DMP 696
目录号 : GC31030
DMP696是一种促肾上腺素皮质激素释放激素受体1(CRHR1)拮抗剂，常用于治疗焦虑和抑郁症。
Cas No.:202578-52-7
Sample solution is provided at 25 µL, 10mM.
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DMP 696 is a selective corticotropin-releasing hormone receptor 1 (CRHR1) antagonist, used for the treatment of anxiety and depression.
DMP696 (3 mg/kg, p.o.) attenuates consolidation of remote fear memories of mice, without affecting their expression and retention. WT mice treated with DMP696 for 1 week starting 24 h after foot shock also show reduced synaptosomal GluR1 levels than do shocked vehicle-treated controls[1]. Rats treated with different doses of DMP696 (1, 3, 10, 30 mg/kg) show very little freezing during the 2-minute preshock interval. Rats treated with DMP696 exhibit a significant overall reduction in CREB phosphorylation, in both the LA, and BLA, but not in the CeA. DMP696 treatment reduces levels of LA and BLA pCREB across all time intervals that do not differ significantly from homecage pCREB levels (P>0.05). In the CeA, both vehicle- and DMP696-treated rats exhibit significantly higher pCREB expression at each post-conditioning time interval than homecage pCREB levels. Rats in the 30 ng DMP696 group exhibit significantly less freezing in comparison to vehicle-treated animals[2].
[1]. Thoeringer CK, et al. Consolidation of remote fear memories involves Corticotropin-Releasing Hormone (CRH) receptor type 1-mediated enhancement of AMPA receptor GluR1 signaling in the dentate gyrus. Neuropsychopharmacology. 2012 Feb;37(3):787-96. [2]. Hubbard DT, et al. Activation of basolateral amygdala corticotropin-releasing factor 1 receptors modulates the consolidation of contextual fear. Neuroscience. 2007 Dec 19;150(4):818-28. Epub 2007 Oct 5.
Animal experiment: | DMP696 is dissolved in saccharose-flavored NaCl 0.9% containing 10% DMSO, 10% PEG 400, and Tween-80 (1 drop/mL). Drug suspension is delivered on an oat flake and then fed to animals at a final dose of 3 mg/kg. Controls receive an oat flake soaked with saccharose-flavored vehicle only. The dose of 3 mg/kg is chosen on the basis of pilot experiments in which doses of 3, 10, and 30 mg/kg have been compared. The drug solutions are always freshly pipetted onto the flake and shortly dried before delivery. Ad libitum-fed mice receive some saccharose-flavored oat flakes 2 days before starting an experiment to habituate them to the novel food. Over the course of treatment, mice show no signs of aversion against the drug-soaked flakes, but readily ate them within a few seconds after delivery. |
References: [1]. Thoeringer CK, et al. Consolidation of remote fear memories involves Corticotropin-Releasing Hormone (CRH) receptor type 1-mediated enhancement of AMPA receptor GluR1 signaling in the dentate gyrus. Neuropsychopharmacology. 2012 Feb;37(3):787-96. | |
| Cas No. | 202578-52-7 | SDF | |
| Canonical SMILES | CC1=NN2C(N=C(C)N=C2NC(COC)COC)=C1C3=CC=C(Cl)C=C3Cl | ||
| 分子式 | C18H21Cl2N5O2 | 分子量 | 410.3 |
| 溶解度 | DMSO : 100 mg/mL (243.72 mM; Need ultrasonic) | 储存条件 | Store 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。 |
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| 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.4372 mL | 12.1862 mL | 24.3724 mL |
| 5 mM | 0.4874 mL | 2.4372 mL | 4.8745 mL |
| 10 mM | 0.2437 mL | 1.2186 mL | 2.4372 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: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet