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SML2717

Sigma-Aldrich

AMG517

≥98% (HPLC)

别名:

AMG 517, AMG-517, N-(4-(6-(4-(Trifluoromethyl)phenyl)pyrimidin-4-yloxy)benzo[d]thiazol-2-yl)acetamide, N-[4-[[6-[4-(Trifluoromethyl)phenyl]-4-pyrimidinyl]oxy]-2-benzothiazolyl]acetamide

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About This Item

经验公式（希尔记法）:
C20H13F3N4O2S
CAS号:
659730-32-2
分子量:
430.40
MDL號碼:
MFCD14584859
分類程式碼代碼:
12352200
NACRES:
NA.77

品質等級

100

化驗

≥98% (HPLC)

形狀

powder

顏色

white to beige

溶解度

DMSO: 2 mg/mL, clear

儲存溫度

2-8°C

InChI

1S/C20H13F3N4O2S/c1-11(28)26-19-27-18-15(3-2-4-16(18)30-19)29-17-9-14(24-10-25-17)12-5-7-13(8-6-12)20(21,22)23/h2-10H,1H3,(H,26,27,28)

InChI 密鑰

YUTIXVXZQIQWGY-UHFFFAOYSA-N

生化／生理作用

AMG517 is an orally active, highly potent and selective vanilloid receptor-1 (TRPV1; VR1; capsaicin receptor) antagonist that blocks TRPV1-mediated cellular Ca2+ influx (h/r/m IC50/stimulant = 0.76 nM/1.01 nM/1.9 nM/500 nM capsaicin; 0.62 nM/0.5 nM/0.63 nM/acid (pH 5) using respective CHO transfectants; IC50 >20 μM against TRPV2/3/4, TRPA1, and TRPM8-mediated responses; <45% binding at 10 μM to 87 receptors, enzymes, and ion channels) and exhibits antihyperalgesic efficacy in vivo (capsaicin-induced flinch = ED50 = 0.33 mg/kg rats, p.o.; CFA-induced thermal hyperalgesia, MED = 0.83 mg/kg rats, p.o.).

儲存類別代碼

11 - Combustible Solids

水污染物質分類（WGK）

WGK 3

閃點（°F）

Not applicable

閃點（°C）

Not applicable

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Elizabeth M Doherty et al.
Journal of medicinal chemistry, 50(15), 3515-3527 (2007-06-26)
A series of novel 4-oxopyrimidine TRPV1 antagonists was evaluated in assays measuring the blockade of capsaicin or acid-induced influx of calcium into CHO cells expressing TRPV1. The investigation of the structure-activity relationships in the heterocyclic A-region revealed the optimum pharmacophoric
Narender R Gavva et al.
The Journal of pharmacology and experimental therapeutics, 323(1), 128-137 (2007-07-27)
Capsaicin, the active ingredient in some pain-relieving creams, is an agonist of a nonselective cation channel known as the transient receptor potential vanilloid type 1 (TRPV1). The pain-relieving mechanism of capsaicin includes desensitization of the channel, suggesting that TRPV1 antagonism

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