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

SBI-115
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 555569

CAS#: 882366-16-7

Description: 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

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 555569
Name: SBI-115
CAS#: 882366-16-7
Chemical Formula: C14H13ClN2O4S
Exact Mass: 340.03
Molecular Weight: 340.778
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	Ready to Ship
25mg	USD 220	Ready to ship
50mg	USD 385	Ready to ship
100mg	USD 685	Ready to ship
200mg	USD 1250	Ready to ship
500mg	USD 2650	Ready to ship
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

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/

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	109.0	319.86

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:	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.
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.

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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.

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