DBIBB
目录号 : GC16558A non-lipid agonist of LPA2
Cas No.:1569309-92-7
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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 [1]. 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 [2].
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 [1].
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 [1].
References:
[1] Patil R, Szabó E, Fells J I, et al. Combined Mitigation of the Gastrointestinal and Hematopoietic Acute Radiation Syndromes by an LPA 2 Receptor-Specific Nonlipid Agonist[J]. Chemistry & biology, 2015, 22(2): 206-216.
[2] Mills G B, Moolenaar W H. The emerging role of lysophosphatidic acid in cancer[J]. Nature Reviews Cancer, 2003, 3(8): 582-591.
| Cas No. | 1569309-92-7 | SDF | |
| 化学名 | 2-[[[4-(1,3-dioxo-1H-benz[de]isoquinolin-2(3H)-yl)butyl]amino]sulfonyl]-benzoic acid | ||
| Canonical SMILES | O=C(C1=C2C(C=CC=C23)=CC=C1)N(CCCCNS(C4=C(C(O)=O)C=CC=C4)(=O)=O)C3=O | ||
| 分子式 | C23H20N2O6S | 分子量 | 452.5 |
| 溶解度 | ≤30mg/ml in DMSO;10mg/ml in dimethyl formamide | 储存条件 | Store at -20°C |
| 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 | 2.2099 mL | 11.0497 mL | 22.0994 mL |
| 5 mM | 0.442 mL | 2.2099 mL | 4.4199 mL |
| 10 mM | 0.221 mL | 1.105 mL | 2.2099 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 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 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % 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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。