, Safyan E, Hollander DA. Alcaftadine 0.25% versus Olopatadine 0.1% in Preventing Cedar Pollen Allergic Conjunctivitis in Japan: A Randomized Study. Ocul Immunol Inflamm. 2019;27(4):622-631. doi: 10.1080/09273948.2018.1432764. Epub 2018 Mar 15. PMID: 29543548. 7: Chigbu DI, Coyne AM. Update and clinical utility of alcaftadine ophthalmic solution 0.25% in the treatment of allergic conjunctivitis. Clin Ophthalmol. 2015 Jul 8;9:1215-25. doi: 10.2147/OPTH.S63790. PMID: 26185412; PMCID: PMC4501164. 8: In brief: OTC alcaftadine (Lastacaft Once Daily Relief) for allergic conjunctivitis. Med Lett Drugs Ther. 2022 May 16;64(1650):78. PMID: 35536123. 9: Simons FE, Simons KJ. Histamine and H1-antihistamines: celebrating a century of progress. J Allergy Clin Immunol. 2011 Dec;128(6):1139-1150.e4. doi: 10.1016/j.jaci.2011.09.005. Epub 2011 Oct 27. PMID: 22035879. 10: Abdel Razeq SA, Abdel Aziz SE, Ahmed NS. Stability-indicating UPLC, TLC- densitometric and UV-spectrophotometric methods for alcaftadine determination. J Chromatogr B Analyt Technol Biomed Life Sci. 2021 Jul 1;1177:122804. doi: 10.1016/j.jchromb.2021.122804. Epub 2021 May 27. PMID: 34098180. 11: Alcaftadine (Lastacaft) for allergic conjunctivitis. Med Lett Drugs Ther. 2011 Mar 7;53(1359):19-20. PMID: 21383667. 12: Bohets H, McGowan C, Mannens G, Schroeder N, Edwards-Swanson K, Shapiro A. Clinical pharmacology of alcaftadine, a novel antihistamine for the prevention of allergic conjunctivitis. J Ocul Pharmacol Ther. 2011 Apr;27(2):187-95. doi: 10.1089/jop.2010.0153. Epub 2011 Feb 12. PMID: 21314437. 13: McLaurin EB, Marsico NP, Ackerman SL, Ciolino JB, Williams JM, Villanueva L, Hollander DA. Ocular itch relief with alcaftadine 0.25% versus olopatadine 0.2% in allergic conjunctivitis: pooled analysis of two multicenter randomized clinical trials. Adv Ther. 2014 Oct;31(10):1059-71. doi: 10.1007/s12325-014-0155-3. Epub 2014 Sep 27. PMID: 25260889; PMCID: PMC4209090. 14: Ciolino JB, McLaurin EB, Marsico NP, Ackerman SL, Williams JM, Villanueva L, Hollander DA. Effect of alcaftadine 0.25% on ocular itch associated with seasonal or perennial allergic conjunctivitis: a pooled analysis of two multicenter randomized clinical trials. Clin Ophthalmol. 2015 May 2;9:765-72. doi: 10.2147/OPTH.S80503. PMID: 25999684; PMCID: PMC4427074. 15: Kim JH, Kim HJ, Kim SW. Allergic contact dermatitis of both eyes caused by alcaftadine 0.25%: a case report. BMC Ophthalmol. 2019 Jul 24;19(1):158. doi: 10.1186/s12886-019-1166-2. PMID: 31340775; PMCID: PMC6657074. 16: Hussar DA, Samuel J. Vilazodone hydrochloride, linagliptin, and alcaftadine. J Am Pharm Assoc (2003). 2011 Jul-Aug;51(4):557-9. doi: 10.1331/JAPhA.2011.11534. PMID: 21752782. 17: Ono SJ, Lane K. Comparison of effects of alcaftadine and olopatadine on conjunctival epithelium and eosinophil recruitment in a murine model of allergic conjunctivitis. Drug Des Devel Ther. 2011 Feb 8;5:77-84. doi: 10.2147/DDDT.S15788. PMID: 21340041; PMCID: PMC3038998. 18: Ackerman S, D'Ambrosio F Jr, Greiner JV, Villanueva L, Ciolino JB, Hollander DA. A multicenter evaluation of the efficacy and duration of action of alcaftadine 0.25% and olopatadine 0.2% in the conjunctival allergen challenge model. J Asthma Allergy. 2013 Apr 8;6:43-52. doi: 10.2147/JAA.S38671. PMID: 24109191; PMCID: PMC3792834. 19: Greiner JV, Edwards-Swanson K, Ingerman A. Evaluation of alcaftadine 0.25% ophthalmic solution in acute allergic conjunctivitis at 15 minutes and 16 hours after instillation versus placebo and olopatadine 0.1%. Clin Ophthalmol. 2011 Jan 13;5:87-93. doi: 10.2147/OPTH.S15379. PMID: 21339800; PMCID: PMC3037035. 20: Torkildsen G, Shedden A. The safety and efficacy of alcaftadine 0.25% ophthalmic solution for the prevention of itching associated with allergic conjunctivitis. Curr Med Res Opin. 2011 Mar;27(3):623-31. doi: 10.1185/03007995.2010.548797. Epub 2011 Jan 21. PMID: 21250860.

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