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CGP 3466B maleate

Catalog No.
B5354
GAPDH inhibitor
Grouped product items
SizePriceStock Qty
10mg
$209.00
Ship with 5-10 days
50mg
$833.00
Ship with 5-10 days

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Email: [email protected]

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Background

R-(2)-Deprenyl represents one of the drugs currently used for the treatment of Parkinson’s disease. The mechanism of action of neuroprotection as well as inhibition of apoptosis remains elusive. CGP 3466 is a structurally related R-(2)-deprenyl analoge that exhibits virtually no monoamine oxidase type B inhibiting activity but is neuroprotective.

In vitro: CGP 3466B is structurally related to both classical monoamine oxidase inhibitors and tricyclic antidepressent agents but lacks the pharmacological properties relevant to their anti-depressant effects. CGP 3466B has been shown to rescue human neuroblastoma and PC-12 cells from apoptotic death and also cerebellar granule cells in vitro from death induced by cytosine arabinoside [1].

In vivo: In pmn/pmn mice, CGP 3466B was administered orally at the onset of the clinical symptoms (2 weeks after birth). CGP 3466B slowed disease progression as determined by a 57% life-span increase, preservation of body weight and motor performance. The data support evaluation of CGP 3466B as a potential motor neuron disease treatment [2].

Clinical trial: Up to now, CGP 3466B is still in the preclinical development stage.

References:
[1] Kragten E, Lalande I, Zimmermann K, Roggo S, Schindler P, Muller D, van Oostrum J, Waldmeier P, Furst P.  Glyceraldehyde-3-phosphate dehydrogenase, the putative target of the antiapoptotic compounds CGP 3466 and R-(-)-deprenyl. J Biol Chem. 1998 Mar 6;273(10):5821-8.
[2] Sagot Y, Toni N, Perrelet D, Lurot S, King B, Rixner H, Mattenberger L, Waldmeier PC, Kato AC.  An orally active anti-apoptotic molecule (CGP 3466B) preserves mitochondria and enhances survival in an animal model of motoneuron disease. Br J Pharmacol. 2000 Oct;131(4):721-8.

Chemical Properties

Physical AppearanceWhite solid
StorageStore at -20°C
M.Wt391.42
Cas No.200189-97-5
FormulaC19H17NO·C4H4O4
SolubilitySoluble in DMSO
Chemical NameN-(dibenzo[b,f]oxepin-10-ylmethyl)-N-methylprop-2-yn-1-amine maleate
SDFDownload SDF
Canonical SMILESCN(CC#C)CC1=CC2=CC=CC=C2OC3=CC=CC=C13.OC(/C=C\C(O)=O)=O
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Quality Control

Quality Control & MSDS

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Chemical structure

CGP 3466B maleate