SBI-115 | CAS#882366-16-7 | TGR5 (GPCR19) antagonist

MedKoo Cat#: 555569 | Name: SBI-115

Description:

WARNING: This product is for research use only, not for human or veterinary use.

SBI-115 is a TGR5 (GPCR19) antagonist. SBI-115 decreases hepatic cystogenesis with polycystic liver diseases via inhibiting TGR5. TGR5 contributes to hepatic cystogenesis by increasing cAMP and enhancing cholangiocyte proliferation; our data suggest that a TGR5 antagonist alone or concurrently with somatostatin receptor agonists represents a potential therapeutic approach in polycystic liver disease

Chemical Structure

SBI-115

CAS#882366-16-7

Theoretical Analysis

MedKoo Cat#: 555569

Name: SBI-115

CAS#: 882366-16-7

Chemical Formula: C14H13ClN2O4S

Exact Mass: 340.0285

Molecular Weight: 340.78

Elemental Analysis: C, 49.34; H, 3.85; Cl, 10.40; N, 8.22; O, 18.78; S, 9.41

Price and Availability

Size	Price	Availability
10mg	USD 110.00	Ready to Ship
25mg	USD 220.00	Ready to ship
50mg	USD 385.00	Ready to ship
100mg	USD 685.00	Ready to ship
200mg	USD 1,250.00	Ready to ship
500mg	USD 2,650.00	Ready to ship

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Related CAS #

No Data

Synonym

SBI-115; SBI 115; SBI115;

IUPAC/Chemical Name

4-Pyrimidinecarboxylic acid, 5-chloro-2-(ethylsulfonyl)-, 3-methylphenyl ester

InChi Key

IJPXOPBVXVPPEW-UHFFFAOYSA-N

InChi Code

InChI=1S/C14H13ClN2O4S/c1-3-22(19,20)14-16-8-11(15)12(17-14)13(18)21-10-6-4-5-9(2)7-10/h4-8H,3H2,1-2H3

SMILES Code

O=C(C1=NC(S(=O)(CC)=O)=NC=C1Cl)OC2=CC=CC(C)=C2

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO

Shelf Life

>3 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Product Data

Product Data

Certificate of Analysis

View CoA: current batch, Lot#T9D08P28

QC Data

View QC data: current batch, Lot#T9D08P28

Safety Data Sheet (SDS)

View Safety Data Sheet (SDS)

Instruction

View handling instruction

Biological target:

SBI-115 is a TGR5 (GPCR19) antagonist.

In vitro activity:

In this study, pancreatic cancer cells were treated with SBI-115. There was a significant reduction in cell proliferation capacity and induction of cell death following SBI-115 treatment. There were disturbances in mitochondrial morphology and alterations in metabolic pathways within the cancer cells under SBI-115 treatment. Reference: Discov Oncol. 2022 Jun 11;13(1):46. https://pubmed.ncbi.nlm.nih.gov/35689739/

In vivo activity:

TBDSBI-115 has potential to alleviate cystogenesis. Animal models demonstrated that SBI-115 significantly reduced hepatic cystic areas when administered alone and even more markedly when combined with pasireotide. Reference: Hepatology. 2017 Oct;66(4):1197-1218. https://pubmed.ncbi.nlm.nih.gov/28543567/

	Solvent	mg/mL	mM
Solubility
	DMSO	109.0	319.86

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 340.78 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. Lei Y, Li G, Li J, Gao S, Lei M, Gong G, Li C, Chen Y, Wang C, Wang X. 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. Discov Oncol. 2022 Jun 11;13(1):46. doi: 10.1007/s12672-022-00504-2. PMID: 35689739; PMCID: PMC9188013. 2. Zhan Y, Wen Y, Zhang LL, Shen XL, Chen XH, Wu XH, Tang XG. Paeoniflorin Improved Constipation in the Loperamide-Induced Rat Model via TGR5/TRPA1 Signaling-Mediated 5-Hydroxytryptamine Secretion. Evid Based Complement Alternat Med. 2021 Dec 8;2021:6076293. doi: 10.1155/2021/6076293. PMID: 34925531; PMCID: PMC8674056. 3. Xu J, Cao J, Tan B, Xie S. 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 Anim Sci. 2023 Jan 3;101:skad307. doi: 10.1093/jas/skad307. PMID: 37715969; PMCID: PMC10576523. 4. Masyuk TV, Masyuk AI, Lorenzo Pisarello M, Howard BN, Huang BQ, Lee PY, Fung X, Sergienko E, Ardecky RJ, Chung TDY, Pinkerton AB, LaRusso NF. TGR5 contributes to hepatic cystogenesis in rodents with polycystic liver diseases through cyclic adenosine monophosphate/Gαs signaling. Hepatology. 2017 Oct;66(4):1197-1218. doi: 10.1002/hep.29284. Epub 2017 Aug 26. PMID: 28543567; PMCID: PMC5605412.

In vitro protocol:

In vivo protocol:

1. Xu J, Cao J, Tan B, Xie S. 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 Anim Sci. 2023 Jan 3;101:skad307. doi: 10.1093/jas/skad307. PMID: 37715969; PMCID: PMC10576523. 2. Masyuk TV, Masyuk AI, Lorenzo Pisarello M, Howard BN, Huang BQ, Lee PY, Fung X, Sergienko E, Ardecky RJ, Chung TDY, Pinkerton AB, LaRusso NF. TGR5 contributes to hepatic cystogenesis in rodents with polycystic liver diseases through cyclic adenosine monophosphate/Gαs signaling. Hepatology. 2017 Oct;66(4):1197-1218. doi: 10.1002/hep.29284. Epub 2017 Aug 26. PMID: 28543567; PMCID: PMC5605412.

1: Masyuk TV, Masyuk AI, Lorenzo Pisarello M, Howard BN, Huang BQ, Lee PY, Fung X, Sergienko E, Ardecky RJ, Chung TDY, Pinkerton AB, LaRusso NF. TGR5 contributes to hepatic cystogenesis in rodents with polycystic liver diseases through cyclic adenosine monophosphate/Gαs signaling. Hepatology. 2017 Oct;66(4):1197-1218. doi: 10.1002/hep.29284. Epub 2017 Aug 26. PubMed PMID: 28543567; PubMed Central PMCID: PMC5605412.