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SBI-115

SBI-115 是TGR5 (GPCR19)拮抗剂，对 TGR5 降低多囊性肝病的肝囊肿形成具有抑制作用。

CAS号

882366-16-7

分子式

C14H13ClN2O4S

主要靶点

GPCR19

仅限科研使用

Cat No : CM04301

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Synonyms

验证数据展示

  • CAS No.: 882366-16-7

    SBI-115
    CAS#: 882366-16-7

产品信息

SBI-115 is an antagonist of TGR5. SBI-115 decreases hepatic cystogenesis with polycystic liver diseases via inhibiting TGR5

CAS号 882366-16-7
分子式 C14H13ClN2O4S
主要靶点 GPCR19
主要通路 G蛋白偶联受体
分子量 340.78
纯度 99.67%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名

体内活性

Stimulation of cholangiocytes with TLCA following by SBI-115 treatment resulted in dose-dependent (by 32–48%) inhibition of cell proliferation.

溶解度

DMSO:150 mg/mL (440.17 mM)

细胞实验

cAMP was detected by the Bridge-It cAMP designer cAMP assay. Cholangiocytes (10,000/well) were incubated with TLCA, OA, C1 and C2 (all, 25 μM), SBI-115 (100 and 200 μM) and pasireotide (20 μM) for 15–30 min. Doses of drugs were chosen based on published data or dose ranging (SBI-115). Cell proliferation was determined by CellTiter 96 Aqueous One Solution Cell Proliferation Assay ?and by cell counting using the Cellometer Auto4 ?cell counter.?Cholangiocytes (2500 cells/well) were grown for 24–48 hours and then treated with TGR5 agonists (all, 25 μM), SBI-115 (100 and 200 μM) and pasireotide (20 μM) for additional 24 hours.?Alterations in cell proliferation after treatment were expressed as percent change compared to un-treated cholangiocytes in which cell proliferation was considered to be equal 100%.

参考文献

1.Masyuk TV, Masyuk AI, 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 Oct;66(4):1197-1218.

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