2. Membrane Transporter/Ion Channel Neuronal Signaling JAK/STAT Signaling Stem Cell/Wnt
  3. nAChR STAT
  4. TC-2559 free base

TC-2559 free base 是一种 α4β2 烟碱型乙酰胆碱受体 (nAChR) 激动剂，其 EC50 为0.18 μM。TC-2559 free base 对β4亚基的 nAChR 基因型 (α2β4、α4β4 和 α3β4 受体) 的激动效力较弱，其EC50 在 10-30 μM之间。TC-2559 free base 能在体外增加大鼠腹侧被盖区 (VTA) 中的多巴胺细胞放电，增强 VTA 多巴胺能神经元的兴奋性和爆发性行为。TC-2559 free base 可抑制 STAT3 来发挥抗炎作用，缓解小鼠的机械性异常疼痛，并改善大鼠认知缺陷。TC-2559 free base 可用于研究神经疼痛。

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TC-2559 free base Chemical Structure

TC-2559 free base Chemical Structure

CAS No. : 189274-78-0

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

TC-2559 free base is a α4β2 nicotinic acetylcholine receptor (nAChR) agonists with an EC50 of 0.18 μM. TC-2559 free base shows much weaker potencies on the group of b4-containing nAChR subtypes, α2β4, α4β4 and α3β4 receptors, with EC50s in the range of 10-30 µM. TC-2559 free base can increase the discharge of dopamine cells in the ventral tegmental area (VTA) of rats in vitro, enhancing the excitability and aggressive behavior of VTA dopamine neurons. TC-2559 free base inhibits STAT3 to exert anti-inflammatory properties and relieves mice mechanical allodynia and improve rats cognitive deficits. TC-2559 free base can be used for the study of nerve pain[1][2][3][4][5].

体外研究
(In Vitro)

TC-2559 free base (free base) 能有效与 [3H]-莫可托品结合 (Ki = 5 nM)[1]。
TC-2559 free base (0-100nM) 能够增强大鼠纹状体突触小体多巴胺 (EC50 = 203 nM, E = 97%) 和大脑丘脑突触小体Rb蛋白的释放 (EC50 = 367 nM, E = 107%)，并且在 1mM 浓度下对 TE671/RD 细胞和 PC12 细胞无活性[1]。
TC-2559 free base (10 μM, 2 h) 能显著降低胎鼠脑细胞中的神经元死亡[1]。
TC-2559 free base (200-500 μM, 3-6 h) 能够抑制小鼠巨噬细胞中细胞因子配体 3 (CCL3) 和白细胞介素 1b (IL-1b) 的上调表达[3]。
TC-2559 free base (500 μM, 1-6 h) 能够抑制小鼠巨噬细胞中信号转导及转录激活因子 3 (pSTAT3) 的磷酸化[3]。
TC-2559 free base (0.5 mM, 24 h) 能够抑制小鼠腹腔巨噬细胞 PSL 处理后受损的 SCN 中白细胞介素-1β (IL-1β) 的过度表达[4]。
TC-2559 free base 对β4亚基的 nAChR 基因型 (α2β4、α4β4 和 α3β4 受体) 含有展示了较弱的激动效力，其 EC50 分别为 14、12.5、>30、>100 和 >100 μM[5]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

TC-2559 free base 相关抗体:

RT-PCR[3]

Cell Line: Mouse macrophage J774A.1 cells
Concentration: 20-500 μM with LPS
Incubation Time: 3 and 6 h
Result: Suppressed the mRNA expressions of CCL3 and IL-1b.

Western Blot Analysis[3]

Cell Line: Mouse macrophage J774A.1 cells
Concentration: 500 μM with LPS
Incubation Time: 1,3 and 6 h
Result: Inhibited the upregulation of pSTAT3 at 6 h.
Had no effect on pp65 expression at 1 and 6 h.
体内研究
(In Vivo)

TC-2559 free base (free base) (0.124-2.063 mg/kg, s.c., 单次剂量) 能够剂量依赖性地逆转由胆碱能阻断所导致的大鼠记忆障碍[1]。
HC-2559 (0.124-1.238 mg/kg, s.c., 单次给药或连续 5 天给药) 能显著减少工作记忆错误，并持续改善工作记忆[1]。
HC-2559 (0.206-2.063 mg/kg, s.c., 单次给药或连续 14 天给药) 单次给药时会导致运动抑制，而连续给药则不会引发行为耐受性[1]。
TC-2559 free base (0.021-1.32 mg/kg, i.v., 累计给药或单次给药) 通过 α4β2 样烟碱型受体激活伏隔核的多巴胺神经元[2]。
TC-2559 free base (0.47-4.70 mg/kg, s.c. 或 20 nmol, 神经周围注射, 3 天) 显著缓解了小鼠行为模型中的机械性异常疼痛[4]。
TC-2559 free base (20 nmol, 神经周围注射, 3 天) 能够抑制由小鼠周围神经损伤所引发的 SDH 中的微胶质细胞活化[4]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Attenuation of scopolamine-induced amnesia established in male Sprague-Dawley rats (200-350 g)[1]
Dosage: 0.124, 0.206, 0.619, 1.238 and 2.063 mg/kg (0.6, 1, 3, 6 and 10 μmol/mg)
Administration: Subcutaneous Injections (s.c.), single dose
Result: Attenuated scopolamine-induced decrease of avoidance latencies of 21.5 s at doses of 3 and 6 μmol/kg.
Exhibited the median step-through latencies of 88.7 and 105.7 s for 3 and 6 μmol/kg, respectively.
Animal Model: Radial-arm maze performance model established in male Sprague-Dawley rats (200-350 g)[1]
Dosage: 0.124, 0.206, 0.619 and 1.238 mg/kg (0.6, 1, 3 and 6 μmol/mg)
Administration: Subcutaneous Injections (s.c.), single dose or for 5 days
Result: Significantly reduced the number of working memory errors at 3 and 10 μmol/kg in Day 1.
Significantly reduced working memory errors following 6 days of repeated administration at 1, 3, and 6 μmol/kg.
Animal Model: Locomotor activity model established in male Sprague-Dawley rats (200-350 g)[1]
Dosage: 0.124, 0.412 and 2.063 mg/kg for acute administration and 0.721 mg/kg for repeated administration
Administration: Subcutaneous Injections (s.c.), single dose or once daily or for 14 days
Result: Resulted in significant reductions in horizontal counts at the 30-min time point.
Resulted in a dose-dependent monophasic change in locomotor behavior with a sustained hypolocomotion at 60 min for the 0.206 mg/kg dose.
No apparent sensitization developed following repeated administration.
Animal Model: Electrophysiological model established in male Sprague-Dawley rats (260-350 g)[2]
Dosage: 0.021-1.32 mg/kg or 0.66 and 1.32 mg/kg
Administration: Intravenous injection (i.v.), cumulative doses or single dose
Result: Increase the discharge frequency by 185%-206%.
Increase the peak discharge frequency to 141% at 0.66 mg/kg.
induced bursting in one of two nonbursting VTA DA neurones tested.
Evoked a significant increase in both spontaneous and burst firing for up to 15 min of the testing period at 1.32 mg/kg.
Were blocked by DHbE, but not by MLA.
Animal Model: Behavioral testing in male ICR mice aged 4 to 5 weeks[4]
Dosage: 0.470, 1.41 and 4.70 mg/kg (2.28, 6.84 and 22.8 μmol/kg) (s.c.) or 20 nmol (p.n.)
Administration: Subcutaneous Injections (s.c.) or perineural Injections (p.n.) for 3 days
Result: Significantly increase the mechanical pain threshold at 22.8 μmol/kg during either the early (days 0–3) or middle/late (days 7–10).
Improved mechanical allodynia with Sazetidine A (HY-14319A) with p.n. admisitraion during the early or middle phase.
Relieved mechanical allodynia with p.n. during the late (days 21-24) phase.
Animal Model: Microglial activation assay in male ICR mice aged 4 to 5 weeks[4]
Dosage: 20 nmol
Administration: Perineural Injections (p.n.) for 3 days
Result: Suppressed microglial activation in the SDH evaluated by Iba1 expression.
Significantly down-regulate inflammatory markers such as CD68, IRF5, and IL-1β.
分子量

206.28

Formula

C12H18N2O
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

TC-2559 free base 相关分类

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

TC-2559189274-78-0TC2559TC 2559nAChRSTATNicotinic acetylcholine receptorsSazetidine ANeuroinflammationCytokineChemokineAllodyninicotineVTAInhibitorinhibitorinhibit

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