1. GPCR/G Protein Neuronal Signaling
  2. Opioid Receptor
  3. SR-16435

SR-16435 是 NOP/μ-opioid 受体部分激动剂,具有较高的结合亲和力 (NOP 受体 Ki=7.49; μ-opioid 受体 Ki=2.70)。SR-16435 具有缓解疼痛的作用。

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SR-16435 Chemical Structure

SR-16435 Chemical Structure

CAS No. : 857262-16-9

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

SR-16435 is a nociceptin/orphanin FQ (NOP)/μ-opioid receptor partial agonist, with high binding affinity (NOP receptor Ki=7.49; μ-Opioid receptor Ki=2.70). SR-16435 can relieve pain[1].

IC50 & Target[1]

NOP receptor

7.49 (Ki)

μ-opioid

2.70 (Ki)

κ-opioid

219.47 (Ki)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
CHO EC50
< 10000 nM
Compound: 2
Agonist activity at human kappa opioid receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis
Agonist activity at human kappa opioid receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis
[PMID: 23623415]
CHO EC50
28.7 nM
Compound: 2
Agonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis
Agonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis
[PMID: 23623415]
CHO EC50
29 nM
Compound: 2
Agonist activity at human mu opioid receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis
Agonist activity at human mu opioid receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis
[PMID: 23623415]
体内研究
(In Vivo)

SR 16435 (10, 30 mg/kg; s.c.; single-dose) produces dose-dependent increase in tail-flick latency and induces antinociception[1].
SR 16435 (10, 30 mg/kg; s.c. once daily for 9 days) produces an increase in tail-lick latency across days, induces conditioned place preference, and decreases global activity[1].

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

Animal Model: 20 to 25 g male ICR mice[1]
Dosage: 10, 30 mg/kg
Administration: s.c. for single-dose
Result: Produced dose-dependent increase in tail-flick latency and induced antinociception.
Animal Model: 20 to 25 g male ICR mice[1]
Dosage: 10, 30 mg/kg
Administration: s.c. once daily for 9 days
Result: Produced an increase in tail-lick latency across days, induced conditioned place preference, and decreased global activity.
分子量

338.49

Formula

C22H30N2O

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
  • 摩尔计算器

  • 稀释计算器

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× = ×
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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.

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HY-122681
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