Clemastine Fumarate | CAS#14976-57-9 | Selective Histamine H1 Antagonist

MedKoo Cat#: 317539 | Name: Clemastine Fumarate

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Description:

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

Clemastine fumarate is a histamine H1 antagonist used as the hydrogen fumarate in hay fever, rhinitis, allergic skin conditions, and pruritus. Clemastine fumarate blocks the H1 histamine receptor and prevents the symptoms that are caused by histamine activity on capillaries, bronchial and gastrointestinal smooth muscles, including vasodilation, increased capillary permeability, bronchoconstriction, and spasmodic contraction of gastrointestinal smooth muscles. It may cause cause drowsiness. This drug also prevents histamine-induced pain and itching of mucous membranes.

Chemical Structure

Clemastine Fumarate

CAS#14976-57-9 (fumarate)

Theoretical Analysis

MedKoo Cat#: 317539

Name: Clemastine Fumarate

CAS#: 14976-57-9 (fumarate)

Chemical Formula: C25H30ClNO5

Exact Mass: 0.0000

Molecular Weight: 459.96

Elemental Analysis: C, 65.28; H, 6.57; Cl, 7.71; N, 3.05; O, 17.39

Price and Availability

Size	Price	Availability
100mg	USD 265.00	2 Weeks
250mg	USD 450.00	2 Weeks
500mg	USD 750.00	2 Weeks
1g	USD 1,150.00	2 Weeks

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Related CAS #

15686-51-8 (free base) 14976-57-9 (fumarate)

Synonym

Clemastine Fumarate; Mecloprodine; Tavist; Agasten; Aloginan; Clemastine; HS 592; HS-592; HS592; Meclastine; Mecloprodin; Tavegyl; Tavist;

IUPAC/Chemical Name

(R)-2-(2-((R)-1-(4-chlorophenyl)-1-phenylethoxy)ethyl)-1-methylpyrrolidine fumarate

InChi Key

PMGQWSIVQFOFOQ-YKVZVUFRSA-N

InChi Code

InChI=1S/C21H26ClNO.C4H4O4/c1-21(17-7-4-3-5-8-17,18-10-12-19(22)13-11-18)24-16-14-20-9-6-15-23(20)2;5-3(6)1-2-4(7)8/h3-5,7-8,10-13,20H,6,9,14-16H2,1-2H3;1-2H,(H,5,6)(H,7,8)/b;2-1+/t20-,21-;/m1./s1

SMILES Code

CN1[C@@H](CCO[C@](C2=CC=CC=C2)(C3=CC=C(Cl)C=C3)C)CCC1.O=C(O)/C=C/C(O)=O

Appearance

White to light yellow crystalline 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

Instruction

View handling instruction

Preparing Stock Solutions

The following data is based on the product molecular weight 459.96 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

1: Green AJ, Gelfand JM, Cree BA, Bevan C, Boscardin WJ, Mei F, Inman J, Arnow S, Devereux M, Abounasr A, Nobuta H, Zhu A, Friessen M, Gerona R, von Büdingen HC, Henry RG, Hauser SL, Chan JR. Clemastine fumarate as a remyelinating therapy for multiple sclerosis (ReBUILD): a randomised, controlled, double-blind, crossover trial. Lancet. 2017 Dec 2;390(10111):2481-2489. doi: 10.1016/S0140-6736(17)32346-2. Epub 2017 Oct 10. PMID: 29029896. 2: Zhu J, Ma R, Li G. Drug repurposing: Clemastine fumarate and neurodegeneration. Biomed Pharmacother. 2023 Jan;157:113904. doi: 10.1016/j.biopha.2022.113904. Epub 2022 Nov 9. PMID: 36370521. 3: Drugs and Lactation Database (LactMed®) [Internet]. Bethesda (MD): National Institute of Child Health and Human Development; 2006–. Clemastine. 2021 Sep 20. PMID: 30000667. 4: Palma A, Chara JC, Montilla A, Otxoa-de-Amezaga A, Ruíz-Jaén F, Planas AM, Matute C, Pérez-Samartín A, Domercq M. Clemastine Induces an Impairment in Developmental Myelination. Front Cell Dev Biol. 2022 Mar 17;10:841548. doi: 10.3389/fcell.2022.841548. PMID: 35372341; PMCID: PMC8970281. 5: LiverTox: Clinical and Research Information on Drug-Induced Liver Injury [Internet]. Bethesda (MD): National Institute of Diabetes and Digestive and Kidney Diseases; 2012–. Clemastine. 2017 Jan 16. PMID: 31644019. 6: Zhu J, Jiang X, Chang Y, Wu Y, Sun S, Wang C, Zheng S, Wang M, Yao Y, Li G, Ma R. Clemastine fumarate attenuates tauopathy and meliorates cognition in hTau mice via autophagy enhancement. Int Immunopharmacol. 2023 Jul 24;123:110649. doi: 10.1016/j.intimp.2023.110649. Epub ahead of print. PMID: 37494840. 7: Chen JF, Liu K, Hu B, Li RR, Xin W, Chen H, Wang F, Chen L, Li RX, Ren SY, Xiao L, Chan JR, Mei F. Enhancing myelin renewal reverses cognitive dysfunction in a murine model of Alzheimer's disease. Neuron. 2021 Jul 21;109(14):2292-2307.e5. doi: 10.1016/j.neuron.2021.05.012. Epub 2021 Jun 7. PMID: 34102111; PMCID: PMC8298291. 8: Meng S, Sun X, Juan Z, Wang M, Wang R, Sun L, Li Y, Xin A, Li S, Li Y. Clemastine Fumarate Attenuates Myocardial Ischemia Reperfusion Injury Through Inhibition of Mast Cell Degranulation. Front Pharmacol. 2021 Aug 27;12:704852. doi: 10.3389/fphar.2021.704852. PMID: 34512339; PMCID: PMC8430029. 9: Rodríguez-Acevedo B, Rovira A, Vidal-Jordana A, Moncho D, Pareto D, Sastre- Garriga J. Neuritis óptica: etiopatogenia, diagnóstico, pronóstico y manejo [Optic neuritis: aetiopathogenesis, diagnosis, prognosis and management]. Rev Neurol. 2022 Feb 1;74(3):93-104. Spanish. doi: 10.33588/rn.7403.2021473. PMID: 35084734. 10: Mina JGM, Charlton RL, Alpizar-Sosa E, Escrivani DO, Brown C, Alqaisi A, Borsodi MPG, Figueiredo CP, de Lima EV, Dickie EA, Wei W, Coutinho-Silva R, Merritt A, Smith TK, Barrett MP, Rossi-Bergmann B, Denny PW, Steel PG. Antileishmanial Chemotherapy through Clemastine Fumarate Mediated Inhibition of the Leishmania Inositol Phosphorylceramide Synthase. ACS Infect Dis. 2021 Jan 8;7(1):47-63. doi: 10.1021/acsinfecdis.0c00546. Epub 2020 Dec 8. PMID: 33291887; PMCID: PMC7802075. 11: Cohen JA, Tesar PJ. Clemastine fumarate for promotion of optic nerve remyelination. Lancet. 2017 Dec 2;390(10111):2421-2422. doi: 10.1016/S0140-6736(17)32639-9. Epub 2017 Oct 10. PMID: 29029894. 12: Tian L, Liu Y, Fei Y, Lv H, Yan F, Li L, Shi J. Effect of Clemastine Fumarate on Perioperative Hemodynamic Instability Mediated by Anaphylaxis During Cardiopulmonary Bypass Surgery. Med Sci Monit. 2022 Jun 2;28:e936367. doi: 10.12659/MSM.936367. PMID: 35651299; PMCID: PMC9172263. 13: Yuan X, Juan Z, Zhang R, Sun X, Yan R, Yue F, Huang Y, Yu J, Xia X. Clemastine Fumarate Protects Against Myocardial Ischemia Reperfusion Injury by Activating the TLR4/PI3K/Akt Signaling Pathway. Front Pharmacol. 2020 Feb 10;11:28. doi: 10.3389/fphar.2020.00028. PMID: 32116705; PMCID: PMC7025565. 14: Wang F, Ren SY, Chen JF, Liu K, Li RX, Li ZF, Hu B, Niu JQ, Xiao L, Chan JR, Mei F. Myelin degeneration and diminished myelin renewal contribute to age- related deficits in memory. Nat Neurosci. 2020 Apr;23(4):481-486. doi: 10.1038/s41593-020-0588-8. Epub 2020 Feb 10. PMID: 32042174; PMCID: PMC7306053. 15: Sodeifian G, Garlapati C, Razmimanesh F, Ghanaat-Ghamsari M. Measurement and modeling of clemastine fumarate (antihistamine drug) solubility in supercritical carbon dioxide. Sci Rep. 2021 Dec 21;11(1):24344. doi: 10.1038/s41598-021-03596-y. PMID: 34934101; PMCID: PMC8692556. 16: Wang F, Yang YJ, Yang N, Chen XJ, Huang NX, Zhang J, Wu Y, Liu Z, Gao X, Li T, Pan GQ, Liu SB, Li HL, Fancy SPJ, Xiao L, Chan JR, Mei F. Enhancing Oligodendrocyte Myelination Rescues Synaptic Loss and Improves Functional Recovery after Chronic Hypoxia. Neuron. 2018 Aug 22;99(4):689-701.e5. doi: 10.1016/j.neuron.2018.07.017. Epub 2018 Aug 2. PMID: 30078577; PMCID: PMC6170028. 17: Sapko K, Jamroz-Wiśniewska A, Rejdak K. Novel Drugs in a Pipeline for Progressive Multiple Sclerosis. J Clin Med. 2022 Jun 10;11(12):3342. doi: 10.3390/jcm11123342. PMID: 35743410; PMCID: PMC9225445. 18: Pan S, Mayoral SR, Choi HS, Chan JR, Kheirbek MA. Preservation of a remote fear memory requires new myelin formation. Nat Neurosci. 2020 Apr;23(4):487-499. doi: 10.1038/s41593-019-0582-1. Epub 2020 Feb 10. PMID: 32042175; PMCID: PMC7213814. 19: Tong LY, Deng YB, Du WH, Zhou WZ, Liao XY, Jiang X. Clemastine Promotes Differentiation of Oligodendrocyte Progenitor Cells Through the Activation of ERK1/2 via Muscarinic Receptors After Spinal Cord Injury. Front Pharmacol. 2022 Jul 5;13:914153. doi: 10.3389/fphar.2022.914153. PMID: 35865954; PMCID: PMC9294397. 20: Yang L, Pei RJ, Li H, Ma XN, Zhou Y, Zhu FH, He PL, Tang W, Zhang YC, Xiong J, Xiao SQ, Tong XK, Zhang B, Zuo JP. Identification of SARS-CoV-2 entry inhibitors among already approved drugs. Acta Pharmacol Sin. 2021 Aug;42(8):1347-1353. doi: 10.1038/s41401-020-00556-6. Epub 2020 Oct 28. PMID: 33116249; PMCID: PMC7594953.

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