SBI-115
目录号 : GC34775
SBI-115是一种G蛋白胆汁酸偶联受体1（TGR5；GPCR19）拮抗剂。
Cas No.:882366-16-7
Sample solution is provided at 25 µL, 10mM.
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SBI-115 is an antagonist of the G protein-coupled bile acid receptor 1 (TGR5; GPCR19)[1]. TGR5 is involved in inflammatory responses, and SBI-115 inhibits TGR5, which can increase the concentration and mRNA expression of pro-inflammatory factors both in vivo and in vitro[2].
In vitro, treatment of cystic cholangiocytes with SBI-115 (100, 200μM) for 24 hours resulted in a reduction of cell numbers by 20%-33% and a decrease in cyclic adenosine monophosphate (cAMP) levels[3]. Treatment of human pancreatic cancer cell lines PANC-1 and BXPC-3 with SBI-115 (1-20μM) for 48 hours showed significant inhibitory activity on PANC-1 and BXPC-3 cells at 10 μM and 5 μM, respectively, leading to morphological changes, a significant increase in vacuoles, and mitochondrial membrane disruption[4].
In vivo, a single intrathecal injection of SBI-115 (15μg) in spared nerve injury (SNI) mice blocked the therapeutic effect of TGR5 agonists on the mechanical hyperalgesia response in mice[5].
References:
[1] Ye D, He J, He X. The role of bile acid receptor TGR5 in regulating inflammatory signalling[J]. Scandinavian Journal of Immunology, 2024: e13361.
[2] Xu J, Cao J, Tan B, et al. G protein-coupled bile acid receptor 1 reduced hepatic immune response and inhibited NFκB, PI3K/AKT, and PKC/P38 MAPK signaling pathway in hybrid grouper[J]. Journal of Animal Science, 2023, 101: skad307.
[3] Masyuk T V, Masyuk A I, Lorenzo Pisarello M, et al. TGR5 contributes to hepatic cystogenesis in rodents with polycystic liver diseases through cyclic adenosine monophosphate/Gαs signaling[J]. Hepatology, 2017, 66(4): 1197-1218.
[4] Lei Y, Li G, Li J, et al. Investigation of the potential role of TGR5 in pancreatic cancer by a comprehensive molecular experiments and the liquid chromatography mass spectrometry (LC–MS) based metabolomics[J]. Discover Oncology, 2022, 13(1): 46.
[5] Wu Y, Qiu Y, Su M, et al. Activation of the bile acid receptors TGR5 and FXR in the spinal dorsal horn alleviates neuropathic pain[J]. CNS Neuroscience & Therapeutics, 2023, 29(7): 1981-1998.
SBI-115是一种G蛋白胆汁酸偶联受体1（TGR5；GPCR19）拮抗剂[1]。TGR5参与炎症反应，SBI-115抑制TGR5，可升高体内或体外促炎因子的浓度和mRNA表达[2]
在体外，SBI-115（100，200μM）处理囊性胆管细胞24 h，使细胞数量减少了20%-33%，降低了环磷酸腺苷（cAMP）水平[3]。SBI-115（1-20μM）处理人胰腺癌细胞株PANC-1和BXPC 3细胞48 h，分别在10 μM和5 μM时对PANC-1和BXPC 3细胞表现出显著的抑制活性，细胞形态学改变，空泡明显增多，线粒体膜破裂[4]。
在体内，SBI-115（15μg）通过单次鞘内注射处理保留神经损伤（SNI）小鼠，阻断了TGR5激动剂对小鼠机械性痛觉超敏反应的治疗效果[5]。
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Cell experiment [1]: |
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Cell lines |
Cholangiocytes |
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Preparation method |
Cholangiocytes (2,500 cells/well) were grown for 24-48 hours and then treated with TGR5 agonists (all, 25 lM), SBI-115 (100 and 200μM), and pasireotide (20μM) for additional 24 hours. |
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Reaction Conditions |
100, 200μM; 24 h |
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Applications |
Cholangiocytes were decreased after treatment with SBI-115 by 20%-33% and by 35%-40% in response to pasireotide. |
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Animal experiment [2]: |
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Animal models |
Male C57BL/6 mice |
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Preparation method |
Mice were catheterized and underwent SNI surgery on day 0. After 7 days of recovery, TGR5 agonist INT-777 or FXR agonist INT-747 was infused into the subarachnoid space via the catheter, and 50% PWT was measured by behavioral tests 1-9 hours and 1-6 days after drug treatment. Intrathecal injection of SBI-115(15μg in 5μL), Z-guggulsterone, or bicuculline was used to block TGR5, FXR, or GABAA receptors, respectively. |
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Dosage form |
15μg (5μL); i.t. |
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Applications |
Activation of TGR5 alleviated the established neuropathic pain induced by SNI, and the effect was blocked by SBI-115. |
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References: |
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| Cas No. | 882366-16-7 | SDF | |
| Canonical SMILES | O=C(C1=NC(S(=O)(CC)=O)=NC=C1Cl)OC2=CC=CC(C)=C2 | ||
| 分子式 | C14H13ClN2O4S | 分子量 | 340.78 |
| 溶解度 | DMSO : 150 mg/mL (440.17 mM);Water : < 0.1 mg/mL (insoluble) | 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 | 2.9344 mL | 14.6722 mL | 29.3444 mL |
| 5 mM | 0.5869 mL | 2.9344 mL | 5.8689 mL |
| 10 mM | 0.2934 mL | 1.4672 mL | 2.9344 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，
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2.
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Quality Control & SDS
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- Purity: >98.00%
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