2. GPCR/G Protein Neuronal Signaling
  3. Opioid Receptor
  4. KOR agonist 6

KOR agonist 6 是一种 KOR 激动剂 (Ki = 0.25 pM)。KOR agonist 6 在 CHO 细胞中对 MOR 和 DOR 显示出激动活性，并抑制 Forskolin (HY-15371) 刺激的 cAMP 积累。KOR agonist 6 刺激 KOR 介导的 [35S]GTPγS 结合，并在表达 KOR 的 HEK293 细胞中以强效激动活性抑制 cAMP 积累，同时显示出较低的 β-arrestin 募集效力。KOR agonist 6 在小鼠中表现出镇痛效果。KOR agonist 6 可用于研究具有减少中枢神经系统 (CNS) 副作用的镇痛剂。

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KOR agonist 6

KOR agonist 6 Chemical Structure

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KOR agonist 6 相关抗体

Top Publications Citing Use of Products

查看 Opioid Receptor 亚型特异性产品:

查看所有亚型
μ Opioid Receptor/MOR κ Opioid Receptor/KOR δ Opioid Receptor/DOR NOP Receptor/ORL1

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

KOR agonist 6 is a KOR agonist (Ki = 0.25 pM). KOR agonist 6 shows agonistic activity at MOR and DOR in CHO cells and inhibits Forskolin (HY-15371)-stimulated cAMP accumulation. KOR agonist 6 stimulates KOR-mediated [35S]GTPγS binding and inhibits cAMP accumulation in KOR-expressing HEK293 cells with potent agonistic activity, while showing lower β-arrestin recruitment potency. KOR agonist 6 demonstrates anti-nociceptive efficacy in mice. KOR agonist 6 can be used for the study of analgesics with reduced central nervous system (CNS) side effects[1].

IC50 & Target[1]

κ Opioid Receptor/KOR

0.25 pM (Ki)

μ Opioid Receptor/MOR

14.1 nM (Ki)

δ Opioid Receptor/DOR

120.7 nM (Ki)

μ Opioid Receptor/MOR

44.78 nM (EC50)

δ Opioid Receptor/DOR

15.26 nM (EC50)

体外研究
(In Vitro)

KOR agonist 6 (Compound 5i) 对 κ-阿片受体 (KOR (Ki = 0.00025 nM)) 表现出超高结合亲和力，并对 μ-阿片受体 (MOR (Ki = 14.1 nM)) 和 δ-阿片受体 (DOR (Ki = 120.7 nM)) 具有出色的亚型选择性[1]。
KOR agonist 6 在 CHO 细胞中对 MOR (EC50 = 44.78 nM, Emax = 88.71%) 和 DOR (EC50 = 15.26 nM, Emax = 85.16%) 显示出激动活性，并抑制 Forskolin (HY-15371) 刺激的 cAMP 积累 (EC50 = 200.3 nM, Emax = 99.51%)[1]。
KOR agonist 6 在表达 KOR 的细胞膜中刺激 KOR 介导的 [35S]GTPγS 结合，表现出强效活性 (EC50 = 0.024 nM, Emax = 106.9%)，在表达 KOR 的 HEK293 细胞中以超强激动活性抑制 cAMP 积累 (EC50 = 0.43 pM, Emax = 63.63%)，并在转染 KOR-Tango 质粒的 HTLA 细胞中以较低效力诱导 β-arrestin 蛋白募集 (EC50 = 0.143 nM, Emax = 42.89%)[1]。

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

KOR agonist 6 相关抗体:
体内研究
(In Vivo)

KOR激动剂6 (Compound 5i) (0.4-8.0 mg/kg，腹腔注射，给药后 6 小时检测) 在小鼠热板试验中显示出剂量依赖性的镇痛效果 (ED50 = 0.6 mg/kg)[1]。
KOR激动剂6 (0.08-8.0 mg/kg，腹腔注射，给药后 6 小时检测) 在小鼠腹部收缩试验中表现出剂量依赖性的镇痛活性 (ED50 = 1.5 mg/kg)[1]。
KOR激动剂6 (0.8-8.0 mg/kg，腹腔注射，连续 6 天条件化，第 8 天进行 15 分钟自由探索测试) 在雄性 CD1 小鼠中未显示出显著的条件性位置厌恶[1]。
KOR激动剂6 (0.8-8.0 mg/kg，腹腔注射，给药后 6 小时监测 1 小时) 在雄性昆明小鼠中未导致自发运动活动 (总移动距离) 的显著减少[1]。

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

Animal Model: Female Kunming mice (18-22 g) were used, with the nociceptive response (latency to licking back paws) assessed on a 55 °C heated smooth surface; mice with no response within 30 s before administration were excluded, and a 60 s cutoff time was set to prevent tissue damage[1]
Dosage: 0.4, 0.8, 1.2, 1.6, 8.0 mg/kg
Administration: i.p., detected at 6 h post-administration
Result: Showed dose-dependent antinociceptive efficacy in mice hot plate test (ED50 = 0.6 mg/kg).
Animal Model: Male Kunming mice (18-22 g)[1]
Dosage: 0.08, 0.8, 3.2, 6.4, 8.0 mg/kg
Administration: i.p., detected at 6 h post-administration followed by 0.6% acetic acid injection
Result: Showed dose-dependent antinociceptive activity in mice abdominal constriction test(ED50 = 1.5 mg/kg).
分子量

580.72

Formula

C35H40N4O4
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

KOR agonist 6 相关分类

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  • 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:

KOR agonist 6KOR agonist6KOR agonist-6Opioid ReceptorKORDORMOR,β-arrestincAMPInhibitorinhibitorinhibit

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