CPP-115 hydrochloride 

CPP-115 hydrochloride is an orally active, selective GABA-AT inhibitor with a K_i value of 9.7 μM. CPP-115 hydrochloride blocks GABA degradation and increases GABA levels in the brain. CPP-115 hydrochloride does not bind to GABA transporters, does not displace GABA from GABA_A/GABA_B receptors, and does not act as an agonist/antagonist of GABA_C receptors. CPP-115 hydrochloride reduces cocaine-induced dopamine release, blocks cocaine-induced conditioned place preference, and suppresses seizure activity in a rat model of infantile spasms. CPP-115 hydrochloride can be used in research related to infantile spasms and epilepsy^[1][2].

CPP-115 hydrochloride potently and irreversibly inactivates GABA-AT with a k_inact/K_I of 52 mM·min^-1, 187 times more efficiently than vigabatrin^[1].
CPP-11 (6 mM) hydrochloride does not exhibit inhibitory or inactivating activity against alanine aminotransferase or aspartate aminotransferase at concentrations up to 6 mM^[1].
CPP-115 (0-4.0 equiv; up to 120 h) hydrochloride time-dependently inactivates pig brain GABA-AT with a turnover number of 1.3 per active site, with greater inactivation observed at higher equivalents of the compound^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

CPP-115 (1 mg/kg) hydrochloride completely blocks the expression of cocaine-induced conditioned place preference in rats, with efficacy comparable to that of 300 mg/kg Vigabatrin^[1].
CPP-115 (1 mg/kg) hydrochloride reduces cocaine-induced dopamine release in the nucleus accumbens (NAcc) of rats to 250% of the basal level, and its potency is over 300 times higher than that of Vigabatrin^[1].
CPP-115 (0.1-1 mg/kg) hydrochloride suppresses seizure episodes in the adrenocorticotropic hormone (ACTH)-resistant multi-hit infantile spasm rat model, with a potency 100-fold higher than that of Vigabatrin and better tolerability^[1].
CPP-115 (20 mg/kg per day for 45 consecutive days) hydrochloride causes only 5%-30% loss of electroretinogram in rats after 45 days of administration, showing extremely low retinal toxicity compared to the effective dose of Vigabatrin^[1].
CPP-115 (0.7-7 mg/kg/day; p.o.; daily; 28 days) hydrochloride is well tolerated in healthy Beagle dogs^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

213.61

C₇H₁₀ClF₂NO₂

760947-97-5

OC([C@H]1C/C([C@H](C1)N)=C(F)\F)=O.Cl

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Silverman RB. The 2011 E. B. Hershberg award for important discoveries in medicinally active substances: (1S,3S)-3-amino-4-difluoromethylenyl-1-cyclopentanoic acid (CPP-115), a GABA aminotransferase inactivator and new treatment for drug addiction and infantile spasms. J Med Chem. 2012 Jan 26;55(2):567-75.  [Content Brief]

  [2]. Lee H, et al. Mechanism of inactivation of γ-aminobutyric acid aminotransferase by (1S,3S)-3-amino-4-difluoromethylene-1-cyclopentanoic acid (CPP-115). Journal of the American Chemical Society. 2015 Feb 25;137(7):2628-40.  [Content Brief]