SBFI-26
目录号 : GC39236
SBFI-26 是脂肪酸结合蛋白 FABP5 和 FABP7 的选择性和竞争性抑制剂，SBFI-26 与 FABP5 的典型配体结合口袋结合，Kjs 为 0.9 μM FABP5 和 ABP7 分别为 0.4 μM。
Cas No.:1541207-06-0
Sample solution is provided at 25 µL, 10mM.
SBFI-26 is a selective and competitive inhibitor of fatty acid binding proteins FABP5 and FABP7, SBFI-26 binds to the canonical ligand-binding pocket of FABP5[2],with Kjs of 0.9 μM and 0.4 μM for FABP5 and ABP7, respectively. SBFI-26 produces anti-nociceptive and anti-inflammatory effects[1,2].
The FABP inhibitor SBFI-26 does not decrease the amplitude of EPSCs and is a weak agonist of PPARα and PPARγ receptors. Confirming its selectivity for FABPs, SBFI-26failed to reduce AEA uptake in cells bearing a knockdown of FABP5, the main FABP expressed in HeLa cells. Additionally, SBFI-26 does not inhibit FAAH. Collectively, SBFI-26 is a selective FABP inhibitor[1].
SBFI-26 produces analgesic and anti-inflammatory effects in mice, SBFI-26 (20 mg/kg) significantly reduced carrageenan-induced thermal hyperalgesia and paw edema[1]. FABP5 was the only one dramatically upregulated along with increased protein expression in the established PH-LHD mouse model. Inhibition of FABP5 by SBFI-26 injection abrogated pulmonary artery remodelling in PH-LHD and improved cardiac function[3].
References:
[1]: Berger WT, Ralph BP, et,al. Targeting fatty acid binding protein (FABP) anandamide transporters - a novel strategy for development of anti-inflammatory and anti-nociceptive drugs. PLoS One. 2012;7(12):e50968. doi: 10.1371/journal.pone.0050968. Epub 2012 Dec 7. PMID: 23236415; PMCID: PMC3517626.
[2]: Hsu HC, Tong S, et,al. The Antinociceptive Agent SBFI-26 Binds to Anandamide Transporters FABP5 and FABP7 at Two Different Sites. Biochemistry. 2017 Jul 11;56(27):3454-3462. doi: 10.1021/acs.biochem.7b00194. Epub 2017 Jun 28. PMID: 28632393; PMCID: PMC5884075.
[3]: Lei Q, Yu Z, et,al. Fatty acid-binding protein 5 aggravates pulmonary artery fibrosis in pulmonary hypertension secondary to left heart disease via activating wnt/β-catenin pathway. J Adv Res. 2022 Sep;40:197-206. doi: 10.1016/j.jare.2021.11.011. Epub 2021 Nov 26. PMID: 36100327; PMCID: PMC9481948.
SBFI-26 是脂肪酸结合蛋白 FABP5 和 FABP7 的选择性和竞争性抑制剂，SBFI-26 与 FABP5[2] 的典型配体结合口袋结合，Kjs 为 0.9 μM FABP5 和 ABP7 分别为 0.4 μM。 SBFI-26 具有抗伤害和抗炎作用[1,2]。
FABP 抑制剂 SBFI-26 不会降低 EPSC 的振幅，并且是 PPARα 和 PPARγ 受体的弱激动剂。证实其对 FABP 的选择性，SBFI-26 未能减少具有 FABP5 敲低的细胞中的 AEA 摄取，FABP5 是 HeLa 细胞中表达的主要 FABP。此外，SBFI-26 不抑制 FAAH。总的来说，SBFI-26 是一种选择性 FABP 抑制剂[1]。
SBFI-26 在小鼠体内产生镇痛和抗炎作用，SBFI-26 (20 mg/kg) 显着减轻角叉菜胶诱导的热痛觉过敏和爪水肿[1]。在已建立的 PH-LHD 小鼠模型中，FABP5 是唯一一种随着蛋白质表达的增加而显着上调的基因。 SBFI-26 注射液抑制 FABP5 可消除 PH-LHD 肺动脉重构并改善心功能[3]。
| Cell experiment [1]: | |
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Cell lines |
HeLa cells |
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Preparation Method |
Cells were transfected with the PPAR reporter system, incubated with GW7647, rosiglitazone, or SBFI-26 for 6 hrs, followed by measurement of luciferase and β-galactosidase activity using a luminometer as described. |
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Reaction Conditions |
10uM SBFI-26 for 6 hrs |
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Applications |
Confirming its selectivity for FABPs, SBFI-26 failed to reduce AEA uptake in cells bearing a knockdown of FABP5, the main FABP expressed in HeLa cells. Additionally, SBFI-26 does not inhibit FAAH. Collectively,SB-FI-26 is a selective FABP inhibitor. |
| Animal experiment [2]: | |
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Animal models |
Male C57Bl6 mice (22-30 g) |
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Preparation Method |
SBFI-26 (20 mg/kg) was dissolved in ethanol∶emulphor∶saline (1∶1∶18), requiring sonication and gentle heating for solubilization, and administered 45 min prior to injection of carrageenan. |
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Dosage form |
20 mg/kg SBFI-26 for 45min |
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Applications |
SBFI-26 (20 mg/kg) significantly reduced carrageenan-induced thermal hyperalgesia and paw edema |
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References: [1]: Berger WT, Ralph BP, et,al. Targeting fatty acid binding protein (FABP) anandamide transporters - a novel strategy for development of anti-inflammatory and anti-nociceptive drugs. PLoS One. 2012;7(12):e50968. doi: 10.1371/journal.pone.0050968. Epub 2012 Dec 7. PMID: 23236415; PMCID: PMC3517626. | |
| Cas No. | 1541207-06-0 | SDF | |
| Canonical SMILES | O=C([C@H]1[C@@H](C2=CC=CC=C2)[C@H](C(O)=O)[C@@H]1C3=CC=CC=C3)OC4=CC=CC5=C4C=CC=C5.[Relative stereochemistry] | ||
| 分子式 | C28H22O4 | 分子量 | 422.47 |
| 溶解度 | DMSO: 100 mg/mL (236.70 mM) | 储存条件 | Store at -20°C, protect from light |
| 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 | 2.367 mL | 11.8352 mL | 23.6703 mL |
| 5 mM | 0.4734 mL | 2.367 mL | 4.7341 mL |
| 10 mM | 0.2367 mL | 1.1835 mL | 2.367 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。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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Related Biological Data
FABP5 affected breast cancer cell drug resistance.Cell viability was examined by CCK-8 assays in cells cultured with FABP5 inhibitor SBFI 26 for 72 h, and the protein expression level of FABP5 in MCF-7/ADR cells was determined.
12 h after seeding, cells were treated with Dox(0.1, 0.3, 1, 3, 10, 30, 100, 300, and 1000 μM) for 48 h or cultured with SBFI-26(GlpBio) (0.1, 0.3, 1, 3, 10, 30, 100, and 300 μM) for 72 h.
Front Pharmacol 14 (2023): 1150861 PMID: 37538178 IF: 5.5999 -
Related Biological Data
SBFI26 in combination with Fer-1, erastin, GSH, and Vitamin C on cell viability. (A) SBFI26 (50,100,150 μM) combined with Fer-1( 60 nM) on MDA-MB- 231 cell viability.
The cells were seeded in 90-mm dishes, cultured overnight and subsequently treated with 100 μM SBFI26(GLPBIO) for 24 h.
J Cell Mol Med 28.7 (2024): e18212 PMID: 38516826 IF: 5.2999