DBIBB
产品编号 SR5562
DBIBB 是一种特异性溶血磷脂酸 (LPA2) 的 2 型 G 蛋白偶联受体的非脂质激动剂，是一种能够治疗高强度γ 射线对造血和胃肠系统引起的急性放射综合征的潜在活性分子 ，是一种作未有机合成和药物研究中的中间体。 DBIBB 可用于制备各种化合物，可减轻胃肠道辐射综合征，增加肠隐窝存活率和肠细胞增殖，并减少细胞凋亡 。
CAS 1569309-92-7
分子量 452.48
分子式 C23H20N2O6S
CAS No. 1569309-92-7
存储 : -20°C
溶解度：DMSO: 90.0 mg/mL (198.9 mM)
产品应用
DBIBB, a butylsulfamoyl benzoic acid analog, is a non-lipid agonist of LPA2 with an EC50 of 0.10 μM. DBIBB has no effect at other LPA receptor subtypes . The bioactive phospholipid lysophosphatidic acid (LPA) has been involved in stimulating cell proliferation, migration and survival by acting on its cognate G-protein-coupled receptors. Aberrant LPA production, receptor expression and signalling probably contribute to cancer initiation, progression and metastasis .
In vitro: DBIBB treatment postirradiation significantly (p< 0.01) increased the clonogenic survival of IEC-6 cells in the 2-6 Gy dose range. DBIBB reduced DNA fragmentation 4hr after irradiation in a dose dependent manner. DBIBB also reduced caspase 3/7 activity and DNA fragmentation in LPA2MEF treated with adriamycin. In purified CD34+ progenitor cells, DBIBB significantly increased the total number of colonies and specifically enhanced the survival of the granulocyte/macrophage lineages .
In vivo: Using a murine GI-ARS mice model of partial-body irradiation (PBI) with shielding of the bone marrow contained in the tibiae, fibulae, and paws, administrations of up to 10 mg/kg of DBIBB for 10 days showed no visually observable adverse effects and pathological findings at necropsy, indicating the lack of toxicity. The group that received 10 mg/kg DBIBB showed a significant increase in survival. In C57BL/6 mice, DBIBB showed a dose-dependent increase in the number of surviving crypts compared with the vehicle control.
储液制备推荐
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制备储备液 |
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1 mg |
5 mg |
10 mg |
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1 mM |
2.2099 mL |
11.0497 mL |
22.0994 mL |
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5 mM |
0.442 mL |
2.2099 mL |
4.4199 mL |
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10 mM |
0.221 mL |
1.105 mL |
2.2099 mL |
结构式
