Synonym
Tazifylline hydrochloride; Tazifylline HCl; LN 2974; RS-49014; RS 49014; RS49014; LN2974; LN-2974;
IUPAC/Chemical Name
7-(2-hydroxy-3-(4-(3-(phenylthio)propyl)piperazin-1-yl)propyl)-1,3-dimethyl-3,7-dihydro-1H-purine-2,6-dione dihydrochloride
InChi Key
HFYFNZKRWQJSLF-UHFFFAOYSA-N
InChi Code
InChI=1S/C23H32N6O3S.2ClH/c1-25-21-20(22(31)26(2)23(25)32)29(17-24-21)16-18(30)15-28-12-10-27(11-13-28)9-6-14-33-19-7-4-3-5-8-19;;/h3-5,7-8,17-18,30H,6,9-16H2,1-2H3;2*1H
SMILES Code
O=C(N1C)N(C)C2=C(N(CC(O)CN3CCN(CCCSC4=CC=CC=C4)CC3)C=N2)C1=O.[H]Cl.[H]Cl
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
2934.99.03.00
Preparing Stock Solutions
The following data is based on the
product
molecular weight
545.52
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: Poizot A, Dumez D, Ferrandon P, Lefournier C, Michel A, Armstrong JM. Animal pharmacology of the selective histamine H1-receptor antagonist tazifylline. Arzneimittelforschung. 1986 Apr;36(4):695-702. PubMed PMID: 2424463.
2: Ring J, Galosi A, Harlow BJ, Reuter CA, Bieber T, Ruzicka T, Yee KF. Antiallergic effects of the new histamine H1-receptor antagonist tazifylline in healthy atopic and non-atopic subjects. Arzneimittelforschung. 1988 Feb;38(2):308-11. PubMed PMID: 2897197.
3: Bruno R, Jullien I, Auger J, Iliadis A, Dow R, McEwen J, Cano JP, Pinhas H. Multiple-dose pharmacokinetics of the new H1-receptor antagonist tazifylline in healthy volunteers. Biopharm Drug Dispos. 1989 Jan-Feb;10(1):115-9. PubMed PMID: 2564283.
4: Kiviranta K, Stenius-Aarniala B, Reuter C, Harlow B, Scott J. The reducing effects of tazifylline on histamine-induced bronchoconstriction in atopic asthmatics. Methods Find Exp Clin Pharmacol. 1989 Feb;11(2):119-21. PubMed PMID: 2565416.
5: Nicholson AN, Stone BM. Antihistamines: impaired performance and the tendency to sleep. Eur J Clin Pharmacol. 1986;30(1):27-32. PubMed PMID: 3086105.
6: Savin JA, Dow R, Harlow BJ, Massey H, Yee KF. The effect of a new non-sedative H1-receptor antagonist (LN2974) on the itching and scratching of patients with atopic eczema. Clin Exp Dermatol. 1986 Nov;11(6):600-2. PubMed PMID: 2889550.
