貨號	規格	價格	上海	北京	武漢	南京
S81514-1mg	99.6%	￥204.00 S81514-1mg ￥204.00 現貨	9 9	-	-	-
S81514-5mg	99.6%	￥490.00 S81514-5mg ￥490.00 現貨	6 6	-	-	-
S81514-10mg	99.6%	￥890.00 S81514-10mg ￥890.00 現貨	6 6	-	-	-
S81514-25mg	99.6%	￥1910.00 S81514-25mg ￥1910.00 現貨	7 7	-	-	-
S81514-50mg	99.6%	￥3700.00 S81514-50mg ￥3700.00 現貨	5 5	-	-	-

產品介紹

AMG 517 is a potent and selective vanilloid receptor-1 (TRPV1) antagonist with an IC50 of 0.5 nM.

產品描述：

AMG 517 is a potent and selective vanilloid receptor-1 (TRPV1) antagonist with an IC50 of 0.5 nM.

靶點：

IC50: 0.5 nM (TRPV1);TRP/TRPVChannel

體內研究：

AMG 517 is shown to be effective in a rodent “on-target” biochemical challenge model (capsaicin-induced flinch, ED50=0.33 mg/kg p.o.) and is antihyperalgesic in a model of inflammatory pain (CFA-induced thermal hyperalgesia, MED=0.83 mg/kg, p.o.).The minimally effective dose is 0.3 mg/kg for AMG 517 and the corresponding plasma concentration is 90 ng/mL. Oral administration of AMG 517 reverses established thermal hyperalgesia in a dose-dependent manner at 21 h after CFA injection. AMG 517 causes transient hyperthermia in rodents, dogs, and monkeys. AMG 517 induces hyperthermia in a steep dose-dependent manner, with 0.3, 1, and 3 mg/kg associated with 0.5, 0.6, and 1.6°C increases in body temperature, respectively. Body temperatures of rats treated with all doses of AMG 517 return to baseline within 10 to 20 h.

參考文獻：

1. Doherty EM, et al. Novel vanilloid receptor-1 antagonists: 2. Structure-activity relationships of 4-oxopyrimidines leading to the selection of a clinical candidate. J Med Chem. 2007 Jul 26;50(15):3515-27. 2. Gavva NR, et al. Repeated administration of vanilloid receptor TRPV1 antagonists attenuates hyperthermia elicited by TRPV1 blockade. J Pharmacol Exp Ther. 2007 Oct;323(1):128-37.

溶解性：

DMSO : 41.67 mg/mL (96.82 mM; Need ultrasonic)

保存條件：

-20℃

配置溶液濃度參考：

	1mg	5mg	10mg
1 mM	2.323 ml	11.617 ml	23.234 ml
5 mM	0.465 ml	2.323 ml	4.647 ml
10 mM	0.232 ml	1.162 ml	2.323 ml
50 mM	0.046 ml	0.232 ml	0.465 ml

注意：

部分產品我司僅能提供部分信息，我司不保證所提供信息的權威性，僅供客戶參考交流研究之用。

參考文獻

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Amg 517