MB 05032 | CAS#261365-11-1 | inhibitor

MedKoo Cat#: 584753 | Name: MB 05032

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Description:

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

MB 05032 is a potent FBPase inhibitor that promotes HSC expansion.

Chemical Structure

MB 05032

CAS#261365-11-1 (free base)

Theoretical Analysis

MedKoo Cat#: 584753

Name: MB 05032

CAS#: 261365-11-1 (free base)

Chemical Formula: C11H15N2O4PS

Exact Mass: 302.0490

Molecular Weight: 302.28

Elemental Analysis: C, 43.71; H, 5.00; N, 9.27; O, 21.17; P, 10.25; S, 10.61

Price and Availability

Size	Price	Availability	Quantity
5mg	USD 350.00	2 weeks
25mg	USD 800.00	2 weeks

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Related CAS #

261365-09-7 (HBr) 261365-11-1 (free base)

Synonym

MB 05032; MB05032; MB-05032

IUPAC/Chemical Name

P-[5-[2-Amino-5-(2-methylpropyl)-4-thiazolyl]-2-furanyl]phosphonic acid

InChi Key

XJMYIJPPDSZOPN-UHFFFAOYSA-N

InChi Code

InChI=1S/C11H15N2O4PS/c1-6(2)5-8-10(13-11(12)19-8)7-3-4-9(17-7)18(14,15)16/h3-4,6H,5H2,1-2H3,(H2,12,13)(H2,14,15,16)

SMILES Code

OP(O)(C1=CC=C(C2=C(CC(C)C)SC(N)=N2)O1)=O

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

Instruction

View handling instruction

Biological target:

MB05032 is a special and efficacious gluconeogenesis inhibitor targeted the AMP binding site of fructose 1,6-bisphosphatase (FBPase) with an IC50 value of 16 nM.

In vitro activity:

MB05032 inhibits human liver FBPase with a potency (IC50 = 16 ± 1.5 nM) significantly greater than the natural inhibitor, AMP (IC50 = 1 μM), and the most well characterized AMP mimetic, ZMP (IC50 = 12 ± 1.4 μM) (Fig. 2 and Table 1). MB05032 displaces [14C]AMP bound to FBPase in a concentration-dependent manner confirming the AMP site as the site of interaction. Reference: Proc Natl Acad Sci U S A. 2005 May 31;102(22):7970-5. https://pubmed.ncbi.nlm.nih.gov/15911772/

In vivo activity:

Pretreatment of mice with the MB05032 prodrug MB06322 could potentiate GSIS in vivo and improve their glucose tolerance. Therefore, FBPase plays an important role in regulating glucose sensing and insulin secretion of β-cells and serves a promising target for diabetes treatment. Reference: Endocrinology. 2010 Oct;151(10):4688-95. https://pubmed.ncbi.nlm.nih.gov/20719858/

	Solvent	mg/mL	mM
Solubility
	DMSO	40.1	132.71

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 302.28 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. Erion MD, van Poelje PD, Dang Q, Kasibhatla SR, Potter SC, Reddy MR, Reddy KR, Jiang T, Lipscomb WN. MB06322 (CS-917): A potent and selective inhibitor of fructose 1,6-bisphosphatase for controlling gluconeogenesis in type 2 diabetes. Proc Natl Acad Sci U S A. 2005 May 31;102(22):7970-5. doi: 10.1073/pnas.0502983102. Epub 2005 May 23. PMID: 15911772; PMCID: PMC1138262. 2. Zhang Y, Xie Z, Zhou G, Zhang H, Lu J, Zhang WJ. Fructose-1,6-bisphosphatase regulates glucose-stimulated insulin secretion of mouse pancreatic beta-cells. Endocrinology. 2010 Oct;151(10):4688-95. doi: 10.1210/en.2009-1185. Epub 2010 Aug 18. PMID: 20719858.

In vitro protocol:

In vivo protocol:

1. Zhang Y, Xie Z, Zhou G, Zhang H, Lu J, Zhang WJ. Fructose-1,6-bisphosphatase regulates glucose-stimulated insulin secretion of mouse pancreatic beta-cells. Endocrinology. 2010 Oct;151(10):4688-95. doi: 10.1210/en.2009-1185. Epub 2010 Aug 18. PMID: 20719858.

Guo et al (2018) Antagonism of PPAR-γ signaling expands human hematopoietic stem and progenitor cells by enhancing glycolysis. Nat.Med. 24 360 PMID: 29377004 van Poelje et al (2011) Fructose-1, 6-bisphosphatase inhibitors for reducing excessive endogenous glucose production in type 2 diabetes. Handb.Exp.Pharmacol. 203 279 PMID: 21484576