[CAS NO. 121494-09-5] TCV-309chloride
PRODUCTS SPECIFICATIONS [121494-09-5]
DESCRIPTION [121494-09-5]
Overview
| MDL | MFCD30343857 |
|---|---|
| Molecular Weight | 629.97 |
| Molecular Formula | C30H34BrClN4O4 |
| SMILES | CCC[N+]1=CC(C(N(CCC(NCCOC(N2CC3=C(C=CC=C3)CC2)=O)=O)C4=CC=CC=C4)=O)=CC(Br)=C1.[Cl-] |
Summary
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 IC 50 values of 33 nM, 58 nM and 27 nM, respectively. TCV-309 chloride has beneficial effects in anaphylactic shock [1] [2] .
In Vivo
In rats, TCV-309 selectively inhibits the PAF-induced hypotension, hemoconcentration and death with ED
50
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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : ≥ 6.3 mg/mL ( 10.00 mM )
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.5874 mL | 7.9369 mL | 15.8738 mL |
| 5 mM | 0.3175 mL | 1.5874 mL | 3.1748 mL |
| 10 mM | 0.1587 mL | 0.7937 mL | 1.5874 mL |
References
- [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.