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(S)-PMPA

Cat. No. M6270
(S)-PMPA Structure
Synonym:

Phosphonic acid

Size Price Availability Quantity
10mg USD 220  USD220 In stock
50mg USD 420  USD420 In stock
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Quality Control & Documentation
Biological Activity

For the development of PSMA ligands, the structurally unrelated PSMA inhibitor 2-(phosphonomethyl)pentanedioic acid (PMPA) is commonly used as a competitor in blocking studies to demonstrate the specific binding of the molecule of interest. In this respect, simultaneous coinjection of a 50 mg/kg dose of PMPA resulted in complete blocking of MIP1095 binding sites in tumor and kidneys

Protocol (for reference only)
Cell Experiment
Cell lines
Preparation method
Concentrations
Incubation time
Animal Experiment
Animal models Mice bearing LNCaP tumors
Formulation HEPES buffered saline
Dosages 50, 10, 1, or 0.2 mg/kg
Administration i.p.
Chemical Information
Molecular Weight 287.21
Formula C9H14N5O4P
CAS Number 147127-19-3
Form Solid
Solubility (25°C) 10 mM in DMSO
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] Rais R, et al. PLoS One. Selective CNS Uptake of the GCP-II Inhibitor 2-PMPA following Intranasal Administration.

[2] Kratochwil C, et al. J Nucl Med. PMPA for nephroprotection in PSMA-targeted radionuclide therapy of prostate cancer.

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