2. GPCR/G Protein
  3. Apelin Receptor (APJ) Arrestin
  4. APJ receptor agonist 6

APJ receptor agonist 6 (compound 9) 是一种有效的 APJ (apelin 受体)激动剂，其 Ki 为 0.059 μM。APJ receptor agonist 6 对钙 (calcium)、cAMP 和 β-arrestin 的 EC50 分别为 0.800、0.844 和 6.22 μM。

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APJ receptor agonist 6 Chemical Structure

APJ receptor agonist 6 Chemical Structure

CAS No. : 1965244-85-2

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APJ receptor agonist 6 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

APJ receptor agonist 6 (compound 9) is a potent APJ (apelin receptor) agonist, with Ki of 1.3 μM. APJ receptor agonist 6 has EC50 values of 0.070 , 0.097, and 0.063 μM for calcium, cAMP, and β-arrestin, respectively[1].

IC50 & Target

EC50: 0.800 ± 0.1 μM (Apelin Receptor calcium), 0.844 ± 0.2 μM (Apelin Receptor cAMP), 6.22 ± 2.0 μM (Apelin Receptor β-arrestin), >10 μM (AT1 calcium)[1]
细胞效力
(Cellular Effect)
Cell Line Type Value Description References
CHO EC50
> 10 μM
Compound: 9
Agonist activity at human AGTR1 stably expressed in CHO cells assessed as increase in intracellular calcium mobilization measured at 1 sec intervals for 90 sec by calcium 5 dye based FLIPR assay
Agonist activity at human AGTR1 stably expressed in CHO cells assessed as increase in intracellular calcium mobilization measured at 1 sec intervals for 90 sec by calcium 5 dye based FLIPR assay
[PMID: 31948845]
CHO EC50
0.8 μM
Compound: 9
Agonist activity at human APJ receptor stably expressed in CHO cells co-expressing Galphaq16 assessed as increase in intracellular calcium mobilization measured at 1 sec intervals for 90 secs by calcium 5 dye based FLIPR assay
Agonist activity at human APJ receptor stably expressed in CHO cells co-expressing Galphaq16 assessed as increase in intracellular calcium mobilization measured at 1 sec intervals for 90 secs by calcium 5 dye based FLIPR assay
[PMID: 31948845]
CHO EC50
0.844 μM
Compound: 9
Agonist activity at human APJ receptor stably expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
Agonist activity at human APJ receptor stably expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
[PMID: 31948845]
CHO-K1 EC50
3406 nM
Compound: 22
Partial agonist activity at rat NTS2 receptor expressed in CHOK1 cells assessed as calcium mobilization by FLIPR assay
Partial agonist activity at rat NTS2 receptor expressed in CHOK1 cells assessed as calcium mobilization by FLIPR assay
[PMID: 27369451]
CHO-K1 EC50
6.22 μM
Compound: 9
Agonist activity at human APJ receptor stably expressed in CHOK1 cells assessed as induction of beta-arrestin 2 recruitment incubated for 90 mins by PathHunter assay
Agonist activity at human APJ receptor stably expressed in CHOK1 cells assessed as induction of beta-arrestin 2 recruitment incubated for 90 mins by PathHunter assay
[PMID: 31948845]
分子量

523.60

Formula

C29H34FN3O5
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

APJ receptor 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:

APJ receptor agonist 61965244-85-2APJ receptor agonist6APJ receptor agonist-6Apelin Receptor (APJ)ArrestinApelinapelin receptorAgonistPyrazoleAGTRL1APLNRcardiometabolic diseasesInhibitorinhibitorinhibit

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APJ receptor agonist 6
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