MedKoo Cat#: 501203 | Name: MBX-2982
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Description:

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

MBX-2982, also known as SAR-260093, is a potential first-in-class treatment for type 2 diabetes that targets G protein-coupled receptor 119 (GPR119), a receptor that interacts with bioactive lipids known to stimulate glucose-dependent insulin secretion. Preclinical data indicate that MBX-2982 is a potent selective orally-active GPR119 agonist that functions through a unique dual mechanism of action. First, it acts directly on the beta cell to increase insulin secretion. In addition, MBX-2982 stimulates release of the incretin GLP-1 from the gut. This dual action is unique and may offer improved glucose homeostasis over existing diabetes therapies, with potential for weight loss and improved islet health.

Chemical Structure

MBX-2982
MBX-2982
CAS#1037792-44-1

Theoretical Analysis

MedKoo Cat#: 501203

Name: MBX-2982

CAS#: 1037792-44-1

Chemical Formula: C22H24N8OS

Exact Mass: 448.1794

Molecular Weight: 448.54

Elemental Analysis: C, 58.91; H, 5.39; N, 24.98; O, 3.57; S, 7.15

Price and Availability

Size Price Availability Quantity
25mg USD 250.00 2 weeks
50mg USD 450.00 2 weeks
100mg USD 750.00 2 weeks
200mg USD 1,150.00 2 weeks
500mg USD 1,950.00 2 weeks
1g USD 2,950.00 2 weeks
2g USD 4,950.00 2 weeks
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Synonym
MBX-2982; MBX 2982; MBX2982; SAR-260093; SAR260093; SAR 260093
IUPAC/Chemical Name
4-((4-(1H-tetrazol-1-yl)phenoxy)methyl)-2-(1-(5-ethylpyrimidin-2-yl)piperidin-4-yl)thiazole
InChi Key
NFTMKHWBOINJGM-UHFFFAOYSA-N
InChi Code
InChI=1S/C22H24N8OS/c1-2-16-11-23-22(24-12-16)29-9-7-17(8-10-29)21-26-18(14-32-21)13-31-20-5-3-19(4-6-20)30-15-25-27-28-30/h3-6,11-12,14-15,17H,2,7-10,13H2,1H3
SMILES Code
CCC1=CN=C(N2CCC(C3=NC(COC4=CC=C(N5N=NN=C5)C=C4)=CS3)CC2)N=C1
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, not in water
Shelf Life
>2 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
Biological target:
MBX-2982 is a selective, orally-available G protein-coupled receptor 119 (GPR119) agonist.
In vitro activity:
The advantage of NAD coenzyme vs. thio-NAD is proven. Manifest activation of glucokinase by MBX-2982 compound (GPR119 agonist) in a wide range of concentrations is demonstrated experimentally. Reference: Bull Exp Biol Med. 2017 Sep;163(5):695-698. https://pubmed.ncbi.nlm.nih.gov/28944428/
In vivo activity:
Oral administration of MBX (MBX-2982) in mice fed a high-fat diet potently inhibited hepatic lipid accumulation and expression levels of SREBP-1 and lipogenesis-related genes, whereas the hepatic antilipogenesis effects of MBX were abolished in GPR119 KO mice. MBX activated AMPK and increased Ser-372 phosphorylation of SREBP-1c, an inhibitory form of SREBP-1c. Moreover, inhibition of AMPK recovered MBX-induced down-regulation of SREBP-1. Reference: FASEB J. 2016 Jan;30(1):324-35. https://pubmed.ncbi.nlm.nih.gov/26399788/
Solvent mg/mL mM
Solubility
DMSO 50.0 111.47
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 448.54 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.

Recalculate based on batch purity %
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. Spasov AA, Kosolapov VA, Babkov DA, Maika OY. Effect of GRP119 Receptor Agonist, Compound MBX-2982, on Activity of Human Glucokinase. Bull Exp Biol Med. 2017 Sep;163(5):695-698. doi: 10.1007/s10517-017-3881-0. Epub 2017 Sep 25. PMID: 28944428. 2. Yang JW, Kim HS, Im JH, Kim JW, Jun DW, Lim SC, Lee K, Choi JM, Kim SK, Kang KW. GPR119: a promising target for nonalcoholic fatty liver disease. FASEB J. 2016 Jan;30(1):324-35. doi: 10.1096/fj.15-273771. Epub 2015 Sep 23. PMID: 26399788.
In vitro protocol:
1. Spasov AA, Kosolapov VA, Babkov DA, Maika OY. Effect of GRP119 Receptor Agonist, Compound MBX-2982, on Activity of Human Glucokinase. Bull Exp Biol Med. 2017 Sep;163(5):695-698. doi: 10.1007/s10517-017-3881-0. Epub 2017 Sep 25. PMID: 28944428.
In vivo protocol:
1. Yang JW, Kim HS, Im JH, Kim JW, Jun DW, Lim SC, Lee K, Choi JM, Kim SK, Kang KW. GPR119: a promising target for nonalcoholic fatty liver disease. FASEB J. 2016 Jan;30(1):324-35. doi: 10.1096/fj.15-273771. Epub 2015 Sep 23. PMID: 26399788.
1: Kang SU. GPR119 agonists: a promising approach for T2DM treatment? A SWOT analysis of GPR119. Drug Discov Today. 2013 Dec;18(23-24):1309-15. doi: 10.1016/j.drudis.2013.09.011. Epub 2013 Sep 20. PubMed PMID: 24060477.