2. Metabolic Enzyme/Protease
  3. Glucokinase
  4. BMS-820132

BMS-820132 is an orally active and partial glucokinase (GK) activator with a AC50 of 29 nM. BMS-820132 decreases the glucose levels in glucose tolerance test (OGTT) model in normal rats, but not Zucker diabetic fatty (ZDF) rats. BMS-820132 exhibits pharmacological toxicity secondary to strong GK activation.

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BMS-820132 Chemical Structure

BMS-820132 Chemical Structure

CAS No. : 1001419-18-6

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 1 publication(s) in Google Scholar

BMS-820132 Related Antibodies

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Description

BMS-820132 is an orally active and partial glucokinase (GK) activator with a AC50 of 29 nM. BMS-820132 decreases the glucose levels in glucose tolerance test (OGTT) model in normal rats, but not Zucker diabetic fatty (ZDF) rats. BMS-820132 exhibits pharmacological toxicity secondary to strong GK activation[1][2].

In Vivo

BMS-820132 (compound 31) (3 μmol/kg, 30 μmol/kg; po; single dose) decreases glucose levels in high-fat diet-induced obese (DIO) mice, in an oral glucose tolerance test (OGTT)[1].
BMS-820132 (10-200 mg/kg; po; once daily for 1 mo) results in body weight reduction in normal rat but not ZDF rats, indicating that the toxicity is secondary to the exaggerated pharmacology of potent GK activation[2].
BMS-820132 (10 mg/kg, 60 mg/kg, 120 mg/kg; po; once daily for 1 mo) results insignificant effects on dogs food consumption[2].

Pharmacokinetic Analysis in Animal Model[1]

Route Dose (mg/kg) Cmax (μM) Tmax (h) AUC0-24 h (μM·h) T1/2 (h) CLTp (mL/min/kg) Vss (L/kg) F (L/kg)
mouse iv 2.5 24.9 2.1 2.9 0.3
po 5 14.1 0.5 49.7 100
rat iv 2.5 16.6 0.9 4.4 0.3
po 5 13.0 0.9 29.5 90
dog iv 3 12.3 1.8 7.2 0.5
po 3 4.9 0.8 8.0 66
monkey iv 3 3.8 1.9 22.7 1.1
po 3 3.8 1.3 0.57 15

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Zucker diabetic fatty (ZDF) rats and normal SD rats[2]
Dosage: 10 mg/kg, 50 mg/kg, 200 mg/kg
Administration: PO; once daily for 1 month
Result: Resulted reductions in body weight gains starting on day 7 in SD rats (11% lower than controls), but not ZDF rats.
Animal Model: Beagle dogs[2]
Dosage: 10 mg/kg, 60 mg/kg, 120 mg/kg
Administration: PO; once daily for 1 month
Result: There were no meaningful differences in food consumption in dogs model.
Clinical Trial
Molecular Weight

572.55

Formula

C26H33N6O7P
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(NC1=NN(CP(OCC)(OCC)=O)C=C1)C2=CC(OC(C)C)=CC(OC3=NC=C(C(N4CCC4)=O)N=C3)=C2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (43.66 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7466 mL 8.7329 mL 17.4657 mL
5 mM 0.3493 mL 1.7466 mL 3.4931 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (4.37 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (4.37 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.7466 mL 8.7329 mL 17.4657 mL 43.6643 mL
5 mM 0.3493 mL 1.7466 mL 3.4931 mL 8.7329 mL
10 mM 0.1747 mL 0.8733 mL 1.7466 mL 4.3664 mL
15 mM 0.1164 mL 0.5822 mL 1.1644 mL 2.9110 mL
20 mM 0.0873 mL 0.4366 mL 0.8733 mL 2.1832 mL
25 mM 0.0699 mL 0.3493 mL 0.6986 mL 1.7466 mL
30 mM 0.0582 mL 0.2911 mL 0.5822 mL 1.4555 mL
40 mM 0.0437 mL 0.2183 mL 0.4366 mL 1.0916 mL
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BMS-820132 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

BMS-8201321001419-18-6BMS820132BMS 820132GlucokinaseHexokinase IVHexokinase Dtype 2 diabetesglucose homeostasisInhibitorinhibitorinhibit

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