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CGP 3466B maleate (Synonyms: CGP 3466B)

Catalog No.GC13611

CGP 3466B maleate, an orally bioavailable GAPDH nitrosylation inhibitor, abrogates Aβ1-42-induced tau acetylation, memory impairment, and locomotor dysfunction in mice.

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CGP 3466B maleate Chemical Structure

Cas No.: 200189-97-5

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Sample solution is provided at 25 µL, 10mM.

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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

Cas No. 200189-97-5 SDF
Synonyms CGP 3466B
Chemical Name N-(dibenzo[b,f]oxepin-10-ylmethyl)-N-methylprop-2-yn-1-amine maleate
Canonical SMILES CN(CC#C)CC1=CC2=CC=CC=C2OC3=CC=CC=C13.OC(/C=C\C(O)=O)=O
Formula C19H17NO.C4H4O4 M.Wt 391.42
Solubility DMF: 20 mg/ml,DMSO: 20 mg/ml,Ethanol: 0.5 mg/ml,PBS (pH 7.2): 0.5 mg/ml Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 2.5548 mL 12.774 mL 25.548 mL
5 mM 0.511 mL 2.5548 mL 5.1096 mL
10 mM 0.2555 mL 1.2774 mL 2.5548 mL
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