A GAPDH ligand
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CGP 3466 (maleate)

Item No. 23362

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-methyl-N-2-propyn-1-yl-dibenz[b,f]oxepin-10-methanamine, (2Z)-2-butenedioate
CAS Number
200189-97-5
Synonyms
  • CGP 3466B
Molecular Formula
C19H17NO • C4H4O4
Formula Weight
391.4
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 20 mg/mlDMSO: 20 mg/mlEthanol: 0.5 mg/mlPBS (pH 7.2): 0.5 mg/ml
λmax
205, 282 nm
SMILES
CN(CC#C)CC1=CC2=CC=CC=C2OC3=C1C=CC=C3.OC(/C=C\C(O)=O)=O
InChi Code
InChI=1S/C19H17NO.C4H4O4/c1-3-12-20(2)14-16-13-15-8-4-6-10-18(15)21-19-11-7-5-9-17(16)19;5-3(6)1-2-4(7)8/h1,4-11,13H,12,14H2,2H3;1-2H,(H,5,6)(H,7,8)/b;2-1-
InChi Key
SQAZQLMBEHYFJA-BTJKTKAUSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $33

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    5 mg

    $115

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    Product Description

    CGP 3466 is a GAPDH ligand.1,2 Immobilized CGP 3466 binds to GAPDH from rat hippocampus extracts and to purified recombinant rabbit muscle GAPDH using affinity purification.2 CGP 3466 reduces PAJU cell apoptosis induced by rotenone (Item No. 13995). CGP 3466 dose-dependently increases survival of trophically withdrawn PC12 cells, decreases cytosine arabinoside-induced apoptosis of cerebellar granule cells, and increases the number of tyrosine hydroxylase-positive (TH+) mesencephalic dopaminergic neurons in vitro.1 Oral administration of CGP 3466 (0.14 mg/kg) increases the number of TH+ dopaminergic neurons in a rat model of Parkinson's disease induced by MPTP. It also reduces delayed acquisition in the Morris maze in a 6-OHDA-treated rat model of Parkinson's disease and increases survival in progressive motor neuronopathy (pmn) mice, a genetic model of amyotrophic lateral sclerosis (ALS). Formulations containing CGP 3466 are under clinical investigation for the treatment of Parkinson’s disease and ALS.3,4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Waldemeier, P.C., Boulton, A.A., Cools, A.R., et al. Neurorescuing effects of the GAPDH ligand CGP 34668. J. Neural Transm. Suppl. 60, 197-214 (2000).

    2. Kragten, E., Lalande, I., Zimmermann, K., et al. Glyceraldehyde-3-phosphate dehydrogenase, the putative target of the antiapoptotic compounds CGP 3466 and R-(2)-deprenyl. The Journal of Biological Chemisty 273(10), 5821-5828 (1998).

    3. Miller, R., Bradley, W., Cudkowicz, M., et al. Phase II/III randomized trial of TCH346 in patients with ALS. Neurology 69(8), 776-784 (2007).

    4. Olanow, C.W., Schapira, A.H., LeWitt, P.A., et al. TCH346 as a neuroprotective drug in Parkinson’s disease: a double blind, randomised, controlled trial. Lancet. Neurol. 5(12), 1013-1020 (2006).