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MB05032 

Cat. No.: HY-16307 Purity: >98.0%
Data Sheet SDS Handling Instructions

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

For research use only. We do not sell to patients.
MB05032 Chemical Structure

MB05032 Chemical Structure

CAS No. : 261365-11-1

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 264 In-stock
5 mg USD 240 In-stock
10 mg USD 360 In-stock
50 mg USD 960 In-stock
100 mg USD 1680 In-stock
200 mg   Get quote  
500 mg   Get quote  

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  • Biological Activity

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Description

MB05032 is a special and efficacious GNG inhibitor targeted the AMP binding site of fructose 1,6-bisphosphatase (FBPase) with an IC50 value of 16 nM. IC50 Value: 16 nM (Human Liver FBPase) [1] Target: Fructose 1, 6-bisphosphatase Oral delivery of MB05032 was achieved by using the bisamidate prodrug MB06322 (CS-917), which is converted to MB05032 in two steps through the action of an esterase and a phosphoramidase. in vitro: 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). MB05032 inhibits rat FBPase 3-fold weaker (IC50 of 61 ± 4 nM) than human FBPase, whereas AMP is 20-fold weaker as an inhibitor [1]. Inhibition of FBPase activity in islet β-cells by its specific inhibitor MB05032 led to significant increase of their glucose utilization and cellular ATP to ADP ratios and consequently enhanced GSIS in vitro [2]. in vivo: 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) results in dose-dependent glucose lowering. The dose-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 [1]. Pretreatment of mice with the MB05032 prodrug MB06322 could potentiate GSIS in vivo and improve their glucose tolerance [2]. Toxicity: Neither lactate nor triglycerides increased in 8- to 9-week-old ZDF rats with mild diabetes treated with high doses of MB06322. In ZDF rats with more advanced disease, lactate and triglyceride levels were elevated but only modestly (<2-fold). These results suggest that, unlike inhibitors of other GNG enzymes, FBPase inhibitors may lower glucose with an adequate safety margin [1]. Clinical trial: Evaluation of Glucose Lowering Effect, Safety and Tolerability of CS-917. Phase 2b

References
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 3.3081 mL 16.5404 mL 33.0808 mL
5 mM 0.6616 mL 3.3081 mL 6.6162 mL
10 mM 0.3308 mL 1.6540 mL 3.3081 mL
Please refer to the solubility information to select the appropriate solvent.
References
Molecular Weight

302.29

Formula

C₁₁H₁₅N₂O₄PS

CAS No.

261365-11-1

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Product Name:
MB05032
Cat. No.:
HY-16307
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