Synonym
L 636499; L-636499; L636499;
IUPAC/Chemical Name
dibenzo[b,f]thiepine-3-carboxylic acid 5,5-dioxide
InChi Key
ASJSKZXRWOAFGL-UHFFFAOYSA-N
InChi Code
InChI=1S/C15H10O4S/c16-15(17)12-8-7-11-6-5-10-3-1-2-4-13(10)20(18,19)14(11)9-12/h1-9H,(H,16,17)
SMILES Code
O=C(C1=CC=C(C=CC2=CC=CC=C23)C(S3(=O)=O)=C1)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
286.30
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: Siegfried ME, Bush LR. Dual antagonism by L-636,499 of serotonin and thromboxane A2 induced aggregation of canine platelets. Thromb Res. 1990 Dec 1;60(5):343-53. PubMed PMID: 2084956.
2: Hedlund H, Andersson KE, Fovaeus M, Holmquist F, Uski T. Characterization of contraction-mediating prostanoid receptors in human penile erectile tissues. J Urol. 1989 Jan;141(1):182-6. PubMed PMID: 2521189.
3: Liel N, Mais DE, Halushka PV. Desensitization of platelet thromboxane A2/prostaglandin H2 receptors by the mimetic U46619. J Pharmacol Exp Ther. 1988 Dec;247(3):1133-8. PubMed PMID: 2974487.
4: Fitzgerald DJ, Fragetta J, FitzGerald GA. Prostaglandin endoperoxides modulate the response to thromboxane synthase inhibition during coronary thrombosis. J Clin Invest. 1988 Nov;82(5):1708-13. PubMed PMID: 3183064; PubMed Central PMCID: PMC442741.
5: Swayne GT, Maguire J, Dolan J, Raval P, Dane G, Greener M, Owen DA. Evidence for homogeneity of thromboxane A2 receptor using structurally different antagonists. Eur J Pharmacol. 1988 Aug 2;152(3):311-9. PubMed PMID: 2975605.
6: Vargaftig B, Joseph D, Hatmi M. Interference of the thromboxane antagonist SK&F 88046 with platelet activation and subsequent desensitization by arachidonic acid and the thromboxane mimetics U46619 and EP171. Thromb Res. 1987 May 15;46(4):509-17. PubMed PMID: 3039684.
7: Fitzgerald DJ, Fragetta J, Fenelon LC, FitzGerald GA. Thromboxane synthase inhibition and thromboxane/endoperoxide receptor antagonism in a chronic canine model of coronary thrombosis. Adv Prostaglandin Thromboxane Leukot Res. 1987;17A:496-500. PubMed PMID: 2959103.
8: Uski TK, Andersson KE. Effects of the thromboxane-receptor antagonist L-636,499 on feline cerebral arteries. Acta Physiol Scand. 1986 Dec;128(4):605-11. PubMed PMID: 2949488.
9: Fitzgerald DJ, Doran J, Jackson E, FitzGerald GA. Coronary vascular occlusion mediated via thromboxane A2-prostaglandin endoperoxide receptor activation in vivo. J Clin Invest. 1986 Feb;77(2):496-502. PubMed PMID: 3003161; PubMed Central PMCID: PMC423371.
10: Foegh ML, Alijani MR, Helfrich GB, Khirabadi BS, Ramwell PW. Prolongation of cardiac allograft survival with the PAF antagonist BN-52021 and the thromboxane receptor antagonists L640035 and L636499. Adv Prostaglandin Thromboxane Leukot Res. 1985;15:381-4. PubMed PMID: 2936126.
