LY 225910
(Synonyms: 2-[2-(5-溴-1H-吲哚-3-基)乙基]-3-[3-(1-甲基乙氧基)苯基]-4-(3H-)-喹唑啉酮) 目录号 : GC11305LY 225910是一种有效的胆囊收缩素受体拮抗剂，可特异性阻断CCK2受体并影响神经递质释放
Cas No.:133040-77-4
Sample solution is provided at 25 µL, 10mM.
LY 225910 is a potent and selective cholecystokinin receptor antagonist that specifically blocks the CCK2 receptor and influences neurotransmitter release[1-2]. LY 225910 is utilized to investigate the role of the CCK2 receptor in brain processes such as emotion, anxiety, and pain, as well as its modulation of GABAergic neurotransmission[3-4].
In vivo, LY 225910 (25ng; single injection) administered intrathecally in a rat model of lipopolysaccharide-induced central nervous system inflammation enhances the analgesic effects of morphine[5]. LY 225910 (0.1mg/kg) was administered as a single intraperitoneal injection to male Sprague-Dawley rats. LY 225910 exhibited anxiolytic-like effects within 24 hours, but at 24 hours post-administration, LY 225910 impaired the rats' novel object recognition and spatial recognition abilities[6].
References:
[1] Crosby KM, Baimoukhametova DV, Bains JS, et al. Postsynaptic Depolarization Enhances GABA Drive to Dorsomedial Hypothalamic Neurons through Somatodendritic Cholecystokinin Release. J Neurosci. 2015 Sep 23;35(38):13160-70.
[2] Rust VA, Crosby KM. Cholecystokinin acts in the dorsomedial hypothalamus of young male rats to suppress appetite in a nitric oxide-dependent manner. Neurosci Lett. 2021 Nov 1;764:136295.
[3] Lee JH, Kim SY, Kwon YK, et al. Characteristics of the cholecystokinin-induced depolarization of pacemaking activity in cultured interstitial cells of Cajal from murine small intestine. Cell Physiol Biochem. 2013;31(4-5):542-54.
[4] Soltani N, Roohbakhsh A, Allahtavakoli M, et al. Heterogeneous effects of cholecystokinin on neuronal response properties in deep layers of rat barrel cortex. Somatosens Mot Res. 2018 Jun;35(2):131-138.
[5] Xanthos DN, Kumar N, Theodorsson E, et al. The roles of nerve growth factor and cholecystokinin in the enhancement of morphine analgesia in a rodent model of central nervous system inflammation. Neuropharmacology. 2009 Mar;56(3):684-91.
[6] Ballaz SJ, Bourin M, Akil H, et al. Blockade of the cholecystokinin CCK-2 receptor prevents the normalization of anxiety levels in the rat. Prog Neuropsychopharmacol Biol Psychiatry. 2020 Jan 10;96:109761.
LY 225910是一种有效的胆囊收缩素受体拮抗剂，可特异性阻断CCK2受体并影响神经递质释放[1-2]。LY 225910可用于研究CCK2受体在情绪、焦虑和疼痛等大脑过程中的作用机制，以及其对GABA神经传递的调节[3-4]。
在体内，LY 225910 (25ng；单次注射)鞘内注射用于处理经脂多糖诱导中枢神经系统炎症的大鼠模型。LY 225910能够增强吗啡的镇痛效果[5]。LY 225910(0.1mg/kg)单次腹腔注射用于处理雄性Sprague-Dawley大鼠。LY 225910在24小时内表现出抗焦虑样作用，但在24小时后，LY 225910损害了大鼠对新物体识别和位置识别能力[6]。
| Animal experiment [1]: | |
Animal models | Sprague-Dawley rats |
Preparation Method | Rats were intraperitoneally administered a single dose of LY 225910 (0.1mg/kg) and behavioral tests (Elevated Plus Maze, Novel Object Recognition) were conducted at acute and 24-hour time points. |
Dosage form | 0.1mg/kg; i.p.; Single injection. |
Applications | LY 225910 exhibited anxiolytic-like effects within 24 hours, but at 24 hours post-administration, LY 225910 impaired the rats' novel object recognition and spatial recognition abilities. |
References: | |
| Cas No. | 133040-77-4 | SDF | |
| 别名 | 2-[2-(5-溴-1H-吲哚-3-基)乙基]-3-[3-(1-甲基乙氧基)苯基]-4-(3H-)-喹唑啉酮 | ||
| 化学名 | 2-(2-(5-bromo-1H-indol-3-yl)ethyl)-3-(3-isopropoxyphenyl)quinazolin-4(3H)-one | ||
| Canonical SMILES | BrC1=CC=C2NC=C(C2=C1)CCC(N3C4=CC=CC(OC(C)C)=C4)=NC5=CC=CC=C5C3=O | ||
| 分子式 | C27H24BrN3O2 | 分子量 | 502.41 |
| 溶解度 | Soluble to 100 mM in DMSO | 储存条件 | Desiccate at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
||
| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 1.9904 mL | 9.952 mL | 19.9041 mL |
| 5 mM | 398.1 μL | 1.9904 mL | 3.9808 mL |
| 10 mM | 199 μL | 995.2 μL | 1.9904 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet