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MedKoo Cat#: 317777 | Name: Epinastine Hydrochloride
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Description:

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

Epinastine Hydrochloride is a histamine H1 receptor antagonist without sedative activity. Epinastine hydrochloride blocks the histamine H1 receptor and inhibits the release of histamine from mast cells. This prevents the typical allergic symptoms that are caused by histamine activity on capillaries, skin, and mucous membranes. Typical histamine activities include vasodilation, bronchoconstriction, increased vascular permeability, pain, itching, and spasmodic contractions of gastrointestinal smooth muscles. Epinastine HCl also has affinity for histamine H2, 5-HT2, and the alpha-1, alpha-2 adrenergic receptors.

Chemical Structure

Epinastine Hydrochloride
Epinastine Hydrochloride
CAS#108929-04-0 (HCl)

Theoretical Analysis

MedKoo Cat#: 317777

Name: Epinastine Hydrochloride

CAS#: 108929-04-0 (HCl)

Chemical Formula: C16H16ClN3

Exact Mass: 0.0000

Molecular Weight: 285.77

Elemental Analysis: C, 67.25; H, 5.64; Cl, 12.41; N, 14.70

Price and Availability

Size Price Availability Quantity
250mg USD 250.00 2 Weeks
500mg USD 450.00 2 Weeks
1g USD 750.00 2 Weeks
2g USD 1,150.00 2 Weeks
5g USD 2,150.00 2 Weeks
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Related CAS #
108929-04-0 (HCl) 80012-43-7 (free base) 127786-29-2 (HBr)
Synonym
Epinastine hydrochloride; Epinastine HCl; Alesion; Elestat; WAL 801; WAL-801; WAL801; WAL 801CL; WAL-801CL; WAL-801-CL
IUPAC/Chemical Name
3-Amino-9,13b-dihydro-1H-dibenzo[c,f]imidazo[1,5-a]azepine Hydrochloride
InChi Key
VKXSGUIOOQPGAF-UHFFFAOYSA-N
InChi Code
InChI=1S/C16H15N3.ClH/c17-16-18-10-15-13-7-3-1-5-11(13)9-12-6-2-4-8-14(12)19(15)16;/h1-8,15H,9-10H2,(H2,17,18);1H
SMILES Code
C1C2C3=CC=CC=C3CC4=CC=CC=C4N2C(=N1)N.Cl
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, not in water
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 285.77 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: Ariga GG, Naik PN, Nandibewoor ST, Chimatadar SA. Study of fluorescence interaction and conformational changes of bovine serum albumin with histamine H1 -receptor-drug epinastine hydrochloride by spectroscopic and time-resolved fluorescence methods. Biopolymers. 2015 Nov;103(11):646-57. doi: 10.1002/bip.22707. PubMed PMID: 26215421. 2: Fujishima H, Ohashi Y, Takamura E. Efficacy of epinastine hydrochloride ophthalmic solution in allergic conjunctivitis by conjunctival cedar pollen allergen challenge. Ann Allergy Asthma Immunol. 2014 Oct;113(4):476-81. doi: 10.1016/j.anai.2014.07.007. Epub 2014 Aug 20. PubMed PMID: 25163405. 3: Semsettin B, Sinan E, Nigar V. Comparison of the effects of topical cyclosporine a 0.05%, cyclosporine a 2%, epinastine hydrochloride 0.05%, and prednisolone acetate 1% on allergic inflammation in an experimental allergic conjunctivitis model. Cornea. 2013 Nov;32(11):1465-9. doi: 10.1097/ICO.0b013e3182a3655d. PubMed PMID: 24055903. 4: Gotoh M, Hashiguchi K, Okubo K. Efficacy of epinastine hydrochloride for antigen-provoked nasal symptoms in subjects with orchard grass pollinosis. Allergol Int. 2011 Mar;60(1):69-77. doi: 10.2332/allergolint.10-OA-0219. Epub 2011 Dec 25. PubMed PMID: 21173568. 5: Yilinuer H, Yamaoka J, Kawana S. Effect of epinastine hydrochloride on murine self-scratching behavior after skin-scratching stimulation. Arch Dermatol Res. 2010 Jan;302(1):19-26. doi: 10.1007/s00403-009-1006-y. Epub 2009 Nov 24. PubMed PMID: 19937255. 6: Asano K, Furuta A, Kanai K, Sakaue S, Suzaki H, Hisamitsu T. Inhibition of angiogenic factor production from murine mast cells by an antiallergic agent (epinastine hydrochloride) in vitro. Mediators Inflamm. 2008;2008:265095. doi: 10.1155/2008/265095. PubMed PMID: 18725994; PubMed Central PMCID: PMC2518221. 7: Mochizuki Y, Furuta A, Furuya A, Kanai K, Asano K, Suzaki H. Suppressive activity of epinastine hydrochloride on eosinophil activation in vitro. In Vivo. 2008 Jan-Feb;22(1):13-20. PubMed PMID: 18396776. 8: Ghisleni DD, Steppe M, Schapoval EE. Development and validation of liquid chromatographic and ultraviolet derivative spectrophotometric methods for determination of epinastine hydrochloride in coated tablets. J AOAC Int. 2007 Sep-Oct;90(5):1266-71. PubMed PMID: 17955971. 9: Toyoda M, Nakamura M, Nakagawa H. Distribution to the skin of epinastine hydrochloride in atopic dermatitis patients. Eur J Dermatol. 2007 Jan-Feb;17(1):33-6. Epub 2007 Feb 27. PubMed PMID: 17324825. 10: Kanai K, Asano K, Watanabe S, Kyo Y, Suzaki H. Epinastine hydrochloride antagonism against interleukin-4-mediated T cell cytokine imbalance in vitro. Int Arch Allergy Immunol. 2006;140(1):43-52. Epub 2006 Mar 13. PubMed PMID: 16534218. 11: Ohmura T, Kawasaki T. [Pharmacological and clinical profile of epinastine hydrochloride (Alesion Dry Syrup 1%)]. Nihon Yakurigaku Zasshi. 2006 Jan;127(1):37-46. Review. Japanese. PubMed PMID: 16508222. 12: Oshima KZ, Asano K, Kanai K, Suzuki M, Suzaki H. Influence of epinastine hydrochloride, an H1-receptor antagonist, on the function of mite allergen-pulsed murine bone marrow-derived dendritic cells in vitro and in vivo. Mediators Inflamm. 2009;2009:738038. doi: 10.1155/2009/738038. Epub 2009 Apr 9. PubMed PMID: 19381339; PubMed Central PMCID: PMC2667935. 13: Watase F, Watanabe S, Kanai K, Yamada N, Sakaue S, Asano K, Hisamitsu T, Suzaki H. Modulation of eosinophil survival by epinastine hydrochloride, an H1 receptor antagonist, in vitro. In Vivo. 2008 Nov-Dec;22(6):687-91. PubMed PMID: 19180992. 14: Hanashiro K, Sunagawa M, Tokeshi Y, Nakasone T, Ohta S, Nakamura M, Kosugi T. Antiallergic drugs, azelastine hydrochloride and epinastine hydrochloride, inhibit ongoing IgE secretion of rat IgE-producing hybridoma FE-3 cells. Eur J Pharmacol. 2006 Oct 10;547(1-3):174-83. Epub 2006 Jul 22. PubMed PMID: 16925996. 15: Kanai K, Asano K, Hisamitsu T, Suzaki H. Suppressive activity of epinastine hydrochloride on TARC production from human peripheral blood CD4+ T cells in-vitro. J Pharm Pharmacol. 2005 Aug;57(8):1027-36. PubMed PMID: 16102259. 16: Fraunfelder FW. Epinastine hydrochloride for atopic disease. Drugs Today (Barc). 2004 Aug;40(8):677-83. Review. PubMed PMID: 15510239. 17: Takahashi N, Aizawa H, Inoue H, Matsumoto K, Nakano H, Hirose T, Nishima S, Hara N. Effects of epinastine hydrochloride on cholinergic neuro-effector transmission in canine tracheal smooth muscle. Eur J Pharmacol. 1998 Sep 25;358(1):55-61. PubMed PMID: 9809869. 18: Nakagawa T, Kakinuma Y, Akitaya T, Shimada J, Mizushima Y. Modulatory effects of epinastine hydrochloride on IL-4 mRNA expression by peripheral blood mononuclear cells. Int Arch Allergy Immunol. 1997 May-Jul;113(1-3):321-2. PubMed PMID: 9130564.