AM281 - CAS:202463-68-1

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AM281 (Synonyms:AM281 抑制剂)

目录号 : KCM12398 CAS No. : 202463-68-1 纯度 : ≥98%

Data Sheet SDS 产品使用指南

AM281 is a potent and selective central cannabinoid (CB) receptor antagonist/inverse agonist (Ks = 12 nM and 4,200 nM for CB and CB, respectively). Structurally, it is an analog of the CB inverse agonist rimonabant . It has no effect on the vanilloid TRPV1 receptor. AM281 has been used to evaluate the potential effects of compounds at CB It has also been used to study the membrane localization and cycling of CB

规格	价格	是否有货	数量
1mg		In-stock
5mg		In-stock
10mg		In-stock

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Other Forms of Rapamycin:

CB2R/FAAH modulator-3 In-stock
AM-2232 In-stock
Virodhamine In-stock
(±)-Cannabichromene In-stock
AM1241 In-stock

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生物活性

AM281 is a selective CB1 receptor antagonist with an IC₅₀ of 9.91 nM. AM281 inhibits CB2 receptor with an IC₅₀ of 13000 nM.

体外研究

In the presence of 10 μM KSO 1-6, AM281 (0.01-10 μM) concentration-dependently enhanced the neurotoxicity induced by 10 μM Aβ 25-35 in SH-SY5Y cells.

体内研究

Acute administration of AM281 (2.5, 5, and 10 mg/kg) shortened exploration time and improved memory performance, as did chronic administration of AM281 (0.62, 1.25, and 2.5 mg/kg).
Long term use of 2.5 mg/kg AM281 can increase the recognition index to 22.1, single dose use of 5 mg/kg AM281 can increase memory impairment to 8.5, while carrier treatment can increase it to 4.8. Administration of AM281 at a chronic dose of 2.5 mg/kg and an acute dose of 5 mg/kg can improve memory.

Animal Model:	Male NMRI mice with the weight of 25-30 g
Dosage:	0.62, 1.25 and 2.5 mg/kg (chronic administration); 2.5, 5 and 10 mg/kg (acute administration)
Administration:	Administrated i.p. every day concurrently with morphine except the day of experiment (chronic administration); Singly injected 40 min before second trial (acute administration)
Result:	The simultaneous daily administration of AM281 with morphine significantly shortened the exploration time, as compared with morphine-dependent mice receiving vehicle. Acute administration at a dose of 5 mg/kg, significantly augmented recognition index.

分子式

C₂₁H₁₉Cl₂In₄O₂

分子量

557.21

CAS号

202463-68-1

中文名称

1-(2,4-二氯苯)-5-(4-碘苯基)-4-甲基-N-4-吗啉基-1H-吡唑-3-甲酰胺;1-(2,4-二氯苯基)-5-(4-碘苯基)-4-甲基-N-4-吗啉基-1H-吡唑-3-甲酰胺;1-(2,4-二氯苯基)-5-(4-碘苯基)-4-甲基-N-4-吗啉基-1H-吡唑-3-羧胺;1-(2,4-二氯苯基)-5-(4-碘苯基)-4-甲基-N-吗啉-1H-吡唑-3-甲酰胺;4-戊基溴锌;

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 7.14 mg/mL (12.81 mM; ultrasonic and warming and heat to 60°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.7947 mL	8.9733 mL	17.946 mL
5 mM	0.3589 mL	1.7947 mL	3.5893 mL
10 mM	0.1795 mL	0.8973 mL	1.7947 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO → 90% corn oil

Solubility: ≥ 0.71 mg/mL (1.27 mM); Clear solution

此方案可获得 ≥ 0.71 mg/mL (1.27 mM，饱和度未知) 的澄清溶液，此⽅案不适⽤于实验周期在半个⽉以上的实验。

以 1 mL 工作液为例，取 100 μL 7.1 mg/mL 的澄清 DMSO 储备液加到 900 μL ⽟⽶油中，混合均匀。