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MedKoo Cat#: 462078 | Name: Temelastine

Description:

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

Temelastine is a selective, competitive histamine H1-receptor antagonist which does not penetrate the central nervous system.

Chemical Structure

Temelastine
Temelastine
CAS#86181-42-2

Theoretical Analysis

MedKoo Cat#: 462078

Name: Temelastine

CAS#: 86181-42-2

Chemical Formula: C21H24BrN5O

Exact Mass: 441.1164

Molecular Weight: 442.36

Elemental Analysis: C, 57.02; H, 5.47; Br, 18.06; N, 15.83; O, 3.62

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.
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Related CAS #
No Data
Synonym
Temelastine; Temelastina; Temelastinum
IUPAC/Chemical Name
4(1H)-Pyrimidinone, 2-((4-(5-bromo-3-methyl-2-pyridinyl)butyl)amino)-5-((6-methyl-3-pyridinyl)methyl)-
InChi Key
OGEAASSLWZDQBM-UHFFFAOYSA-N
InChi Code
InChI=1S/C21H24BrN5O/c1-14-9-18(22)13-25-19(14)5-3-4-8-23-21-26-12-17(20(28)27-21)10-16-7-6-15(2)24-11-16/h6-7,9,11-13H,3-5,8,10H2,1-2H3,(H2,23,26,27,28)
SMILES Code
CC1=CC(Br)=CN=C1CCCC/N=C2NC=C(C(O)=N\2)CC3=CN=C(C=C3)C
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 442.36 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: No effects on sleep of a histamine H1-receptor antagonist: temelastine. K Adam, I Oswald Br J Clin Pharmacol. 1986 Dec; 22(6): 718–720. doi: 10.1111/j.1365-2125.1986.tb02963.x PMCID: PMC1401224 2: Non-invasive instrumental techniques to detect terfenadine and temelastine induced suppression of histamine weals in man. L Shall, R Marks Br J Clin Pharmacol. 1987 Oct; 24(4): 409–413. doi: 10.1111/j.1365-2125.1987.tb03192.x PMCID: PMC1386301 3: Temelastine does not affect theophylline pharmacokinetics in normal subjects. B G Charles, J J Schneider, R L Norris, P J Ravenscroft Br J Clin Pharmacol. 1987 Nov; 24(5): 673–675. doi: 10.1111/j.1365-2125.1987.tb03229.x PMCID: PMC1386342 4: Pharmacological studies with SK&F 93944 (temelastine), a novel histamine H1-receptor antagonist with negligible ability to penetrate the central nervous system. E. A. Brown, R. Griffiths, C. A. Harvey, D. A. Owen Br J Pharmacol. 1986 Mar; 87(3): 569–578. doi: 10.1111/j.1476-5381.1986.tb10199.x PMCID: PMC1916561 5: Characteristics of the binding of [3H]-mepyramine to intact human U373 MG astrocytoma cells: evidence for histamine-induced H1-receptor internalisation. S. Hishinuma, J. M. Young Br J Pharmacol. 1995 Nov; 116(6): 2715–2723. doi: 10.1111/j.1476-5381.1995.tb17232.x PMCID: PMC1909113 6: Modulation of antagonist binding to histamine H1-receptors by sodium ions and by 2-amino-2-hydroxymethyl-propan-1,3-diol HCl. W. J. Gibson, T. W. Roques, J. M. Young Br J Pharmacol. 1994 Apr; 111(4): 1262–1268. doi: 10.1111/j.1476 5381.1994.tb14882.x PMCID: PMC1910162 7: Calcium-dependence of histamine- and carbachol-induced inositol phosphate formation in human U373 MG astrocytoma cells: comparison with HeLa cells and brain slices. J. A. Arias-Montaño, V. Berger, J. M. Young Br J Pharmacol. 1994 Feb; 111(2): 598–608. doi: 10.1111/j.1476-5381.1994.tb14779.x PMCID: PMC1909978 8: Inhibition by cations of antagonist binding to histamine H1-receptors: differential effect of sodium ions on the binding of two radioligands. J. M. Treherne, J. S. Stern, W. J. Flack, J. M. Young Br J Pharmacol. 1991 Jul; 103(3): 1745–1751. doi: 10.1111/j.1476-5381.1991.tb09857.x PMCID: PMC1907796 9: [3H]-(+)-N-methyl-4-methyldiphenhydramine, a quaternary radioligand for the histamine H1-receptor. J. M. Treherne, J. M. Young Br J Pharmacol. 1988 Jul; 94(3): 797–810. doi: 10.1111/j.1476-5381.1988.tb11591.x PMCID: PMC1854022 10: Effects of administration of histamine and its H1, H2, and H3 receptor antagonists into the primary somatosensory cortex on inflammatory pain in rats Esmaeal Tamaddonfard, Nasrin Hamzeh-Gooshchi Iran J Basic Med Sci. 2014 Jan; 17(1): 55–61. PMCID: PMC3938887