MB-05032
- Product Name
- MB-05032
- CAS No.
- 261365-11-1
- Chemical Name
- MB-05032
- Synonyms
- MB-05032;MB-05032; MB05032;2-Amino-5-isobutyl-4-[5-phosphono-2-furanyl]thiazole;[5-(2-Amino-5-isobutyl-1,3-thiazol-4-yl)-2-furyl]phosphonic acid;P-[5-[2-Amino-5-(2-methylpropyl)-4-thiazolyl]-2-furanyl]phosphonic acid;Phosphonic acid, P-[5-[2-amino-5-(2-methylpropyl)-4-thiazolyl]-2-furanyl]-
- CBNumber
- CB62628073
- Molecular Formula
- C11H15N2O4PS
- Formula Weight
- 302.29
- MOL File
- 261365-11-1.mol
MB-05032 Property
- Boiling point:
- 576.7±60.0 °C(Predicted)
- Density
- 1.47±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- Soluble in DMSO
- form
- Powder
- pka
- 0.98±0.10(Predicted)
- color
- Off-white to yellow
N-Bromosuccinimide Price
- Product number
- SML3207
- Product name
- MB05032
- Purity
- ≥98% (HPLC)
- Packaging
- 5MG
- Price
- $100
- Updated
- 2024/03/01
- Product number
- SML3207
- Product name
- MB05032
- Purity
- ≥98% (HPLC)
- Packaging
- 25MG
- Price
- $323
- Updated
- 2024/03/01
- Product number
- 6618
- Product name
- MB05032
- Purity
- ≥98%(HPLC)
- Packaging
- 10
- Price
- $212
- Updated
- 2021/12/16
- Product number
- 6618
- Product name
- MB05032
- Purity
- ≥98%(HPLC)
- Packaging
- 50
- Price
- $891
- Updated
- 2021/12/16
- Product number
- A3586
- Product name
- MB05032
- Packaging
- 2mg
- Price
- $221
- Updated
- 2021/12/16
MB-05032 Chemical Properties,Usage,Production
Biological Activity
mb05032 is a potent and selective gng inhibitor targeted the amp binding site of fructose 1,6-bisphosphatase (fbpase) with an ic50 value of 16 nm [1].gluconeogenesis (gng) is a metabolic pathway which could result in the generation of glucose from certain non-carbohydratecarbon substrates.
in vitro
mb06322 inhibited glucose synthesis by human hepatocytes over a narrow concentration range with full inhibition achieved at 1 μm in a concentration-dependent manner [2]. mb05032 inhibited human liver fbpase with a potency (ic50 of 16 ± 1.5 nm) significantly greater than the natural inhibitor, amp (ic50 of 1 μm), and the most well characterized amp mimetic, zmp (ic50of 12 ± 1.4 μm). mb05032 inhibited rat fbpase 3-fold weaker (ic50 of 61 ± 4 nm) than human fbpase, whereas amp was 20-fold weaker as an inhibitor [1]. in islet β-cells,inhibition of fbpase activity by mb05032 led to a significant increase of their glucose utilization and cellular atp to adp ratios and consequently enhanced gsis in vitro [2].
in vivo
in male zdf rats, oral administration of mb06322 resulted in dose-dependent inhibition of [14c]bicarbonate incorporation into glucose. maximal gng inhibition (≈80%) is achieved at 100–300 mg/kg mb06322. in mb06322-treated rats, intermediates upstream of fbpase were elevated 1.5- to 3.1-fold relative to vehicle-treated mice. mb06322 treatment also resulted in elevated lactate levels (79%) only in aged zdf rats. [2]. oral administration of mb06322 to young (8–9 weeks old) zdf rats with mild diabetes (basal insulin levels of 7.7 ± 0.7 ng/ml) and aged (12–13 weeks) zdf rats with overt diabetes (basal insulin levels of 0.65 ± 0.16 ng/ml) lowered the level of glucose in a dose-dependent manner [1]. the dose–dependent response is relatively steep, with 6–10 mg/kg and 30–100 mg/kg being the approximate doses associated with minimal and maximal activity, respectively. after drug administration 2.5–5 h, glucose lowering occurs rapidly with maximal effects [1].
target
IC50: 16 nM (Human Liver FBPase)
storage
Store at -20°C
References
[1] erion m d, van poelje p d, dang q, et al. mb06322 (cs-917): a potent and selective inhibitor of fructose 1, 6-bisphosphatase for controlling gluconeogenesis in type 2 diabetes[j]. proceedings of the national academy of sciences, 2005, 102(22): 7970-7975.
[2] zhang y, xie z, zhou g, et al. fructose-1, 6-bisphosphatase regulates glucose-stimulated insulin secretion of mouse pancreatic β-cells[j]. endocrinology, 2010, 151(10): 4688-4695.
MB-05032 Preparation Products And Raw materials
Raw materials
Preparation Products
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