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PB-201

Cat. No. M31408
PB-201 Structure
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Biological Activity

PB-201 is a glucokinase activator (GKA) that can be used in studies related to type 2 diabetes.

Chemical Information
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Miao Zhang, et al. CPT Pharmacometrics Syst Pharmacol. Development of a PBPK model to quantitatively understand absorption and disposition mechanism and support future clinical trials for PB-201

[2] Ying Du, et al. Diabetes Obes Metab. A multicentre, randomized, double-blind, parallel, active- and placebo-controlled Phase 3 clinical study of the glucokinase activator PB-201 in treatment-naive patients with type 2 diabetes mellitus: A study protocol

[3] Yixin Ren, et al. J Enzyme Inhib Med Chem. Glucokinase as an emerging anti-diabetes target and recent progress in the development of its agonists

[4] Dongyang Liu, et al. EClinicalMedicine. Safety, tolerability, pharmacokinetics, and pharmacodynamics of the glucokinase activator PB-201 and its effects on the glucose excursion profile in drug-naïve Chinese patients with type 2 diabetes: a randomised controlled, crossover, single-centre phase 䲧癐Ỵ癑

[5] F Tárkányi, et al. Appl Radiat Isot. Investigation of activation cross-sections of proton induced nuclear reactions on natTl up to 42MeV: review, new data and evaluation

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Keywords: PB-201 supplier, Glucokinase (GK), inhibitors, activators


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