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AM281

Name: AM281
Brand: TargetMol
SKU: T2264
Price: 692 CNY
Availability: InStock
Rating: 5 (10 reviews)

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很棒

纯度: 98.6%

货号 T2264Cas号 202463-68-1

别名 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

AM281 是选择性CB1受体拮抗剂，IC50=9.91 nM。它抑制 CB2 受体，IC50=13000 nM。

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AM281

一键复制产品信息

很棒

纯度: 98.6%

货号 T2264 别名 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Cas号 202463-68-1

AM281 是选择性CB1受体拮抗剂，IC50=9.91 nM。它抑制 CB2 受体，IC50=13000 nM。

规格	价格	库存
1 mg	¥ 692	现货
2 mg	¥ 987	现货
5 mg	¥ 1,820	现货
10 mg	¥ 2,880	现货
25 mg	¥ 4,760	现货
50 mg	¥ 6,630	现货
100 mg	¥ 8,930	现货
500 mg	¥ 17,900	现货
1 mL x 10 mM (in DMSO)	¥ 2,320	现货

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TargetMol的所有产品仅用作科学研究或药证申报，不能被用于人体，我们不向个人提供产品和服务。请您遵守承诺用途，不得违反法律法规规定用于任何其他用途。

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纯度: >99.99%

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COA 产品操作手册

产品介绍

AM281 AI Summary

AM281 exhibits high affinity for the cannabinoid CB1 receptor, acting as both an inverse agonist and antagonist, with a Ki value ranging from 4.5 nM to 422.0 nM depending on the assay system used. It demonstrates significantly lower affinity for the CB2 receptor, with a Ki value of 4200.0 nM. In various cellular assays, AM281 shows broad bioactivity, including inhibition of Menin-MLL interaction, Jumonji Domain 2E, Tyrosyl-DNA Phosphodiesterase (TDP1), several cytochrome P450 enzymes (2C19, 2D6, 2C9), Tau fibril formation, 15-human lipoxygenase, Anthrax lethal toxin internalization, lipid storage modulation, Regulator of G Protein Signaling 4, and USP1/UAF1. It also exhibits antagonist activity at the CB1 receptor with negative intrinsic activity levels of -80.0% and -42.0% in human recombinant and rat brain cortical membranes, respectively, and agonist activity at the human GPR55 receptor (EC50 = 13600.0 nM). Additionally, AM281 has antiviral properties, inhibiting SARS-CoV-2 induced cytotoxicity in Caco-2 and VERO-6 cells at 10 µM concentration. It possesses mild inhibition of the SARS-CoV-2 3CL-Pro protease (21.46% at 20 µM) and exhibits minimal inhibition of the human HDAC6 enzyme. The compound also has a distribution coefficient with a CLogD value of 3.71. Overall, AM281 displays a diverse range of bioactivities, including enzyme inhibition, receptor modulation, and antiviral effects..

Note: Summary generated by AI. Data source: ChEMBL

生物活性

产品描述	AM 281, a cannabinoid antagonist, reduces neurologic dysfunction and mortality rate after cecal ligation and puncture in rats.
靶点活性	CB1:9.91 nM (IC50), CB2:13000 nM (IC50)
别名	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

化学信息

分子量	557.21
分子式	C₂₁H₁₉Cl₂IN₄O₂
CAS No.	202463-68-1
Smiles	CC1=C(N(N=C1C(NN2CCOCC2)=O)C3=C(Cl)C=C(Cl)C=C3)C4=CC=C(I)C=C4
密度	1.7g/cm3

储存&溶解度

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

溶解度信息

DMSO: 12 mg/mL (21.54 mM), Sonication is recommended.

体内实验配方

10% DMSO+90% Corn Oil: 0.5 mg/mL (0.9 mM), Sonication is recommeded.

请按顺序添加溶剂，在添加下一种溶剂之前，尽可能使溶液澄清。如有必要，可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考，体内配方并不是绝对的，请根据不同情况进行调整。

溶液配制表

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.7947 mL	8.9733 mL	17.9466 mL	89.7328 mL
5 mM	0.3589 mL	1.7947 mL	3.5893 mL	17.9466 mL
10 mM	0.1795 mL	0.8973 mL	1.7947 mL	8.9733 mL
20 mM	0.0897 mL	0.4487 mL	0.8973 mL	4.4866 mL