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CGP 3466B maleate
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
CGP 3466B maleate图片
CAS NO:200189-97-5
包装与价格:
包装价格(元)
1mg电议
5mg电议

产品介绍
CGP 3466B 马来酸盐是一种口服生物可利用的 GAPDH 亚硝基化抑制剂,可消除 Aβ1-42 诱导的小鼠 tau 乙酰化、记忆障碍和运动功能障碍。
Cas No.200189-97-5
别名CGP3466B maleate
化学名N-(dibenzo[b,f]oxepin-10-ylmethyl)-N-methylprop-2-yn-1-amine maleate
Canonical SMILESCN(CC#C)CC1=CC2=CC=CC=C2OC3=CC=CC=C13.OC(/C=C\C(O)=O)=O
分子式C19H17NO.C4H4O4
分子量391.42
溶解度DMF: 20 mg/ml,DMSO: 20 mg/ml,Ethanol: 0.5 mg/ml,PBS (pH 7.2): 0.5 mg/ml
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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.