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HT-2157 Sale

(Synonyms: SNAP 37889) 目录号 : GC36261

A GAL3 receptor antagonist

HT-2157 Chemical Structure

Cas No.:303149-14-6

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥1,958.00
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1mg
¥810.00
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5mg
¥2,430.00
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10mg
¥3,870.00
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50mg
¥11,700.00
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100mg
¥18,900.00
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200mg 待询 待询
500mg 待询 待询

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Sample solution is provided at 25 µL, 10mM.

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实验参考方法

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.
[2]. Ash BL, et al. The galanin-3 receptor antagonist, SNAP 37889, reduces operant responding for ethanol in alcohol-preferring rats. Regul Pept. 2011 Jan 17;166(1-3):59-67.

产品描述

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)

Chemical Properties

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
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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
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