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Merck

SML0667

PF-429242 dihydrochloride

≥98% (HPLC), S1P inhibitor, powder

Synonyme(s) :

4-[(Diethylamino)methyl]-N-[2-(2-methoxyphenyl)ethyl]-N-(3R)-3-pyrrolidinyl-benzamide dihydrochloride, PF 429242 dihydrochloride

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A propos de cet article

Formule empirique (notation de Hill) :
C25H35N3O2 · 2HCl
Numéro CAS:
Poids moléculaire :
482.49
UNSPSC Code:
12352200
NACRES:
NA.77
Assay:
≥98% (HPLC)
Form:
powder
Quality level:
Storage condition:
desiccated
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Nom du produit

PF-429242 dihydrochloride, ≥98% (HPLC)

SMILES string

N1C[C@@H](CC1)N(CCc3c(cccc3)OC)C(=O)c2ccc(cc2)CN(CC)CC

InChI

1S/C25H35N3O2/c1-4-27(5-2)19-20-10-12-22(13-11-20)25(29)28(23-14-16-26-18-23)17-15-21-8-6-7-9-24(21)30-3/h6-13,23,26H,4-5,14-19H2,1-3H3/t23-/m1/s1

InChI key

XKPJTOHUPQWSOJ-HSZRJFAPSA-N

assay

≥98% (HPLC)

form

powder

storage condition

desiccated

color

white to beige

solubility

H2O: 15 mg/mL, clear

storage temp.

2-8°C

Quality Level

Application

PF-429242 dihydrochloride has been used as an inhibitor of sterol regulatory element-binding protein (SREBP).

Biochem/physiol Actions

PF-429242 is a potent inhibitor of S1P (cellular proprotein convertase sterol regulatory element-binding protein (SREBP) site 1 protease) that reduces expression levels of hepatic SREBP target genes and lower rates of cholesterol and fatty acid synthesis in mice. PF-429242 is a potent antiviral agent against prototypic arenavirus lymphocytic choriomeningitis virus (LCMV) and LASV in cultured cells. PF-429242 efficiently prevented the processing of GPC from the LCMV and LASV. PF-429242 is expected to be active against CCHFV.
PF-429242 is a potent inhibitor of S1P (cellular proprotein convertase sterol regulatory element-binding protein (SREBP) site 1 protease).

pictograms

Exclamation markEnvironment

signalword

Warning

Hazard Classifications

Aquatic Acute 1 - Aquatic Chronic 1 - Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3

target_organs

Respiratory system

Classe de stockage

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable


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Consulter la Bibliothèque de documents

Siqingaowa et al.
Biochemical and biophysical research communications, 488(1), 136-140 (2017-05-10)
Sterol regulatory element-binding protein1 (SREBP1) is a key regulatory factor that controls lipid homeostasis. Overactivation of SREBP1 and elevated lipid biogenesis are considered the major characteristics in malignancies of prostate cancer, endometrial cancer, and glioblastoma. However, the impact of SREBP1
Fatostatin inhibits cancer cell proliferation by affecting mitotic microtubule spindle assembly and cell division.
Gholkar A A, et al.
The Journal of Biological Chemistry, 291(33), 17001-17008 (2016)
Ruofan Wang et al.
Cell, 184(1), 106-119 (2020-12-18)
The Coronaviridae are a family of viruses that cause disease in humans ranging from mild respiratory infection to potentially lethal acute respiratory distress syndrome. Finding host factors common to multiple coronaviruses could facilitate the development of therapies to combat current
Tian Du et al.
Breast cancer research : BCR, 20(1), 106-106 (2018-09-06)
Invasive lobular breast carcinoma (ILC) is a histological subtype of breast cancer that is characterized by loss of E-cadherin and high expression of estrogen receptor alpha (ERα). In many cases, ILC is effectively treated with adjuvant aromatase inhibitors (AIs); however
Jessica D Rosarda et al.
ACS chemical biology, 16(12), 2852-2863 (2021-11-20)
The extracellular accumulation of glutamate is a pathologic hallmark of numerous neurodegenerative diseases including ischemic stroke and Alzheimer's disease. At high extracellular concentrations, glutamate causes neuronal damage by promoting oxidative stress, which can lead to cellular death. This has led

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