[CAS NO. 254737-29-6] 2-MPPA
PRODUCTS SPECIFICATIONS [254737-29-6]
DESCRIPTION [254737-29-6]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 206.26 |
| Molecular Formula | C8H14O4S |
| SMILES | O=C(O)C(CCCS)CCC(O)=O |
Summary
2-MPPA (GPI-5693) is an orally active and selective glutamate carboxypeptidase II (GCP II; PSMA) inhibitor with an IC 50 of 90 nM [1] [2] .
IC50 & Target
IC 50 : 90 nM (GCP II) [2]
In Vivo
2-MPPA (10, 30 or 100 mg/kg) significantly attenuates Dizocilpine (HY-15084B) (0.1 mg/kg)-induced prepulse inhibition (PPI) deficits in mice, in a dose dependent manner. The efficacy of 2-MPPA on dizocilpine-induced PPI deficits is significantly antagonized by pretreatment with the selective group II metabotropic glutamate receptor (mGluR) antagonist LY341495 (HY-70059) (1.0 mg/kg)
[1]
.
2-MPPA (30 mg/kg) significantly prevents the deficit in SNCV induced by both 5 and 25 mg/kg taxol by 96.3 ± 4.4% and 98.3± 11.6% respectively
[2]
.
2-MPPA (10 mg/kg) inhibits tumor growth in the high expressor PSMA model CWR22RS by 70%
[2]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Oil
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Pure form | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 100 mg/mL ( 484.82 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 4.8482 mL | 24.2412 mL | 48.4825 mL |
| 5 mM | 0.9697 mL | 4.8482 mL | 9.6965 mL |
| 10 mM | 0.4848 mL | 2.4241 mL | 4.8482 mL |
References
- [1] Takatsu Y, et al. Orally active glutamate carboxypeptidase II inhibitor 2-MPPA attenuates dizocilpine-induced prepulse inhibition deficits in mice. Brain Res. 2011 Jan 31;1371:82-6.
- [2] She Y, et al. 2-MPPA, a selective inhibitor of PSMA, delays prostate cancer growth and attenuates taxol-induced neuropathy in mice. Journal of Clinical Oncology, 2005, 23(16_suppl): 8054-8054.