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SML2802

Sigma-Aldrich

ATR-101

≥98% (HPLC)

Synonyme(s) :

1[[1[4(Dimethylamino)phenyl]cyclopentyl]methyl]3[2,6di(propan2yl)phenyl]urea hydrochloride, ATR 101, ATR101, CI-984, N-[2,6-bis(1-Methylethyl)phenyl]-N-[[1-[4-(dimethylamino)phenyl]cyclopentyl]methyl]urea hydrochloride, Nevanimibe HCl, PD 132301 HCl, PD 132301-02, PD 132301-2, PD132301 HCl, PD132301-02, PD132301-2

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About This Item

Formule empirique (notation de Hill):
C27H39N3O·HCl
Numéro CAS:
133825-81-7
Poids moléculaire :
458.08
Numéro MDL:
MFCD00899568
Code UNSPSC :
12352200
Nomenclature NACRES :
NA.77

Niveau de qualité

100

Pureté

≥98% (HPLC)

Forme

powder

Conditions de stockage

desiccated

Couleur

white to beige

Solubilité

DMSO: 2 mg/mL, clear

Température de stockage

2-8°C

InChI

1S/C27H39N3O.ClH/c1-19(2)23-10-9-11-24(20(3)4)25(23)29-26(31)28-18-27(16-7-8-17-27)21-12-14-22(15-13-21)30(5)6;/h9-15,19-20H,7-8,16-18H2,1-6H3,(H2,28,29,31);1H

Clé InChI

SDOOGTHIDFZUNM-UHFFFAOYSA-N

Actions biochimiques/physiologiques

ATR-101 (PD 132301-02; Nevanimibe HCl) is an orally active, potent and selective acyl-CoA:cholesterol acyltransferase 1 (ACAT1, SOAT1) inhibtior (IC50 = 52 nM; intestinal microsome from cholesterol-fed rabbits) that reduces plasma cholesterol in both acute (by 77%; 50 mg/kg po.) and chronic (by 80%; 10 mg/kg po.) cholesterol-fed rat models. In addition, ATR-101 is reported to exhibit therapeutic efficacy against adrenocortical carcinoma (ACC), congenital adrenal hyperplasia (CAH), and Cushing′s syndrome (CS).

Code de la classe de stockage

11 - Combustible Solids

Classe de danger pour l'eau (WGK)

WGK 3

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Yunhui Cheng et al.
Endocrine-related cancer, 23(4), 1-19 (2016-02-05)
Adrenocortical carcinoma (ACC) generally has poor prognosis. Existing treatments provide limited benefit for most patients with locally advanced or metastatic tumors. We investigated the mechanisms for the cytotoxicity, xenograft suppression, and adrenalytic activity of ATR-101 (PD132301-02), a prospective agent for
M A Dominick et al.
Fundamental and applied toxicology : official journal of the Society of Toxicology, 20(2), 217-224 (1993-02-01)
PD 132301-2 is a substituted urea hypolipidemic and antiatherosclerotic agent that is a potent inhibitor of acyl-CoA:cholesterol acyltransferase (ACAT). To determine its subacute toxicity, PD 132301-2 was administered orally to beagle dogs at 0, 6, 12, 25, 50, 200, 400
J F Reindel et al.
Toxicologic pathology, 22(5), 510-518 (1994-09-01)
PD 132301-2, an acyl-CoA: cholesterol acyltransferase (ACAT) inhibitor, was administered orally to cynomolgus monkeys for 2 wk at doses of 25, 50, 100, and 200 mg/kg to assess potential subacute toxicity. Sporadic episodes of soft feces and diarrhea increased in
M A Dominick et al.
Toxicologic pathology, 21(1), 54-62 (1993-01-01)
PD 132301-2, a novel inhibitor of acyl-CoA:cholesterol acyltransferase, is adrenotoxic to several laboratory animal species. Morphogenesis of a zona fasciculata-specific cytotoxicity was evaluated in male Hartley guinea pigs administered 100 mg/kg of PD 132301-2 for up to 7 days. Reversibility
G H Wolfgang et al.
Life sciences, 56(13), 1089-1093 (1995-02-17)
To assess whether previously reported ultrastructural alterations of adrenocortical mitochondria induced by the acyl-CoA:cholesterol acyltransferase (ACAT) inhibitor PD 132301-2 are accompanied by functional deficits in tissue energy stores, phosphorylated adenine nucleotide levels in guinea pig adrenal cortex were quantitated. Adrenals
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