Home >> Research Area >>Proteases/Proteasome>>Gamma Secretase>> gamma-secretase modulator 1

gamma-secretase modulator 1

Useful for Alzheimer's disease. CAS# 1172637-87-4

gamma-secretase modulator 1

Catalog No. BCC1583----Order now to get a substantial discount!

Product Name & Size Price Stock
gamma-secretase modulator 1:10mg $345.00 In stock
gamma-secretase modulator 1:20mg $587.00 In stock
gamma-secretase modulator 1:50mg $1380.00 In stock
gamma-secretase modulator 1:100mg $2415.00 In stock
Related Products

Quality Control of gamma-secretase modulator 1

Number of papers citing our products

Chemical structure

gamma-secretase modulator 1

3D structure

Chemical Properties of gamma-secretase modulator 1

Cas No. 1172637-87-4 SDF Download SDF
PubChem ID 42647277 Appearance Powder
Formula C24H24N4OS M.Wt 416.54
Type of Compound N/A Storage Desiccate at -20°C
Solubility DMSO : < 1 mg/mL (insoluble or slightly soluble)
Chemical Name N-[3-methoxy-4-(4-methylimidazol-1-yl)phenyl]-4-phenyl-4,5,6,7-tetrahydro-1,3-benzothiazol-2-amine
SMILES CC1=CN(C=N1)C2=C(C=C(C=C2)NC3=NC4=C(S3)CCCC4C5=CC=CC=C5)OC
Standard InChIKey VFSGAZRYSCNFDF-UHFFFAOYSA-N
Standard InChI InChI=1S/C24H24N4OS/c1-16-14-28(15-25-16)20-12-11-18(13-21(20)29-2)26-24-27-23-19(9-6-10-22(23)30-24)17-7-4-3-5-8-17/h3-5,7-8,11-15,19H,6,9-10H2,1-2H3,(H,26,27)
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 gamma-secretase modulator 1

Descriptionγ-secretase inhibitior-1 is a gamma-secretase modulator, γ-secretase inhibitior-1 is useful for Alzheimer's disease.

References:
[1]. Baumann, Karlheinz; Flohr, Alexander; Preparation of 4,5,6,7-tetrahydrobenzothiazolyl- or 5,6,7,8-tetrahydroquinazolinylphenylamine derivatives as modulators for amyloid beta. PCT Int. Appl. (2009), 111pp. CODEN: PIXXD2 WO 2009087127 A1

gamma-secretase modulator 1 Dilution Calculator

Concentration (start)
x
Volume (start)
=
Concentration (final)
x
Volume (final)
 
 
 
C1
V1
C2
V2

calculate

gamma-secretase modulator 1 Molarity Calculator

Mass
=
Concentration
x
Volume
x
MW*
 
 
 
g/mol

calculate

Preparing Stock Solutions of gamma-secretase modulator 1

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.4007 mL 12.0036 mL 24.0073 mL 48.0146 mL 60.0182 mL
5 mM 0.4801 mL 2.4007 mL 4.8015 mL 9.6029 mL 12.0036 mL
10 mM 0.2401 mL 1.2004 mL 2.4007 mL 4.8015 mL 6.0018 mL
50 mM 0.048 mL 0.2401 mL 0.4801 mL 0.9603 mL 1.2004 mL
100 mM 0.024 mL 0.12 mL 0.2401 mL 0.4801 mL 0.6002 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.

Organizitions Citing Our Products recently

 
 
 

Calcutta University

University of Minnesota

University of Maryland School of Medicine

University of Illinois at Chicago

The Ohio State University

University of Zurich

Harvard University

Colorado State University

Auburn University

Yale University

Worcester Polytechnic Institute

Washington State University

Stanford University

University of Leipzig

Universidade da Beira Interior

The Institute of Cancer Research

Heidelberg University

University of Amsterdam

University of Auckland
TsingHua University
TsingHua University
The University of Michigan
The University of Michigan
Miami University
Miami University
DRURY University
DRURY University
Jilin University
Jilin University
Fudan University
Fudan University
Wuhan University
Wuhan University
Sun Yat-sen University
Sun Yat-sen University
Universite de Paris
Universite de Paris
Deemed University
Deemed University
Auckland University
Auckland University
The University of Tokyo
The University of Tokyo
Korea University
Korea University

Background on gamma-secretase modulator 1

γ-secretase inhibitior-1 is useful for Alzheimer's disease.

Featured Products
New Products
 

References on gamma-secretase modulator 1

Effect of potent gamma-secretase modulator in human neurons derived from multiple presenilin 1-induced pluripotent stem cell mutant carriers.[Pubmed:25285942]

JAMA Neurol. 2014 Dec;71(12):1481-9.

IMPORTANCE: Although considerable effort has been expended developing drug candidates for Alzheimer disease, none have yet succeeded owing to the lack of efficacy or to safety concerns. One potential shortcoming of current approaches to Alzheimer disease drug discovery and development is that they rely primarily on transformed cell lines and animal models that substantially overexpress wild-type or mutant proteins. It is possible that drug development failures thus far are caused in part by the limits of these approaches, which do not accurately reveal how drug candidates will behave in naive human neuronal cells. OBJECTIVE: To analyze purified neurons derived from human induced pluripotent stem cells from patients carrying 3 different presenilin 1 (PS1) mutations and nondemented control individuals in the absence of any overexpression. We tested the efficacy of gamma-secretase inhibitor and gamma-secretase modulator (GSM) in neurons derived from both normal control and 3 PS1 mutations (A246E, H163R, and M146L). DESIGN, SETTING, AND PARTICIPANTS: Adult human skin biopsies were obtained from volunteers at the Alzheimer Disease Research Center, University of California, San Diego. Cell cultures were treated with gamma-secretase inhibitor or GSM. Comparisons of total beta-amyloid (Abeta) and Abeta peptides 38, 40, and 42 in the media were made between vehicle- vs drug-treated cultures. MAIN OUTCOMES AND MEASURES: Soluble Abeta levels in the media were measured by enzyme-linked immunosorbent assay. RESULTS: As predicted, mutant PS1 neurons exhibited an elevated Abeta42:Abeta40 ratio (P < .05) at the basal state as compared with the nondemented control neurons. Treatment with a potent non-nonsteroidal anti-inflammatory druglike GSM revealed a new biomarker signature that differs from all previous cell types and animals tested. This new signature was the same in both the mutant and control neurons and consisted of a reduction in Abeta42, Abeta40, and Abeta38 and in the Abeta42:Abeta40 ratio, with no change in the total Abeta levels. CONCLUSIONS AND RELEVANCE: This biomarker discrepancy is likely due to overexpression of amyloid precursor protein in the transformed cellular models. Our results suggest that biomarker signatures obtained with such models are misleading and that human neurons derived from human induced pluripotent stem cells provide a unique signature that will more accurately reflect drug response in human patients and in cerebrospinal fluid biomarker changes observed during GSM treatment.

1-(3',4'-Dichloro-2-fluoro[1,1'-biphenyl]-4-yl)-cyclopropanecarboxylic acid (CHF5074), a novel gamma-secretase modulator, reduces brain beta-amyloid pathology in a transgenic mouse model of Alzheimer's disease without causing peripheral toxicity.[Pubmed:17895400]

J Pharmacol Exp Ther. 2007 Dec;323(3):822-30.

Some nonsteroidal anti-inflammatory drugs has been shown to allosterically modulate the activity of gamma-secretase, the enzymatic complex responsible for the formation of beta-amyloid (Abeta). 1-(3',4'-Dichloro-2-fluoro[1,1'-biphenyl]-4-yl)-cyclopropanecarboxylic acid (CHF5074) is a new gamma-secretase modulator, devoid of anticyclooxygenase (COX) and Notch-interfering activities in vitro. We evaluated the effects of chronic CHF5074 treatment on brain Abeta pathology in Tg2576 transgenic mice. Twenty-eight animals of 9.5 to 10.5 months of age received CHF5074-medicated diet (375 ppm) or standard diet for 17 weeks. Compared with controls, CHF5074 treatment significantly reduced the area occupied by plaques and the number of plaques in cortex (-52.2 +/- 5.6%, p = 0.0003 and -48.9 +/- 6.6%, p = 0.0004, respectively) and hippocampus (-76.7 +/- 6.4%, p = 0.004 and -66.2 +/- 10.3%, p = 0.037, respectively). Biochemical analysis confirmed the histopathological measures, with CHF5074-treated animals showing reduced total brain Abeta40 (-49.2 +/- 9.2%, p = 0.017) and Abeta42 (-43.5 +/- 9.7%, p = 0.027) levels. In a human neuroglioma cell line expressing Swedish mutated form of amyloid precursor protein (H4swe), CHF5074 reduced Abeta42 and Abeta40 secretion, with an IC50 of 3.6 and 18.4 microM, respectively, values consistent with those measured in the brain of the CHF5074-treated Tg2576 mice (6.4 +/- 0.4 microM). At 5 microM, no effects were observed on Notch intracellular cleavage in human embryonic kidney 293swe cells. CHF5074 was well tolerated by Tg2576 mice. No abnormal findings were observed upon histopathological examination of the gastrointestinal tract, indicating the absence of COX-related toxicity. Semiquantitative histochemical evaluation of goblet cells in the ileum of vehicle- and CHF5074-treated animals yielded similar results, suggesting no effects on Notch pathway. CHF5074 is therefore a promising therapeutic agent for Alzheimer's disease.

Description

γ-secretase inhibitior-1 is a gamma-secretase modulator, γ-secretase inhibitior-1 is useful for Alzheimer's disease.

Keywords:

gamma-secretase modulator 1,1172637-87-4,Natural Products,Gamma Secretase, buy gamma-secretase modulator 1 , gamma-secretase modulator 1 supplier , purchase gamma-secretase modulator 1 , gamma-secretase modulator 1 cost , gamma-secretase modulator 1 manufacturer , order gamma-secretase modulator 1 , high purity gamma-secretase modulator 1

Online Inquiry for:

      Fill out the information below

      • Size:Qty: - +

      * Required Fields

                                      Result: