Mizolastine | CAS#108612-45-9 | antihistamine

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

MedKoo CAT#: 584735

CAS#: 108612-45-9

Description: Mizolastine is a selective histamine H1 receptor antagonist.

Chemical Structure

Mizolastine

CAS# 108612-45-9

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 584735
Name: Mizolastine
CAS#: 108612-45-9
Chemical Formula: C24H25FN6O
Exact Mass: 432.21
Molecular Weight: 432.503
Elemental Analysis: C, 66.65; H, 5.83; F, 4.39; N, 19.43; O, 3.70

Price and Availability

Size	Price	Availability	Quantity
1g	USD 350	2 Weeks
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

Synonym: Mizollen; SL 85.0324; Mistalin; Mistamine; Mizolastina; Mizolastine

IUPAC/Chemical Name: 2-((1-(1-(p-Fluorobenzyl)-2-benzimidazolyl)-4-piperidyl)methylamino)-4(3H)-pyrimidinone

InChi Key: PVLJETXTTWAYEW-UHFFFAOYSA-N

InChi Code: InChI=1S/C24H25FN6O/c1-29(23-26-13-10-22(32)28-23)19-11-14-30(15-12-19)24-27-20-4-2-3-5-21(20)31(24)16-17-6-8-18(25)9-7-17/h2-10,13,19H,11-12,14-16H2,1H3,(H,26,28,32)

SMILES Code: O=C1NC(N(C2CCN(C3=NC4=CC=CC=C4N3CC5=CC=C(F)C=C5)CC2)C)=NC=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

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Product Data:

Product Data

Instruction:

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Biological target:	Mizolastine is a histamine H1 receptor antagonist (second generation antihistamine).
In vitro activity:	This study investigated the influence of MIZ (mizolastine) on proangiogenesis factors, vascular endothelial cell growth factor (VEGF), tumour necrosis factor (TNF)-alpha and keratinocyte-derived chemokine (KC) in murine mast cells by using ELISA and RT-PCR, as compared with dexamethasone (DEX) and loratadine (LOR). These results show that MIZ is effective in the inhibition of KC, VEGF and TNF-alpha release induced by an IgE-dependent mechanism, in a time- and dose-dependent manner. Reference: Clin Exp Dermatol. 2005 Mar;30(2):165-70. https://pubmed.ncbi.nlm.nih.gov/15725247/
In vivo activity:	In the current study, the capacity of YNB (Yunnan Baiyao) to ameliorate inflammation was compared in carrageenan‑induced and AA‑induced acute inflammation of the rat paw with celecoxib and mizolastine, respectively (n=24 per group). Celecoxib ameliorated carrageenan‑induced paw edema, and mizolastine ameliorated AA‑induced rat paw edema. Reference: Mol Med Rep. 2017 Oct;16(4):4045-4053. https://pubmed.ncbi.nlm.nih.gov/28765972/

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	25.0	57.80
	Chloroform	10.0	23.12
	Water	1.0	2.31

Preparing Stock Solutions

The following data is based on the product molecular weight 432.50 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.

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

Formulation protocol:	1. Yan Y, Wang B, Zuo YG, Qu T. Inhibitory effects of mizolastine on ultraviolet B-induced leukotriene B4 production and 5-lipoxygenase expression in normal human dermal fibroblasts in vitro. Photochem Photobiol. 2006 May-Jun;82(3):665-9. doi: 10.1562/2005-08-17-RA-652. PMID: 16402861. 2. Xia Q, Yang S, Zhang SQ, Chen B, Wang DB, Zhu QX, Wang Y, Yan KL, He PP, Zhang XJ. The effect of mizolastine on expression of vascular endothelial cell growth factor, tumour necrosis factor-alpha and keratinocyte-derived chemokine in murine mast cells, compared with dexamethasone and loratadine. Clin Exp Dermatol. 2005 Mar;30(2):165-70. doi: 10.1111/j.1365-2230.2005.01721.x. PMID: 15725247. 3. Ren X, Zhang M, Chen L, Zhang W, Huang Y, Luo H, Li L, He H. The anti-inflammatory effects of Yunnan Baiyao are involved in regulation of the phospholipase A2/arachidonic acid metabolites pathways in acute inflammation rat model. Mol Med Rep. 2017 Oct;16(4):4045-4053. doi: 10.3892/mmr.2017.7104. Epub 2017 Jul 27. PMID: 28765972; PMCID: PMC5647098. 4. Goldhill J, Pichat P, Roome N, Angel I, Arbilla S. Effect of mizolastine on visceral sensory afferent sensitivity and inflammation during experimental colitis. Arzneimittelforschung. 1998 Feb;48(2):179-84. PMID: 9541730.
In vitro protocol:	1. Yan Y, Wang B, Zuo YG, Qu T. Inhibitory effects of mizolastine on ultraviolet B-induced leukotriene B4 production and 5-lipoxygenase expression in normal human dermal fibroblasts in vitro. Photochem Photobiol. 2006 May-Jun;82(3):665-9. doi: 10.1562/2005-08-17-RA-652. PMID: 16402861. 2. Xia Q, Yang S, Zhang SQ, Chen B, Wang DB, Zhu QX, Wang Y, Yan KL, He PP, Zhang XJ. The effect of mizolastine on expression of vascular endothelial cell growth factor, tumour necrosis factor-alpha and keratinocyte-derived chemokine in murine mast cells, compared with dexamethasone and loratadine. Clin Exp Dermatol. 2005 Mar;30(2):165-70. doi: 10.1111/j.1365-2230.2005.01721.x. PMID: 15725247.
In vivo protocol:	1. Ren X, Zhang M, Chen L, Zhang W, Huang Y, Luo H, Li L, He H. The anti-inflammatory effects of Yunnan Baiyao are involved in regulation of the phospholipase A2/arachidonic acid metabolites pathways in acute inflammation rat model. Mol Med Rep. 2017 Oct;16(4):4045-4053. doi: 10.3892/mmr.2017.7104. Epub 2017 Jul 27. PMID: 28765972; PMCID: PMC5647098. 2. Goldhill J, Pichat P, Roome N, Angel I, Arbilla S. Effect of mizolastine on visceral sensory afferent sensitivity and inflammation during experimental colitis. Arzneimittelforschung. 1998 Feb;48(2):179-84. PMID: 9541730.

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1: Molimard M, Diquet B, Benedetti MS. Comparison of pharmacokinetics and metabolism of desloratadine, fexofenadine, levocetirizine and mizolastine in humans. Fundam Clin Pharmacol. 2004 Aug;18(4):399-411. Review. PubMed PMID: 15312146.

2: Xia Q, Zhou WM, Yang S, Zhang SQ, Chen B, Wang DB, Wang Y, Zhang XJ. Influence of mizolastine on antigen-induced activation of signalling pathways in murine mast cells. Clin Exp Dermatol. 2006 Mar;31(2):260-5. PubMed PMID: 16487106.

3: Paśko P, Rodacki T, Domagała-Rodacka R, Palimonka K, Marcinkowska M, Owczarek D. Second generation H1 - antihistamines interaction with food and alcohol-A systematic review. Biomed Pharmacother. 2017 Sep;93:27-39. doi: 10.1016/j.biopha.2017.06.008. Epub 2017 Jun 13. Review. PubMed PMID: 28622592.

4: Bellioni P, Catalano B, Cervellera G, Filiaci F, Mira E, Carraro A. Comparison of mizolastine with loratadine in the treatment of perennial allergic rhinitis. Rhinology. 1996 Jun;34(2):101-4. PubMed PMID: 8876072.

5: Scadding GK, Tasman AJ, Murrieta-Aguttes M, Bachert C. Mizolastine is effective and well tolerated in long-term treatment of perennial allergic rhinoconjunctivitis. Riperex Study Group. J Int Med Res. 1999;27(6):273-85. PubMed PMID: 10726236.

6: Lebrun-Vignes B, Diquet B, Chosidow O. Clinical pharmacokinetics of mizolastine. Clin Pharmacokinet. 2001;40(7):501-7. Review. PubMed PMID: 11510627.

7: Simons FE. Mizolastine: antihistaminic activity from preclinical data to clinical evaluation. Clin Exp Allergy. 1999 Mar;29 Suppl 1:3-8. Review. PubMed PMID: 10209699.

8: Grundmann JU, Böckelmann R, Bonnekoh B, Gollnick HP. UV erythema reducing capacity of mizolastine compared to acetylsalicylic acid or both combined in comparison to indomethacin. Photochem Photobiol. 2001 Oct;74(4):587-92. PubMed PMID: 11683039.

9: Feng S, Nie L, Zou P, Suo J. Drug-loaded PLGA-mPEG microparticles as treatment for atopic dermatitis-like skin lesions in BALB/c mice model. J Microencapsul. 2015;32(2):201-9. doi: 10.3109/02652048.2014.995727. Epub 2014 Dec 24. PubMed PMID: 25539424.

10: Dubertret L, Murrieta Aguttes M, Tonet J. Efficacy and safety of mizolastine 10 mg in a placebo-controlled comparison with loratadine in chronic idiopathic urticaria: results of the MILOR Study. J Eur Acad Dermatol Venereol. 1999 Jan;12(1):16-24. PubMed PMID: 10188144.

11: Bachert C, Brostoff J, Scadding GK, Tasman J, Stalla-Bourdillon A, Murrieta M. Mizolastine therapy also has an effect on nasal blockade in perennial allergic rhinoconjunctivitis. RIPERAN Study Group. Allergy. 1998 Oct;53(10):969-75. PubMed PMID: 9821477.

12: Patat A, Perault MC, Vandel B, Ulliac N, Zieleniuk I, Rosenzweig P. Lack of interaction between a new antihistamine, mizolastine, and lorazepam on psychomotor performance and memory in healthy volunteers. Br J Clin Pharmacol. 1995 Jan;39(1):31-8. PubMed PMID: 7756096; PubMed Central PMCID: PMC1364978.

13: Triggiani M, Giannattasio G, Balestrieri B, Granata F, Gelb MH, de Paulis A, Marone G. Differential modulation of mediator release from human basophils and mast cells by mizolastine. Clin Exp Allergy. 2004 Feb;34(2):241-9. PubMed PMID: 14987304.

14: Delauche-Cavallier MC, Chaufour S, Guérault E, Lacroux A, Murrieta M, Wajman A. QT interval monitoring during clinical studies with mizolastine, a new H1 antihistamine. Clin Exp Allergy. 1999 Jul;29 Suppl 3:206-11. PubMed PMID: 10444239.

15: Brostoff J, Fitzharris P, Dunmore C, Theron M, Blondin P. Efficacy of mizolastine, a new antihistamine, compared with placebo in the treatment of chronic idiopathic urticaria. Allergy. 1996 May;51(5):320-5. PubMed PMID: 8836336.

16: Sharma M, Bennett C, Cohen SN, Carter B. H1-antihistamines for chronic spontaneous urticaria. Cochrane Database Syst Rev. 2014 Nov 14;(11):CD006137. doi: 10.1002/14651858.CD006137.pub2. Review. PubMed PMID: 25397904.

17: Leynadier F, Duarte-Risselin C, Murrieta M. Comparative therapeutic effect and safety of mizolastine and loratadine in chronic idiopathic urticaria. URTILOR study group. Eur J Dermatol. 2000 Apr-May;10(3):205-11. PubMed PMID: 10725819.

18: Depoortere H, Decobert M, Granger P, Françon D. Mizolastine, a novel selective histamine H1 receptor antagonist: lack of sedative potential on the EEG in the rodent. Neuropsychobiology. 1995;32(4):214-21. PubMed PMID: 8587704.

19: Yan Y, Wang B, Zuo YG, Qu T. Inhibitory effects of mizolastine on ultraviolet B-induced leukotriene B4 production and 5-lipoxygenase expression in normal human dermal fibroblasts in vitro. Photochem Photobiol. 2006 May-Jun;82(3):665-9. PubMed PMID: 16402861.

20: Purohit A, Mélac M, Pauli G, Frossard N. Comparative activity of cetirizine and mizolastine on histamine-induced skin wheal and flare responses at 24 h. Br J Clin Pharmacol. 2002 Mar;53(3):250-4. PubMed PMID: 11874388; PubMed Central PMCID: PMC1874315.

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