SBI-115 |
| رقم الكتالوجGC34775 |
SBI-115 هو مضاد TGR5 (GPCR19)
Products are for research use only. Not for human use. We do not sell to patients.
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.
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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 | ||
| Formula | C14H13ClN2O4S | M.Wt | 340.78 |
| الذوبان | DMSO : 150 mg/mL (440.17 mM);Water : < 0.1 mg/mL (insoluble) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.9344 mL | 14.6722 mL | 29.3444 mL |
| 5 mM | 586.9 μL | 2.9344 mL | 5.8689 mL |
| 10 mM | 293.4 μL | 1.4672 mL | 2.9344 mL |
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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Average Rating: 5 (Based on Reviews and 27 reference(s) in Google Scholar.)
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