HT-2157
(Synonyms: SNAP 37889) 目录号 : GC36261
A GAL3 receptor antagonist
Cas No.:303149-14-6
Sample solution is provided at 25 µL, 10mM.
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HT-2157 is an antagonist of the galanin-3 receptor (GAL3; Ki = 17 nM).1 It is selective for GAL3 over GAL1 and GAL2 (Kis = >10 ?M for both). HT-2157 (10 ?M) induces apoptosis in various cell types, including HL-60 leukemia and BV-2 murine microglial cells, as well as isolated human peripheral blood mononuclear cells (PBMCs).2 It decreases operant alcohol, sucrose, and saccharin self-administration in rats when administered at a dose of 30 mg/kg.3 HT-2157 (3 and 10 mg/kg) increases drinking in the Vogel punished drinking task and reduces immobility time in the forced swim test in rats, indicating anxiolytic- and antidepressant-like activities, respectively.4
1.Konkel, M.J., Lagu, B., Boteju, L.W., et al.3-arylimino-2-indolones are potent and selective galanin GAL3 receptor antagonistsJ. Med. Chem.49(13)3757-3758(2006) 2.Koller, A., Rid, R., Beyreis, M., et al.In vitro toxicity of the galanin receptor 3 antagonist SNAP 37889Neuropeptides5683-88(2016) 3.Ash, B.L., Zanatta, S.D., Williams, S.J., et al.The galanin-3 receptor antagonist, SNAP 37889, reduces operant responding for ethanol in alcohol-preferring ratsRegul. Pept.166(1-3)59-67(2011) 4.Swanson, C.J., Blackburn, T.P., Zhang, X., et al.Anxiolytic- and antidepressant-like profiles of the galanin-3 receptor (Gal3) antagonists SNAP 37889 and SNAP 398299Proc. Natl. Acad. Sci. USA102(48)17489-17494(2005)
Kinase experiment: | Binding affinities for HT-2157 (SNAP 37889) and SNAP 398299 at the human Gal1, Gal2, and Gal3 receptors are determined by using the 125I-galanin displacement assay. Additionally, is tested for binding in a broad cross-reactivity panel that included G-protein-coupled receptors, ion channels, enzymes, and transporters. The ability of HT-2157 to antagonize functional responses to galanin is examined in modified HEK-293 cells (PEAKrapid cells) transiently cotransfected with the Gal3 receptor and Gαz by measuring the inhibition of adenylyl cyclase activity[1]. |
Animal experiment: | Rats[2] The effect of HT-2157 on locomotor activity is examined using adult male iP rats (n=12; 418-467 g). Locomotor activity is tested to ensure that any potential change in anxiety or ethanol consumption in subsequent tests is not due to any sedative property of the drug. Rats are habituated to the locomotor cells (26×26×40 cm) for 60 minute sessions which are conducted daily for three consecutive days. To minimise the effect of habituation during the treatment phase, rats are divided into two even groups which received a single injection of either HT-2157 (30 mg/kg, i.p.) or vehicle (1 ml/kg i.p.) 30 min prior to being placed in the locomotor cells for a 60 minute session. The following day the treatments are reversed so that all rats received treatment with both the vehicle and SNAP 37889 compound. Movements in terms of number of moves, move time (s) and total distance travelled (cm), are recorded automatically using TruScan 2.0 software. |
References: [1]. Swanson CJ, et al. Anxiolytic- and antidepressant-like profiles of the galanin-3 receptor (Gal3) antagonists SNAP 37889 and SNAP 398299. Proc Natl Acad Sci U S A. 2005 Nov 29;102(48):17489-94. | |
| Cas No. | 303149-14-6 | SDF | |
| 别名 | SNAP 37889 | ||
| Canonical SMILES | O=C1N(C2=CC=CC=C2)C3=C(C=CC=C3)/C1=N/C4=CC=CC(C(F)(F)F)=C4 | ||
| 分子式 | C21H13F3N2O | 分子量 | 366.34 |
| 溶解度 | DMSO: ≥ 29 mg/mL (79.16 mM) | 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 | 2.7297 mL | 13.6485 mL | 27.297 mL |
| 5 mM | 0.5459 mL | 2.7297 mL | 5.4594 mL |
| 10 mM | 0.273 mL | 1.3649 mL | 2.7297 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
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet