Description
| Description | Men 10376 TFA is an effective and selective tachykinin nk-2 receptor antagonist with a K I value of 4.4 M for the nk-2 receptor in the small intestine of rats. |
| Targets&IC50 | NK2:Ki: 4.4 μM (rat small intestine) |
| In vitro | Men 10376 is a selective tachykinin NK-2 receptor, with a Ki of 4.4 μM, and shows low selectivity for NK-1 and NK-3 receptors (Ki, >10 μM)[1]. Men 10376 shows pA2s of 5.66 and 8.08 for NK-1 (guinea-pig ileum) and NK-2 receptors (endothelium-deprived rabbit pulmonary artery). Men 10376 shows no effect on NK-3 receptor (Ki, >10 μM)[2]. |
| In vivo | Men 10376 (1 and 3 μmol/kg) antagonizes increase in bladder motility produced by the NK-2 receptor agonist in rats[2]. |
| Synonyms | Neurokinin-2 receptor antagonist TFA, Men 10376 TFA |
| Molecular Weight |
1195.25 |
| Formula | C59H69F3N12O12 |
| CAS No. | TP1086 |
Storage
Powder: -20°C for 3 years
In solvent: -80°C for 2 years
Solubility Information
H2O: 1.43 mg/mL (1.20 mM),
Need ultrasonic
( < 1 mg/ml refers to the product slightly soluble or insoluble )
