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
- Molecular Weight:
- 302.29
- MDL Number:
- MFCD14584901
- MOL File:
- 261365-11-1.mol
- MSDS File:
- SDS
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) |
FDA UNII | 9379MH4CAL |
MB-05032 price
Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
---|---|---|---|---|---|---|---|
Sigma-Aldrich | SML3207 | MB05032 ≥98% (HPLC) | 261365-11-1 | 5MG | $100 | 2024-03-01 | Buy |
Sigma-Aldrich | SML3207 | MB05032 ≥98% (HPLC) | 261365-11-1 | 25MG | $323 | 2024-03-01 | Buy |
Tocris | 6618 | MB05032 ≥98%(HPLC) | 261365-11-1 | 10 | $212 | 2021-12-16 | Buy |
Tocris | 6618 | MB05032 ≥98%(HPLC) | 261365-11-1 | 50 | $891 | 2021-12-16 | Buy |
ChemScene | CS-1552 | MB05032 99.69% | 261365-11-1 | 50mg | $960 | 2021-12-16 | Buy |
MB-05032 Chemical Properties,Uses,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
MB-05032 Suppliers
Supplier | Tel | Country | ProdList | Advantage | |
---|---|---|---|---|---|
TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 19892 | 58 |
Career Henan Chemica Co | +86-0371-86658258 15093356674; | laboratory@coreychem.com | China | 30255 | 58 |
Aladdin Scientific | +1-833-552-7181 | sales@aladdinsci.com | United States | 57511 | 58 |
Haoyuan Chemexpress Co., Ltd. | 021-58950125 | info@chemexpress.com | China | 7553 | 61 |
MedChemexpress LLC | 021-58955995 | sales@medchemexpress.cn | United States | 4863 | 58 |
ShangHai Caerulum Pharma Discovery Co., Ltd. | 18149758185 | sales-cpd@caerulumpharma.com | China | 3421 | 58 |
HuBei ShengBaoLai Biological Technology Co., Ltd | 027-027-59105235 13007105135 | sbl1120@163.com | China | 107 | 55 |
SPIRO PHARMA | eric_feng1954@126.com | China | 9254 | 55 | |
Codow Chemical Co.,Ltd. | 18620099427 | amy@howeipharm.com | China | 17698 | 55 |
Shanghai EFE Biological Technology Co., Ltd. | 021-65675885 18964387627 | info@efebio.com | China | 9709 | 58 |