NUCC-390 dihydrochloride
目录号 : GC39573NUCC-390 dihydrochloride是一种新型选择性小分子CXCR4受体激动剂。NUCC-390 dihydrochloride可诱导CXCR4受体内化。
Cas No.:2749281-71-6
Sample solution is provided at 25 µL, 10mM.
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NUCC-390 dihydrochloride is a novel and selective small-molecule CXCR4 receptor agonist[1]. NUCC-390 dihydrochloride induces internalization of CXCR4 receptor[2].
NUCC-390 dihydrochloride (0.625μM-1.25μM; 24h) induces axonal growth in primary cultured neurons via CXCR4 in a dose-dependent manner[1].Treatment of HEK293 cells with NUCC-390 dihydrochloride (10μM; 2h) resulted in a marked internalization of CXCR4-YFP, producing distinct receptor aggregates in the cytoplasm, but excluded from the nucleus. The effects of NUCC-390 dihydrochloride were completely inhibited by AMD-3100 (GC14745)[2].
NUCC-390 dihydrochloride (26mg/kg; ip; 14 days) treatment increased the density of actively regenerating axons in the proximal part of the sciatic nerve in mice with sciatic nerve injury, as well as the number of axons entering the bridging zone[3]. The CXCR4 receptor agonist NUCC-390 dihydrochloride (3.2mg/kg; im; 72h) stimulates the recovery of function of the neuromuscular junction after degeneration of motor axon terminals induced by Taipoxin and promotes nerve regeneration after O. scutellatus scutellatus venom muscle injection in mice[4]. NUCC-390 dihydrochloride (3.2mg/kg; 96h) promotes the recovery of evoked junction potentials (EJPs) of neuromuscular junctions of single muscle fibres of the mouse soleus muscles injected with the venoms of Bungarus caeruleus or β‐bungarotoxin[5].
References:
[1]. Negro S, Zanetti G, Mattarei A, et al. An agonist of the CXCR4 receptor strongly promotes regeneration of degenerated motor axon terminals[J]. Cells, 2019, 8(10): 1183.
[2]. Mishra R K, Shum A K, Platanias L C, et al. Discovery and characterization of novel small-molecule CXCR4 receptor agonists and antagonists[J]. Scientific reports, 2016, 6(1): 30155.
[3]. Zanetti G, Negro S, Megighian A, et al. A CXCR4 receptor agonist strongly stimulates axonal regeneration after damage[J]. Annals of Clinical and Translational Neurology, 2019, 6(12): 2395-2402.
[4]. Stazi M, D’Este G, Mattarei A, et al. An agonist of the CXCR4 receptor accelerates the recovery from the peripheral neuroparalysis induced by Taipan snake envenomation[J]. Plos Neglected Tropical Diseases, 2020, 14(9): e0008547.
[5]. Stazi M, Fabris F, Tan K Y, et al. An agonist of the CXCR4 receptor is therapeutic for the neuroparalysis induced by Bungarus snakes envenoming[J]. Clinical and Translational Medicine, 2022, 12(1)
NUCC-390 dihydrochloride是一种新型选择性小分子CXCR4受体激动剂[1]。NUCC-390 dihydrochloride可诱导CXCR4受体内化[2]。
NUCC-390 dihydrochloride（0.625μM-1.25μM；24h）以剂量依赖性方式通过CXCR4诱导原代培养神经元的轴突生长[1]。用NUCC-390 dihydrochloride（10μM；2h）处理HEK293细胞可导致CXCR4-YFP明显内化，在细胞质中产生明显的受体聚集体，但被排除在细胞核之外。NUCC-390 dihydrochloride的作用被AMD-3100（GC14745）完全抑制[2]。
NUCC-390 dihydrochloride（26mg/kg；ip；14 days）治疗增加了坐骨神经损伤小鼠坐骨神经近端主动再生轴突的密度，以及进入桥接区的轴突数量[3]。CXCR4受体激动剂NUCC-390 dihydrochloride（3.2mg/kg；im；72h）改善了Taipoxin引起的运动轴突终末变性后神经肌肉接头功能的恢复，并促进了小鼠肌肉注射O. scutellatus scutellatus毒液后的神经再生[4]。NUCC-390 dihydrochloride（3.2mg/kg；96h）促进注射了银环蛇毒液或β‐银环蛇毒素的小鼠比目鱼肌单个肌纤维神经肌肉接头的诱发接头电位 (EJP) 的恢复[5]。
| Cell experiment [1]: | |
Cell lines | Cerebellar granule neurons cell (CGN) |
Preparation Method | Rat cerebellar granule neuron cells (CGN) were treated with the indicated concentrations of NUCC-390 dihydrochloride (0.625μM -1.25μM) for 24h. |
Reaction Conditions | 0.625μM -1.25μM; 24h |
Applications | NUCC-390 dihydrochloride induces axonal growth in primary cultured neurons via CXCR4 in a dose-dependent manner. |
| Animal experiment [2]: | |
Animal models | Evoked Junctional Potentials modle |
Preparation Method | Six to eight-week-old CD1 mice were anesthetized with isoflurane, and locally injected in the hind limb with α-LTx (5μg/kg in 15µl of 0.9% NaCl, 0.2% gelatin solution). Four groups of mice were employed: group 1 received daily hind limb injections of NUCC-390 dihydrochloride (3.2mg/kg), group 2 was ip. injected twice daily with AMD3100 (4mg/kg), group 3 received a combination of the 2 treatments, group 4 only vehicle. Seventy-two hours later mice were sacrificed, and subjected to electrophysiological measurement. |
Dosage form | 3.2mg/kg; ip; 72h |
Applications | NUCC-390 dihydrochloride promotes the recovery of the physiological function of the murine neuromuscular junction (NMJ) after complete degeneration of its motor axon terminal. |
References:
[1]. Negro S, Zanetti G, Mattarei A, et al. An agonist of the CXCR4 receptor strongly promotes regeneration of degenerated motor axon terminals[J]. Cells, 2019, 8(10): 1183.
| Cas No. | 2749281-71-6 | SDF | |
| Canonical SMILES | O=C(N1CCCCC1)C2=NN(CCC)C3=C2CC(NCCC4=CC=NC=C4)CC3.Cl.Cl | ||
| 分子式 | C23H35Cl2N5O | 分子量 | 468.46 |
| 溶解度 | DMSO: 250 mg/mL (533.66 mM) | 储存条件 | Store at 2-8°C,stored under nitrogen |
| 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 | 2.1347 mL | 10.6733 mL | 21.3465 mL |
| 5 mM | 0.4269 mL | 2.1347 mL | 4.2693 mL |
| 10 mM | 0.2135 mL | 1.0673 mL | 2.1347 mL |
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| 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 |
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| % 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。
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Quality Control & SDS
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- Purity: >99.00%
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