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

BMS-820132 

Cat. No.: HY-144289 Purity: 99.39%
COA Handling Instructions

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.

For research use only. We do not sell to patients.

BMS-820132 Chemical Structure

BMS-820132 Chemical Structure

CAS No. : 1001419-18-6

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10 mg USD 750 In-stock
25 mg USD 1500 In-stock
50 mg USD 2400 In-stock
100 mg USD 3800 In-stock
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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

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

Appearance

Solid

Formula

C26H33N6O7P
CAS No.
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)

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
10 mM 0.1747 mL 0.8733 mL 1.7466 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are available by MCE.
Purity & Documentation
References
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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.

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Keywords:

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

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