MBX-2982
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MedKoo CAT#: 501203

CAS#: 1037792-44-1

Description: 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

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MBX-2982
CAS# 1037792-44-1

Theoretical Analysis

MedKoo Cat#: 501203
Name: MBX-2982
CAS#: 1037792-44-1
Chemical Formula: C22H24N8OS
Exact Mass: 448.18
Molecular Weight: 448.544
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 2 weeks
50mg USD 450 2 weeks
100mg USD 750 2 weeks
200mg USD 1150 2 weeks
500mg USD 1950 2 weeks
1g USD 2950 2 weeks
2g USD 4950 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/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 50.0 111.47

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.

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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.