产品介绍 |
Otenzepad (AF-DX 116) 是一种选择性的、竞争性的 M2 毒蕈碱乙酰胆碱受体拮抗剂,对兔外周肺和大鼠心脏的 IC50 值分别为 640 nM 和 386 nM。
|
---|
生物活性 |
Otenzepad (AF-DX 116) is a selective and competitive M2 muscarinic acetylcholine receptor antagonist, with IC50 values of 640 nM and 386 nM for rabbit peripheral lung and rat heart, respectively.
|
---|
体外研究 | |
---|
体内研究 |
Otenzepad (0.5, 1 mg/kg, s.c., in rats) significantly improved win-stay acquisition relative to vehicle-injected controls.
Otenzepad (2 mg/kg, s.c., in rats) significantly improved retention relative to vehicle controls.
Otenzepad (0.3, 1.0, or 3.0 mg/kg, ip, in mice) potentiates the effects of glucose and reverses the effects of insulin on memory.
西域 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model: |
Forty-eight male Long-Evans rats (325-350 g). |
Dosage: |
0.25, 0.5, 1.0 and 2.0 mg/kg. |
Administration: |
S.C. on the dorsum of the neck once. |
Result: |
Doses of 0.5 and 1.0 mg/kg significantly improved acquisition relative to vehicle controls, while doses of 0.25 and 2.0 mg/kg had no effect. |
Animal Model: |
Adult male Swiss mice (age 60–70 days; weight 25-30 g). |
Dosage: |
0.3, 1.0, or 3.0 mg/kg. |
Administration: |
IP once. |
Result: |
Enhanced retention in an inverted-U dose–response manner, with significant enhancement seen at 1.0 mg/kg (U15,15 = 49, p < 0.02, compared with saline-saline-injected control group). |
|
---|
体内研究 |
Otenzepad (0.5, 1 mg/kg, s.c., in rats) significantly improved win-stay acquisition relative to vehicle-injected controls.
Otenzepad (2 mg/kg, s.c., in rats) significantly improved retention relative to vehicle controls.
Otenzepad (0.3, 1.0, or 3.0 mg/kg, ip, in mice) potentiates the effects of glucose and reverses the effects of insulin on memory.
西域 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model: |
Forty-eight male Long-Evans rats (325-350 g). |
Dosage: |
0.25, 0.5, 1.0 and 2.0 mg/kg. |
Administration: |
S.C. on the dorsum of the neck once. |
Result: |
Doses of 0.5 and 1.0 mg/kg significantly improved acquisition relative to vehicle controls, while doses of 0.25 and 2.0 mg/kg had no effect. |
Animal Model: |
Adult male Swiss mice (age 60–70 days; weight 25-30 g). |
Dosage: |
0.3, 1.0, or 3.0 mg/kg. |
Administration: |
IP once. |
Result: |
Enhanced retention in an inverted-U dose–response manner, with significant enhancement seen at 1.0 mg/kg (U15,15 = 49, p < 0.02, compared with saline-saline-injected control group). |
|
---|
性状 | Solid |
---|
溶解性数据 |
In Vitro:
DMSO : 25 mg/mL (59.31 mM; ultrasonic and warming and heat to 60°C)
配制储备液
浓度
溶剂体积
质量
|
1 mg |
5 mg |
10 mg |
1 mM |
2.3723 mL |
11.8613 mL |
23.7225 mL |
5 mM |
0.4745 mL |
2.3723 mL |
4.7445 mL |
10 mM |
0.2372 mL |
1.1861 mL |
2.3723 mL |
*
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
|
---|
运输条件 |
Room temperature in continental US; may vary elsewhere.
|
---|
储存方式 |
Powder |
-20°C |
3 years |
|
4°C |
2 years |
In solvent |
-80°C |
6 months |
|
-20°C |
1 month |
|
---|
参考文献 | |
---|