MB-05032 (MB05032) is a novel and potent gluconeogenesis inhibitor and FBPase (fructose 1,6-bisphosphatase) inhibitor with an IC50 value of 16 nM, targeting the AMP binding site of FBPase.
Physicochemical Properties
| Molecular Formula | C11H15N2O4PS |
| Molecular Weight | 302.2848 |
| Exact Mass | 302.049 |
| CAS # | 261365-11-1 |
| Related CAS # | 261365-09-7 (HBr);261365-11-1; |
| PubChem CID | 11289630 |
| Appearance | Off-white to yellow solid powder |
| LogP | 2.568 |
| Hydrogen Bond Donor Count | 3 |
| Hydrogen Bond Acceptor Count | 7 |
| Rotatable Bond Count | 4 |
| Heavy Atom Count | 19 |
| Complexity | 365 |
| Defined Atom Stereocenter Count | 0 |
| 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) |
| Chemical Name | [5-[2-amino-5-(2-methylpropyl)-1,3-thiazol-4-yl]furan-2-yl]phosphonic acid |
| Synonyms | MB-05032 MB05032 MB 05032 |
| HS Tariff Code | 2934.99.9001 |
| 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) |
Biological Activity
| 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 |
| 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. |
| References |
[1]. 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. [2]. Fructose-1,6-bisphosphatase regulates glucose-stimulated insulin secretion of mouse pancreatic beta-cells. Endocrinology. 2010 Oct;151(10):4688-95. |
Solubility Data
| Solubility (In Vitro) | DMSO : ~50 mg/mL (~165.40 mM) |
| 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. 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. 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 corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| 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 |