2. GPCR/G Protein Neuronal Signaling
  3. Opioid Receptor
  4. rel-SB-612111 hydrochloride

rel-SB-612111 hydrochloride 是一种新型高效的人阿片受体孤儿受体 (ORL-1) 拮抗剂，对 hORL-1 具有较高的亲和力 (Ki=0.33 nM)。rel-SB-612111 hydrochloride 对 μ-，κ- 和 δ-receptor 的 Ki 值分别为 57.6 nM，160.5 nM 和 2109 nM。rel-SB-612111 hydrochloride 能有效拮抗 Nociceptin (HY-P0183) 在急性疼痛模型中的造成的痛觉作用。

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rel-SB-612111 hydrochloride Chemical Structure

rel-SB-612111 hydrochloride Chemical Structure

CAS No. : 371980-94-8

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rel-SB-612111 hydrochloride 相关抗体

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μ Opioid Receptor/MOR κ Opioid Receptor/KOR δ Opioid Receptor/DOR NOP Receptor/ORL1

  • 生物活性

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生物活性

rel-SB-612111 hydrochloride is a novel and potent human opiate receptor-like orphan receptor (ORL-1) antagonist with a high affinity for hORL-1 (Ki=0.33 nM). rel-SB-612111 hydrochloride exhibits selectivity for μ-, κ- and δ-receptors with Ki values of 57.6 nM, 160.5 nM and 2109 nM, respecticely. rel-SB-612111 hydrochloride effectively antagonizes the pronociceptive action of Nociceptin (HY-P0183) in an acute pain model[1].
IC50 & Target

Ki: 0.33 nM (hORL-1)
Ki: 57.6 nM (μ-receptor); 160.5 nM (κ-receptor); 2109 nM (δ-receptor)[1]
体内研究
(In Vivo)

rel-SB-612111 hydrochloride (intravenous injection; 0.6-10 nmol/mouse) antagonize nociceptin-induced thermal hyperalgesia in a dose-dependent manner with an ED50 of 0.62 mg/kg[1].
rel-SB-612111 hydrochloride (intravenous injection; 0.1-5 mg/kg) causes a significant inhibition of the carrageenan-induced reduction in paw withdrawal latencies in rat, however, untreated paw are uneffected[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male rats[1]
Dosage: 0.1 mg/kg, 0.3 mg/kg, 1 mg/kg, 3 mg/kg, 5 mg/kg
Administration: Intravenous injection; single dose
Result: Had antihyperalgesic effects on carrageenan-induced rat paw.
分子量

454.86

Formula

C24H30Cl3NO
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

rel-SB-612111 hydrochloride 相关分类

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

rel-SB-612111371980-94-8Opioid ReceptorantinociceptivethermalhyperalgesiapainCHOHEK293AntihyperalgesicInhibitorinhibitorinhibit

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产品名称：
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