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MedKoo Cat#: 412351 | Name: Carebastine
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Description:

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

Carebastine is an active carboxylic acid metablite of ebastine.

Chemical Structure

Carebastine
Carebastine
CAS#90729-42-3

Theoretical Analysis

MedKoo Cat#: 412351

Name: Carebastine

CAS#: 90729-42-3

Chemical Formula: C32H37NO4

Exact Mass: 499.2723

Molecular Weight: 499.65

Elemental Analysis: C, 76.92; H, 7.46; N, 2.80; O, 12.81

Price and Availability

Size Price Availability Quantity
10mg USD 350.00 2 Weeks
25mg USD 650.00 2 Weeks
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Related CAS #
No Data
Synonym
Carebastina; Carebastinum; Carebastine; Carebastinum
IUPAC/Chemical Name
Benzeneacetic acid, 4-(4-(4-(diphenylmethoxy)-1-piperidinyl)-1-oxobutyl)-alpha,alpha-dimethyl-
InChi Key
XGHOVGYJHWQGCC-UHFFFAOYSA-N
InChi Code
InChI=1S/C32H37NO4/c1-32(2,31(35)36)27-17-15-24(16-18-27)29(34)14-9-21-33-22-19-28(20-23-33)37-30(25-10-5-3-6-11-25)26-12-7-4-8-13-26/h3-8,10-13,15-18,28,30H,9,14,19-23H2,1-2H3,(H,35,36)
SMILES Code
O=C(O)C(C)(C)C1=CC=C(C(CCCN2CCC(OC(C3=CC=CC=C3)C4=CC=CC=C4)CC2)=O)C=C1
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
>3 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 499.65 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: Kingham P. Carebastine Almirall Prodesfarma. Curr Opin Investig Drugs. 2000 Sep;1(1):90-6. PMID: 11249602. 2: De Luisi A, Mangialardi G, Ria R, Acuto G, Ribatti D, Vacca A. Anti- angiogenic activity of carebastine: a plausible mechanism affecting airway remodelling. Eur Respir J. 2009 Oct;34(4):958-66. doi: 10.1183/09031936.00165308. Epub 2009 Apr 8. PMID: 19357149. 3: Tamai I, Kido Y, Yamashita J, Sai Y, Tsuji A. Blood-brain barrier transport of H1-antagonist ebastine and its metabolite carebastine. J Drug Target. 2000;8(6):383-93. doi: 10.3109/10611860008997914. PMID: 11328664. 4: Liu KH, Kim MG, Lee DJ, Yoon YJ, Kim MJ, Shon JH, Choi CS, Choi YK, Desta Z, Shin JG. Characterization of ebastine, hydroxyebastine, and carebastine metabolism by human liver microsomes and expressed cytochrome P450 enzymes: major roles for CYP2J2 and CYP3A. Drug Metab Dispos. 2006 Nov;34(11):1793-7. doi: 10.1124/dmd.106.010488. Epub 2006 Aug 8. PMID: 16896065. 5: Zhao Y, Makino T, Honda A, Shimizu H, Yamagishi S, Shimizu T. Carebastine, an H1-receptor antagonist, suppresses the expression of macrophage migration inhibitory factor. Clin Exp Dermatol. 2008 Nov;33(6):785-7. doi: 10.1111/j.1365-2230.2008.02843.x. Epub 2008 Aug 2. PMID: 18681878. 6: Phiri M, Li D, Li T, Ji S, Ling T, Li X, Gao H, Ding L, Shu C. Method development and validation for simultaneous determination of ebastine and its active metabolite carebastine in human plasma by liquid chromatography-tandem mass spectrometry and its application to a clinical pharmacokinetic study in healthy Chinese volunteers. Biomed Chromatogr. 2020 Oct;34(10):e4904. doi: 10.1002/bmc.4904. Epub 2020 Aug 7. PMID: 32449558. 7: Mazier C, Jaouen M, Sari MA, Buisson D. Microbial oxidation of terfenadine and ebastine into fexofenadine and carebastine. Bioorg Med Chem Lett. 2004 Nov 1;14(21):5423-6. doi: 10.1016/j.bmcl.2004.07.076. PMID: 15454238. 8: Lee MJ, Lee HW, Kang JM, Seo JH, Tak SK, Shim W, Yim SV, Hong SJ, Lee KT. Application of a rapid and selective method for the simultaneous determination of carebastine and pseudoephedrine in human plasma by liquid chromatography- electrospray mass spectrometry for bioequivalence study in Korean subjects. Biomed Chromatogr. 2010 Oct;24(10):1031-7. doi: 10.1002/bmc.1392. PMID: 20099369. 9: Van Rooij J, Schoemaker HC, Bruno R, Reinhoudt JF, Breimer DD, Cohen AF. Cimetidine does not influence the metabolism of the H1-receptor antagonist ebastine to its active metabolite carebastine. Br J Clin Pharmacol. 1993 Jun;35(6):661-3. doi: 10.1111/j.1365-2125.1993.tb04199.x. PMID: 8101096; PMCID: PMC1381613. 10: Matsuda M, Mizuki Y, Terauchi Y. Simultaneous determination of the histamine H1-receptor antagonist ebastine and its two metabolites, carebastine and hydroxyebastine, in human plasma using high-performance liquid chromatography. J Chromatogr B Biomed Sci Appl. 2001 Jun 5;757(1):173-9. doi: 10.1016/s0378-4347(00)00494-1. PMID: 11419742. 11: Yamaguchi T, Hashizume T, Matsuda M, Sakashita M, Fujii T, Sekine Y, Nakashima M, Uematsu T. Pharmacokinetics of the H1-receptor antagonist ebastine and its active metabolite carebastine in healthy subjects. Arzneimittelforschung. 1994 Jan;44(1):59-64. PMID: 7907873. 12: Saito J, Yakuwa N, Sandaiji N, Yagishita S, Kawasaki H, Suzuki T, Ozawa K, Kamura S, Yamatani A, Wada S, Sago H, Murashima A. Ebastine during pregnancy and lactation in a patient with chronic urticaria: ebastine and carebastine levels in maternal serum, cord blood, breast milk and the infant's serum. J Eur Acad Dermatol Venereol. 2020 Sep;34(9):e496-e497. doi: 10.1111/jdv.16415. Epub 2020 May 19. PMID: 32249465. 13: Matsuda M, Sakashita M, Mizuki Y, Yamaguchi T, Fujii T, Sekine Y. Comparative pharmacokinetics of the histamine H1-receptor antagonist ebastine and its active metabolite carebastine in rats, guinea pigs, dogs and monkeys. Arzneimittelforschung. 1994 Jan;44(1):55-9. PMID: 7907872. 14: Schwartz H, Liebig-Weber A, Hochstätter H, Böttcher H. Microbial oxidation of ebastine. Appl Microbiol Biotechnol. 1996 Feb;44(6):731-5. doi: 10.1007/BF00178610. PMID: 8867630. 15: Yamauchi Y, Fujikura T, Shimosawa T. The effect of H1 antagonists carebastine and olopatadine on histamine induced expression of CC chemokines in cultured human nasal epithelial cells. Allergol Int. 2007 Jun;56(2):171-7. doi: 10.2332/allergolint.O-06-446. Epub 2007 May 1. PMID: 17460445. 16: Noveck RJ, Preston RA, Swan SK. Pharmacokinetics and safety of ebastine in healthy subjects and patients with renal impairment. Clin Pharmacokinet. 2007;46(6):525-34. doi: 10.2165/00003088-200746060-00006. PMID: 17518511. 17: Simons FE, Watson WT, Simons KJ. Pharmacokinetics and pharmacodynamics of ebastine in children. J Pediatr. 1993 Apr;122(4):641-6. doi: 10.1016/s0022-3476(05)83555-3. PMID: 8096545. 18: Rohatagi S, Gillen M, Aubeneau M, Jan C, Pandit B, Jensen BK, Rhodes G. Effect of age and gender on the pharmacokinetics of ebastine after single and repeated dosing in healthy subjects. Int J Clin Pharmacol Ther. 2001 Mar;39(3):126-34. doi: 10.5414/cpp39126. PMID: 11396753. 19: Cavero I, Mestre M, Guillon JM, Heuillet E, Roach AG. Preclinical in vitro cardiac electrophysiology: a method of predicting arrhythmogenic potential of antihistamines in humans? Drug Saf. 1999;21 Suppl 1:19-31; discussion 81-7. doi: 10.2165/00002018-199921001-00004. PMID: 10597865. 20: Jansat JM, Lastra CF, Mariño EL. Comparative study of different weighting methods in non-linear regression analysis: implications in the parametrization of carebastine after intravenous administration in healthy volunteers. Int J Clin Pharmacol Ther. 1998 Jun;36(6):340-4. PMID: 9660043.