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首页-小分子抑制剂&激动剂-GPCR-Opioid Receptor-Naltrexone
Naltrexone

Chemical Structure : Naltrexone

CAS No.: 16590-41-3

Naltrexone

货号: PC-45979Not For Human Use, Lab Use Only.

Naltrexone is a potent, competitive antagonist for μ, κ, δ, and σ-opioid receptors with Ki of 0.0825 nM, 0.509 nM, and 8.02 nM, for MOR, KOR, and DOR, respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Naltrexone is a potent, competitive antagonist for μ, κ, δ, and σ-opioid receptors with Ki of 0.0825 nM, 0.509 nM, and 8.02 nM, for MOR, KOR, and DOR, respectively.
Naltrexone also inhibits IL-6 and TNFα production in human immune cell subsets following stimulation with ligands for intracellular TLRs.
Naltrexone is a TLR-4 antognist that inhibits LPS-induced TLR4 downstream NO production in microglia BV-2 cells (IC50=105 uM).

物理化学性质&存储条件

分子量 341.4009
分子式 C20H23NO4
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

DMSO: ≥ 31 mg/mL

Chemical Name/SMILES

Morphinan-6-one, 17-(cyclopropylmethyl)-4,5-epoxy-3,14-dihydroxy-, (5α)-

参考文献

1. Codd EE, et al. J Pharmacol Exp Ther. 1995 Sep;274(3):1263-70.

2. Cant R, et al. Front Immunol. 2017 Jul 11;8:809.

3. Selfridge BR, et al. J Med Chem. 2015 Jun 25;58(12):5038-52.

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