| Description | Men 10376 TFA(135306-85-3,free) (Neurokinin-2 receptor antagonist 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. |
| In vitro | Men 10376是一种选择性的tachykinin NK-2受体拮抗剂，其Ki值为4.4 μM，对NK-1和NK-3受体具有较低的选择性(Ki, >10 μM)[1]。Men 10376在NK-1（豚鼠小肠）和NK-2受体（去内皮的兔肺动脉）上的pA2值分别为5.66和8.08。Men 10376对NK-3受体无效(Ki, >10 μM)[2]。 |
| In vivo | Men 10376（1及3 μmol/kg）在大鼠中对NK-2受体激动剂引起的膀胱活动增加具有拮抗作用[2]。 |
| Target activity | NK2:Ki: 4.4 μM (rat small intestine) |
| Synonyms | Men 10376 TFA, Neurokinin-2 receptor antagonist TFA |
| molecular weight | 1195.25 |
| Molecular formula | C59H69F3N12O12 |
| Storage | keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | H2O: 1.43 mg/mL (1.20 mM), Sonication is recommended. |
| References | 1. Quartara L, et al. N-terminal truncated analogs of men 10376 as tachykinin NK-2 receptor antagonists. Life Sci. 1992;51(25):1929-36. |