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PD 168368 

Cat. No. M29125
PD 168368  Structure
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Biological Activity

PD 168368 is a potent, competitive, and selective neuromedin B receptor (NMB-R) antagonist with the Ki of 15–45 nM. PD 168368 is neuromedin B receptor (NMBR; IC50=96 nM) / gastrin-releasing peptide receptor (GRPR IC50=3500 nM) antagonist. PD 168368 also is a mixed FPR1/FPR2/FPR3 agonist with EC50s of 0.57, 0.24, and 2.7 nM, respectively.

Chemical Information
Molecular Weight 554.64
Formula C31H34N6O4
CAS Number 204066-82-0
Form Solid
Solubility (25°C) DMSO 30 mg/mL (Need ultrasonic and warming)
DMF 10 mg/mL (Need ultrasonic and warming)
Storage Powder -20°C
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] Gabriela Silva Monteiro de Paula, et al. J Mol Endocrinol. Neuromedin B receptor disruption impairs adipogenesis in mice and 3T3-L1 cells

[2] Sarah Ehling, et al. Acta Derm Venereol. Neuromedin B Induces Acute Itch in Mice via the Activation of Peripheral Sensory Neurons

[3] Hyun-Joo Park, et al. Int J Oncol. Neuromedin B receptor antagonism inhibits migration, invasion, and epithelial-mesenchymal transition of breast cancer cells

[4] Hyun-Joo Park, et al. Cancer Lett. Neuromedin B receptor antagonist suppresses tumor angiogenesis and tumor growth in vitro and in vivo

[5] R R Ryan, et al. J Pharmacol Exp Ther. Comparative pharmacology of the nonpeptide neuromedin B receptor antagonist PD 168368

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  Catalog
Abmole Inhibitor Catalog




Keywords: PD 168368  supplier, Bombesin Receptor, inhibitors, activators


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