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Merck
모든 사진(1)

문서

SML3278

Sigma-Aldrich

AC-262536

≥95% (HPLC)

동의어(들):

154BG31, 4-(3-endo-Hydroxy-8-azabicyclo[3.2.1]oct-8-yl)naphthalene-1-carbonitrile, 4-[(3-endo)-3-Hydroxy-8-azabicyclo[3.2.1]oct-8-yl]-1-naphthalenecarbonitrile, AC 262536, AC262536

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About This Item

실험식(Hill 표기법):
C18H18N2O
CAS Number:
Molecular Weight:
278.35
MDL number:
UNSPSC 코드:
12352200
NACRES:
NA.77

Quality Level

분석

≥95% (HPLC)

형태

powder

색상

white to beige

solubility

DMSO: 2 mg/mL, clear

저장 온도

−20°C

생화학적/생리학적 작용

AC-262536 is a non-steroidal, tissue-selective androgen receptor (AR) modulator (SARM) that targets AR with high-affinity (pKi = 8.3 vs. 8.9/testosterone), potency (NIH-3T3/MDA-kb2 reporter assay pEC50 = 7.9/8.8 vs. 8.7/8.5/testosterone) and partial agonist activity (Emax = 67% and 72% of testosterone Emax, respectively by NIH-3T3 or MDA-kb2 assay) and high selectivity (no significant affinity for 47 other human nuclear receptors). AC-262536 antagonizes 10 nM DHT-induced LNCaP proliferation (by 47.2% at 100 nM) and prevents castration-induced LH upregulation in rats in vivo (EC50 = 2.8 mg/kg) with greatly reduced adverse effects than testosterone propionate (TP).

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point (°F)

Not applicable

Flash Point (°C)

Not applicable


시험 성적서(COA)

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문서 라이브러리 방문

Charlotte Cutler et al.
Drug testing and analysis, 13(2), 369-385 (2020-09-23)
AC-262536 is one of a number of selective androgen receptor modulators that are being developed by the pharmaceutical industry for treatment of a range of clinical conditions including androgen replacement therapy. Though not available therapeutically, selective androgen receptor modulators are
Fabrice Piu et al.
The Journal of steroid biochemistry and molecular biology, 109(1-2), 129-137 (2008-01-01)
Because of the limitations and liabilities of current testosterone therapies, non-steroidal tissue-selective androgen receptor modulators may provide a clinically meaningful advance in therapy. Using a functional cell-based assay AC-262536 was identified as a potent and selective AR ligand, with partial
Tim Sobolevsky et al.
Drug testing and analysis, 13(2), 283-298 (2020-08-28)
In the recent years, a lot of effort was put into the development of multiclass initial testing procedures (ITP) to streamline analytical workflow in antidoping laboratories. Here, a high-throughput assay based on liquid chromatography-triple quadrupole mass spectrometry suitable for use

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