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CGP 3466B maleate

GAPDH inhibitor CAS# 200189-97-5

CGP 3466B maleate

Catalog No. BCC5955----Order now to get a substantial discount!

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CGP 3466B maleate: 5mg $81 In Stock
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Quality Control of CGP 3466B maleate

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Chemical structure

CGP 3466B maleate

3D structure

Chemical Properties of CGP 3466B maleate

Cas No. 200189-97-5 SDF Download SDF
PubChem ID 9821821 Appearance Powder
Formula C23H21NO5 M.Wt 391.42
Type of Compound N/A Storage Desiccate at -20°C
Synonyms TCH 346 maleate
Solubility Soluble to 10 mM in water and to 100 mM in DMSO
Chemical Name N-(benzo[b][1]benzoxepin-5-ylmethyl)-N-methylprop-2-yn-1-amine;(Z)-but-2-enedioic acid
SMILES CN(CC#C)CC1=CC2=CC=CC=C2OC3=CC=CC=C31.C(=CC(=O)O)C(=O)O
Standard InChIKey SQAZQLMBEHYFJA-BTJKTKAUSA-N
Standard InChI 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-
General tips For 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.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of CGP 3466B maleate

DescriptionOrally active glyceraldehyde-3-phosphate dehydrogenase (GAPDH) inhibitor. Exhibits antiapoptotic activity via inhibition of GAPDH nuclear translocation and mitochondrial complex 1-dependent H2O2 release. Displays neuroprotective activity in vivo.

CGP 3466B maleate Dilution Calculator

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CGP 3466B maleate Molarity Calculator

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Preparing Stock Solutions of CGP 3466B maleate

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.5548 mL 12.774 mL 25.548 mL 51.096 mL 63.87 mL
5 mM 0.511 mL 2.5548 mL 5.1096 mL 10.2192 mL 12.774 mL
10 mM 0.2555 mL 1.2774 mL 2.5548 mL 5.1096 mL 6.387 mL
50 mM 0.0511 mL 0.2555 mL 0.511 mL 1.0219 mL 1.2774 mL
100 mM 0.0255 mL 0.1277 mL 0.2555 mL 0.511 mL 0.6387 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on CGP 3466B maleate

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.

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References on CGP 3466B maleate

Host Proteins Identified in Extracellular Viral Particles as Targets for Broad-Spectrum Antiviral Inhibitors.[Pubmed:30351952]

J Proteome Res. 2018 Nov 5.

Liquid chromatography mass spectrometry (LCMS) proteomic analyses have revealed that host proteins are often captured in extracellular virions. These proteins may play a role in viral replication or infectivity and can represent targets for broad-spectrum antiviral agent development. We utilized LCMS to determine the host protein composition of Lassa virus-like particles (LASV VLPs). Multiple host proteins incorporated in LASV VLPs are also incorporated in unrelated viruses, notably ribosomal proteins. We assembled a data set of host proteins incorporated into extracellular viral particles. The frequent incorporation of specific host proteins into viruses of diverse families suggests that interactions of these proteins with viral factors may be important for effective viral replication. Drugs that target virion-associated host proteins could affect the protein in the extracellular virion or the host cell. Compounds that target proteins incorporated into virions with high frequency, but with no known antiviral activity, were assayed in a scalable viral screening platform, and hits were tested in competent viral systems. One of these molecules, GAPDH modulating small molecule CGP 3466B maleate (Omigapil), exhibited a dose-dependent inhibition of HIV, dengue virus, and Zika virus.

Clorgyline and other propargylamine derivatives as inhibitors of succinate-dependent H(2)O(2) release at NADH:UBIQUINONE oxidoreductase (Complex I) in brain mitochondria.[Pubmed:18763029]

J Bioenerg Biomembr. 2008 Aug;40(4):289-96.

Complex I is the main O(2)(-) producer of the mitochondrial respiratory chain. O(2)(-) release is low with NAD-linked substrates and increases strongly during succinate oxidation, which increases the QH(2)/Q ratio and is rotenone sensitive. We show that the succinate dependent O(2)(-) production (measured as H(2)O(2) release) is inhibited by propargylamine containing compounds (clorgyline, CGP 3466B, rasagiline and TVP-1012). The inhibition does not affect membrane potential and is unaffected by DeltapH modifications. Mitochondrial respiration is similarly unaffected. The propargylamines inhibition of O(2)(-)/H(2)O(2) production is monitored also in the presence of the Parkinson's disease toxin dopaminochrome which stimulates O(2)(-) release. Propargylamine-containing compounds are the first pharmacological inhibitors described for O(2)(-) release at Complex I.

TCH346 prevents motor symptoms and loss of striatal FDOPA uptake in bilaterally MPTP-treated primates.[Pubmed:14572443]

Neurobiol Dis. 2003 Nov;14(2):205-17.

The neuroprotective efficacy of the propargylamine TCH346 was studied in the primate model of Parkinson's disease, the bilaterally MPTP-treated monkey. Male rhesus monkeys received 2.5 mg MPTP into the left carotid artery and, 8 weeks later, 1.25 mg MPTP into the right carotid artery. Starting 2 h after the second MPTP infusion, either 0.014 mg/kg TCH346 or its solvent was subcutaneously injected twice per day for 14 days. The first MPTP treatment induced mild Parkinson symptoms, reduced right limb movements, and reduced FDOPA uptake in the left striatum. The second MPTP treatment made Parkinson symptoms worse, reduced left limb movements, and reduced FDOPA uptake in the right striatum of solvent-treated monkeys. In contrast, the second MPTP treatment did not further worsen motor symptoms and did not decrease FDOPA uptake in the right striatum of TCH346-treated monkeys. Although the effects of the second MPTP treatment were largely prevented, the effects of the first MPTP treatment were not reversed by TCH346. Immunohistochemical examination confirmed the dramatic loss of dopamine cells in vehicle-treated monkeys and the preservation of these neurons in the right brain side of the TCH346-treated animals. In conclusion, systemic administration of TCH346 prevented motor symptoms and nigrostriatal degeneration induced by MPTP in primates.

An orally active anti-apoptotic molecule (CGP 3466B) preserves mitochondria and enhances survival in an animal model of motoneuron disease.[Pubmed:11030721]

Br J Pharmacol. 2000 Oct;131(4):721-8.

Apoptosis and mitochondrial dysfunction are thought to be involved in the aetiology of neurodegenerative diseases. We have tested an orally active anti-apoptotic molecule (CGP 3466B) that binds to glyceraldehyde-3-phosphate dehydrogenase (GAPDH) in an animal model with motoneuron degeneration, i.e. a mouse mutant with progressive motor neuronopathy (pmn). In pmn/pmn mice, CGP 3466B was administered orally (10 - 100 nmol kg(-1)) at the onset of the clinical symptoms (2 weeks after birth). CGP 3466B slowed disease progression as determined by a 57% increase in life-span, preservation of body weight and motor performance. This improvement was accompanied by a decreased loss of motoneurons and motoneuron fibres as well as an increase in retrograde transport. Electron microscopic analysis showed that CGP 3466B protects mitochondria which appear to be selectively disrupted in the motoneurons of pmn/pmn mice. The data support evaluation of CGP 3466B as a potential treatment for motor neuron disease.

Description

GAPDH inhibitor. Neuroprotective

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