For research use only. Not for therapeutic Use.
TCV-309 chloride is a potent and specific platelet activating factor (PAF) antagonist. TCV-309 chloride specifically inhibits PAF-induced aggregation of rabbit and human platelets, and [3H]PAF binding to rabbit platelet microsomes with IC50 values of 33 nM, 58 nM and 27 nM, respectively. TCV-309 chloride has beneficial effects in anaphylactic shock[1][2].
In rats, TCV-309 selectively inhibits the PAF-induced hypotension, hemoconcentration and death with ED50 values of 2.7, 6.4 and 1.7 micrograms/kg (i.v.), respectively. TCV-309 most potently protects mice from death induced by PAF and due to anaphylactic shock with ED50 values of 2.1 and 2.6 micrograms/kg (i.v.), respectively[1].
TCV-309 chloride also reversed PAF-induced hypotension and endotoxin-induced hypotension in rats with ED50 values of 3.3 and 1.2 micrograms/kg (i.v.), respectively[1].
| Catalog Number | I000805 |
| CAS Number | 121494-09-5 |
| Synonyms | 2-[3-(N-(5-bromo-1-propylpyridin-1-ium-3-carbonyl)anilino)propanoylamino]ethyl 3,4-dihydro-1H-isoquinoline-2-carboxylate;chloride |
| Molecular Formula | C30H34BrClN4O4 |
| Purity | ≥95% |
| InChI | InChI=1S/C30H33BrN4O4.ClH/c1-2-15-33-20-25(19-26(31)22-33)29(37)35(27-10-4-3-5-11-27)17-13-28(36)32-14-18-39-30(38)34-16-12-23-8-6-7-9-24(23)21-34;/h3-11,19-20,22H,2,12-18,21H2,1H3;1H |
| InChIKey | HBWMSZWQSYEBPL-UHFFFAOYSA-N |
| SMILES | CCC[N+]1=CC(=CC(=C1)Br)C(=O)N(CCC(=O)NCCOC(=O)N2CCC3=CC=CC=C3C2)C4=CC=CC=C4.[Cl-] |
| Reference | [1]. Terashita Z et al. Beneficial effects of TCV-309, a novel potent and selective platelet activating factor antagonist in endotoxin and anaphylactic shock in rodents. J Pharmacol Exp Ther. 1992 Feb;260(2):748-55. [2]. M Poeze, et al. Decreased organ failure in patients with severe SIRS and septic shock treated with the platelet-activating factor antagonist TCV-309: a prospective, multicenter, double-blind, randomized phase II trial. TCV-309 Septic Shock Study Group. Shock. 2000 Oct;14(4):421-8. |
