4-IBP

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Chemical Structure| 155798-08-6 同义名 : NSC 667672
CAS号 : 155798-08-6
货号 : A147803
分子式 : C19H21IN2O
纯度 : 98%
分子量 : 420.29
MDL号 : MFCD00673910
存储条件：

Pure form Keep in dark place, sealed in dry, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(249.83 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
生物活性
描述 4-IBP is a selective σ1 agonist with a high level of affinity for the σ1 receptor (Ki = 1.7 nM) and a moderate affinity for the σ2 receptor (Ki = 25.2 nM) . 4-IBP has revealed weak antiproliferative effects on human U373-MG glioblastoma and C32 melanoma cells but induced marked concentration-dependent decreases in the growth of human A549 NSCLC and PC3 prostate cancer cells. 4-IBP modified the sensitivity of U373-MG cells in vitro to proapoptotic lomustin and proautophagic temozolomide, and markedly decreased the expression of two proteins involved in drug resistance: glucosylceramide synthase and Rho guanine nucleotide dissociation inhibitor. In vivo, 4-IBP increased the antitumor effects of temozolomide and irinotecan in immunodeficient mice that were orthotopically grafted with invasive cancer cells[2]. In 50% of the neurons recorded, 4-IBP (20 microg/kg i.v.) produced a potentiation of both NMDA(N-methyl-D-aspartate)- and quisqualate (QUIS)-induced responses. In the other 50% of neurons, 4-IBP produced an attenuation of both QUIS and NMDA responses[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.38mL

0.48mL

0.24mL

11.90mL

2.38mL

1.19mL

23.79mL

4.76mL

2.38mL
参考文献

[1]Megalizzi V, Mathieu V, et al. 4-IBP, a sigma1 receptor agonist, decreases the migration of human cancer cells, including glioblastoma cells, in vitro and sensitizes them in vitro and in vivo to cytotoxic insults of proapoptotic and proautophagic drugs. Neoplasia. 2007 May;9(5):358-69.

[2]Mégalizzi V, Mathieu V, Mijatovic T, Gailly P, Debeir O, De Neve N, Van Damme M, Bontempi G, Haibe-Kains B, Decaestecker C, Kondo Y, Kiss R, Lefranc F. 4-IBP, a sigma1 receptor agonist, decreases the migration of human cancer cells, including glioblastoma cells, in vitro and sensitizes them in vitro and in vivo to cytotoxic insults of proapoptotic and proautophagic drugs. Neoplasia. 2007 May;9(5):358-69

[3]Bermack JE, Debonnel G. Distinct modulatory roles of sigma receptor subtypes on glutamatergic responses in the dorsal hippocampus. Synapse. 2005 Jan;55(1):37-44