CGP 3466B maleate
(Synonyms: CGP3466B maleate) 目录号 : GC13611A GAPDH ligand
Cas No.:200189-97-5
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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.
Cas No. | 200189-97-5 | SDF | |
别名 | CGP3466B maleate | ||
化学名 | 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 | ||
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°C |
General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
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 |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方) | ||||||||||
% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
计算结果:
工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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