Synonym
L 643441; L-643441; L643441; L-643,441; L 643,441; L643,441;
IUPAC/Chemical Name
3-amino-4-((3-(3-(piperidin-1-ylmethyl)phenoxy)propyl)amino)-1,2,5-thiadiazole 1-oxide
InChi Key
DUPAVAVETJQPOR-UHFFFAOYSA-N
InChi Code
InChI=1S/C17H25N5O2S/c18-16-17(21-25(23)20-16)19-8-5-11-24-15-7-4-6-14(12-15)13-22-9-2-1-3-10-22/h4,6-7,12H,1-3,5,8-11,13H2,(H2,18,20)(H,19,21)
SMILES Code
NC1=NS(N=C1NCCCOC2=CC=CC(CN3CCCCC3)=C2)=O
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
>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
Preparing Stock Solutions
The following data is based on the
product
molecular weight
363.48
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: Wang RW, Miwa GT, Argenbright LS, Lu AY. In vitro studies on the interaction of famotidine with liver microsomal cytochrome P-450. Biochem Pharmacol. 1988 Aug 1;37(15):3049-53. PubMed PMID: 2899433.
2: Reeves JJ, Stables R. The antisecretory profile of action of the H2-receptor antagonists, famotidine, loxtidine, ranitidine and L-643,441 on the rat isolated gastric mucosa. Agents Actions. 1987 Feb;20(1-2):22-8. PubMed PMID: 2883848.
3: Lin JH, Cocchetto DM, Yeh KC, Duggan DE. Comparative effects of H2-receptor antagonists on drug interaction in rats. Drug Metab Dispos. 1986 Nov-Dec;14(6):649-53. PubMed PMID: 2877821.
4: MacLeod KM, Wenkstern D, McNeill JH. Irreversible antagonism of histamine H2 receptors in guinea-pig myocardium. Eur J Pharmacol. 1986 May 27;124(3):331-6. PubMed PMID: 2874036.
5: Henry DA, Somerville KW, Kitchingman GK, Holmes IB, Tobert JA, Langman MJ. L-643.441: an H2-receptor antagonist with potent and long-lasting effects in man. Br J Clin Pharmacol. 1985 Aug;20(2):133-6. PubMed PMID: 2864050; PubMed Central PMCID: PMC1400675.
6: Pendleton RG, Cook PG, Shepherd-Rose A, Mangel AW. Effects of H2-receptor antagonists upon physiological acid secretory states in animals. J Pharmacol Exp Ther. 1985 Apr;233(1):64-9. PubMed PMID: 2858583.
7: Batzri S, Thompson WF, Toles R. Distortion of H2-antagonist equilibrium constants by uptake in rabbit gastric mucosal cells. Pharmacology. 1985;30(4):215-24. PubMed PMID: 2859616.
8: Shepherd-Rose AJ, Pendleton RG. Studies on the properties of 3-N-[3-[3-(1-piperidinomethyl)phenoxy]-propyl]amino-4-amino-1,2, 5-thiadiazole-1-oxide (L-643,441) as an H2-receptor antagonist in isolated gastric glands. Eur J Pharmacol. 1984 Oct 1;105(1-2):57-63. PubMed PMID: 6149144.
9: Batzri S, Harmon JW, Toles R. Comparison of cimetidine with new H2-antagonists in rabbit and guinea pig gastric cells. Eur J Pharmacol. 1983 Oct 14;94(1-2):1-8. PubMed PMID: 6140169.
10: Torchiana ML, Pendleton RG, Cook PG, Hanson CA, Clineschmidt BV. Apparent irreversible H2-receptor blocking and prolonged gastric antisecretory activities of 3-N-(3-[3-(1-piperidinomethyl)phenoxy]propyl) amino-4-amino-1,2,5-thiadiazole-1-oxide (L-643, 441). J Pharmacol Exp Ther. 1983 Mar;224(3):514-9. PubMed PMID: 6131118.
