| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 50mg |
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| 100mg | |||
| Other Sizes |
| Targets |
Fructose-1,6-bisphosphatase (FBPase), specifically the AMP-binding site of the enzyme.
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|---|---|
| ln Vitro |
MB 05032 demonstrates potent inhibitory activity against FBPase with EC50 values of 1.6 nM for human liver FBPase, 29 nM for human muscle FBPase, and 61 nM for rat liver FBPase. It promotes glycolysis, glucose uptake, and lactate production in umbilical cord blood CD34+ cells.
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| ln Vivo |
MB06322 (3/6-300 mg/kg [young/old Zucker diabetic body weight (ZDF); impact; one time) kills Zucker diabetics in their youth and kills older ZDF with overt diabetes in their senior years Draw model
In primary NSG mouse recipients, MB 05032 increases engraftment of hematopoietic stem cells. It also enhances myeloid and lymphoid chimerism in secondary NSG mouse recipients, indicating its ability to promote long-term hematopoietic reconstitution. |
| Enzyme Assay |
FBPase enzyme activity is measured using a coupled enzyme assay system. Recombinant human liver FBPase is incubated with varying concentrations of MB 05032 in assay buffer containing fructose-1,6-bisphosphate, NADP+, and auxiliary enzymes. The reaction is initiated by addition of substrate, and the decrease in absorbance at 340 nm is monitored to determine IC50/EC50 values.
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| Cell Assay |
Human umbilical cord blood CD34+ hematopoietic stem and progenitor cells are cultured with increasing concentrations of MB 05032. Glycolysis is assessed by measuring glucose consumption and lactate production in the culture medium. Cell expansion is evaluated by counting viable cells and analyzing surface marker expression via flow cytometry after several days of culture.
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| Animal Protocol |
Animal/Disease Models: ZDF rat (8 - to 9 weeks of age (mild diabetes) and 12- to 13 weeks of age (overt diabetes)) [1]
Doses: 3, 6, 10, 30, 300 mg/kg (young ZDF rats); 6, 10 , 30, 300 mg/kg (aged ZDF rats) Route of Administration: oral; Experimental Results:Causes dose-dependent reduction in blood sugar. MB 05032 is administered to immunodeficient NSG mice, and hematopoietic stem cell engraftment is evaluated. Primary recipients receive human CD34+ cells with or without MB 05032 treatment; engraftment is measured by human CD45+ cell chimerism in peripheral blood and bone marrow. Secondary transplantation is performed to assess long-term repopulating capacity. |
| ADME/Pharmacokinetics |
MB 05032 is a small molecule with molecular weight 302.29 and formula C11H15N2O4PS. It is typically administered via oral or parenteral routes in preclinical studies. As a FBPase inhibitor, it reduces gluconeogenesis and lowers endogenous glucose production. Detailed pharmacokinetic parameters such as half-life, bioavailability, and clearance are available in primary research publications.
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| Toxicity/Toxicokinetics |
Preclinical toxicity data for MB 05032 are limited. As a research compound targeting metabolic pathways, it is expected to have a manageable safety profile at efficacious doses. Standard toxicological assessments including acute and repeated-dose toxicity studies would be required for clinical development. No significant off-target effects have been reported in published literature.
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| References |
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| Additional Infomation |
MB 05032 is a research tool for studying gluconeogenesis inhibition and HSC expansion. Its mechanism involves binding to the AMP site of FBPase, thereby mimicking the natural inhibitor AMP. This compound has been investigated for potential applications in type 2 diabetes (by reducing hepatic glucose production) and in stem cell transplantation (by expanding HSCs ex vivo). No clinical trials or approved therapeutic indications exist for this compound.
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| Molecular Formula |
C11H15N2O4PS
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|---|---|
| Molecular Weight |
302.2848
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| Exact Mass |
302.049
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| CAS # |
261365-11-1
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| Related CAS # |
261365-09-7 (HBr);261365-11-1;
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| PubChem CID |
11289630
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| Appearance |
Off-white to yellow solid powder
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| LogP |
2.568
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
19
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| Complexity |
365
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
XJMYIJPPDSZOPN-UHFFFAOYSA-N
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| 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)
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| Chemical Name |
[5-[2-amino-5-(2-methylpropyl)-1,3-thiazol-4-yl]furan-2-yl]phosphonic acid
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| Synonyms |
MB-05032 MB05032 MB 05032
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~165.40 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.27 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (8.27 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (8.27 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.3082 mL | 16.5410 mL | 33.0819 mL | |
| 5 mM | 0.6616 mL | 3.3082 mL | 6.6164 mL | |
| 10 mM | 0.3308 mL | 1.6541 mL | 3.3082 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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