1. GPCR/G Protein
  2. Apelin Receptor (APJ)
  3. [Pyr1]-Apelin-13

[Pyr1]-Apelin-13  (Synonyms: [pGlu1]-Apelin-13)

目录号: HY-P1033 纯度: 99.92%
COA 产品使用指南

[Pyr1]-Apelin-13 是一种高效的,选择性的内源性 apelin 受体激动剂。

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Custom Peptide Synthesis

[Pyr1]-Apelin-13 Chemical Structure

[Pyr1]-Apelin-13 Chemical Structure

CAS No. : 217082-60-5

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1 mg ¥784
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2 mg ¥1254
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Other Forms of [Pyr1]-Apelin-13:

MCE 顾客使用本产品发表的 1 篇科研文献

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

[Pyr1]-Apelin-13 is a highly potent, selective endogenous apelin receptor (APJ) agonist.

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
CHO EC50
0.0003 μM
Compound: Pyr-Apelin-13
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 EC50
0.002 μM
Compound: Pyr-Apelin-13
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-K1 EC50
0.001 μM
Compound: Pyr-Apelin-13
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]
HEK293 EC50
0.047 nM
Compound: 1; (Pyr1)apelin-13
Agonist activity at human APJ-R expressed in HEK293 cells assessed as inhibition of forskolin- stimulated cAMP accumulation incubated for 30 mins by HTRF assay
Agonist activity at human APJ-R expressed in HEK293 cells assessed as inhibition of forskolin- stimulated cAMP accumulation incubated for 30 mins by HTRF assay
[PMID: 31724863]
HEK293 EC50
0.062 nM
Compound: 1; (Pyr1)apelin-13
Agonist activity at rat APJ-R expressed in HEK293 cells assessed as inhibition of forskolin- stimulated cAMP accumulation incubated for 30 mins by HTRF assay
Agonist activity at rat APJ-R expressed in HEK293 cells assessed as inhibition of forskolin- stimulated cAMP accumulation incubated for 30 mins by HTRF assay
[PMID: 31724863]
HEK293 EC50
0.84 nM
Compound: Ape13
Agonist activity at human APJ receptor expressed in HEK293 cells assessed as induction of Galphai1 subunit dissociation incubated for 5 mins by BRET assay
Agonist activity at human APJ receptor expressed in HEK293 cells assessed as induction of Galphai1 subunit dissociation incubated for 5 mins by BRET assay
[PMID: 25668242]
HEK293 EC50
1.1 nM
Compound: Ape13
Activity at human APJ receptor expressed in HEK293 cells assessed as dissociation of Galphai1 from Gbetagamma subunit after 5 mins by BRET assay
Activity at human APJ receptor expressed in HEK293 cells assessed as dissociation of Galphai1 from Gbetagamma subunit after 5 mins by BRET assay
[PMID: 29461833]
HEK293 IC50
1.2 nM
Compound: Ape13
Displacement of [125I]apelin-13[Glp65,Nle75,Tyr77] from YFP epitope-tagged human APJ receptor expressed in HEK293 cell membranes incubated for 1 hr by gamma counting method
Displacement of [125I]apelin-13[Glp65,Nle75,Tyr77] from YFP epitope-tagged human APJ receptor expressed in HEK293 cell membranes incubated for 1 hr by gamma counting method
[PMID: 25668242]
HEK293 EC50
1.4 nM
Compound: Ape13
Agonist activity at human APJ receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced intracellular cAMP production incubated for 30 mins by TR-FRET assay
Agonist activity at human APJ receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced intracellular cAMP production incubated for 30 mins by TR-FRET assay
[PMID: 25668242]
HEK293 EC50
12.2 pM
Compound: [pyr1]-apelin-13
Agonist activity at APJ receptor in HEK293 cells assessed as inhibition of forskolin-induced cAMP level incubated for 5 mins prior to forskolin challenge measured after 30 mins by TR-FRET assay
Agonist activity at APJ receptor in HEK293 cells assessed as inhibition of forskolin-induced cAMP level incubated for 5 mins prior to forskolin challenge measured after 30 mins by TR-FRET assay
[PMID: 25241924]
HEK293 EC50
24 nM
Compound: Ape13
Induction of human HA-tagged APJ receptor internalization expressed in HEK293 cells after 30 mins by ELISA
Induction of human HA-tagged APJ receptor internalization expressed in HEK293 cells after 30 mins by ELISA
[PMID: 29461833]
HEK293 EC50
26 nM
Compound: Ape13
Agonist activity at human APJ receptor expressed in HEK293 cells assessed as induction of beta-arrestin-1 recruitment subunit dissociation incubated for 30 mins by BRET assay
Agonist activity at human APJ receptor expressed in HEK293 cells assessed as induction of beta-arrestin-1 recruitment subunit dissociation incubated for 30 mins by BRET assay
[PMID: 25668242]
HEK293 EC50
29 nM
Compound: Ape13
Agonist activity at human APJ receptor expressed in HEK293 cells assessed as induction of beta-arrestin-2 recruitment subunit dissociation incubated for 30 mins by BRET assay
Agonist activity at human APJ receptor expressed in HEK293 cells assessed as induction of beta-arrestin-2 recruitment subunit dissociation incubated for 30 mins by BRET assay
[PMID: 25668242]
HEK293 EC50
5.9 nM
Compound: Ape13
Agonist activity at human APJ receptor expressed in HEK293 cells assessed as induction of GalphaoA subunit dissociation incubated for 5 mins by BRET assay
Agonist activity at human APJ receptor expressed in HEK293 cells assessed as induction of GalphaoA subunit dissociation incubated for 5 mins by BRET assay
[PMID: 25668242]
HEK293 EC50
60 nM
Compound: Ape13
Activity at GFP10-tagged human APJ receptor expressed in HEK293 cells assessed as induction of RlucII-tagged beta-arrestin-2 recruitment after 30 mins by BRET assay
Activity at GFP10-tagged human APJ receptor expressed in HEK293 cells assessed as induction of RlucII-tagged beta-arrestin-2 recruitment after 30 mins by BRET assay
[PMID: 29461833]
体外研究
(In Vitro)

[Pyr1]-apelin-13 包裹在 lipoPEG 颗粒 (lipoPEG-PA13) 中,可在生理条件下实现持续和延长的药物释放[1]

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

体内研究
(In Vivo)

[Pyr1]-apelin-13 纳米载体在压力过载引起的心力衰竭小鼠模型中表现出[Pyr1]-apelin-13 在预防心功能障碍方面的可持续长期作用[1]。[Pyr1]apelin-13 (1,5 μg) 改善大鼠的运动活动并减少疼痛症状、空腔大小和 caspase-3 水平。[Pyr1]apelin-13 (1,5 μg) 显著增加热缩爪潜伏期。与 SCI 后第二周的 SCI 动物相比,5 μg 剂量的[Pyr1]apelin-13 也会显著降低缩爪阈值[2]

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

分子量

1533.80

Formula

C69H108N22O16S

CAS 号
性状

固体

颜色

White to off-white

Sequence Shortening

{Glp}-RPRLSHKGPMPF

中文名称

[Pyr1]-爱帕琳肽-13

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Sealed storage, away from moisture

Powder -80°C 2 years
-20°C 1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
细胞实验: 

H2O 中的溶解度 : 100 mg/mL (65.20 mM; 超声助溶)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 0.6520 mL 3.2599 mL 6.5198 mL
5 mM 0.1304 mL 0.6520 mL 1.3040 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物实验:

以下溶解方案,请直接配制工作液。建议现用现配,在短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比; 如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶。

  • 方案 一

    请依序添加每种溶剂: PBS

    Solubility: 100 mg/mL (65.20 mM); 澄清溶液; 超声助溶

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
该产品水溶性佳,请具体参考实测 水 / PBS / Saline 中的溶解度数据。
您所需的储备液浓度超过该产品的实测溶解度,如有需要,请与 MCE 中国技术支持联系。
纯度 & 产品资料

纯度: 99.92%

参考文献

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
H2O 1 mM 0.6520 mL 3.2599 mL 6.5198 mL 16.2994 mL
5 mM 0.1304 mL 0.6520 mL 1.3040 mL 3.2599 mL
10 mM 0.0652 mL 0.3260 mL 0.6520 mL 1.6299 mL
15 mM 0.0435 mL 0.2173 mL 0.4347 mL 1.0866 mL
20 mM 0.0326 mL 0.1630 mL 0.3260 mL 0.8150 mL
25 mM 0.0261 mL 0.1304 mL 0.2608 mL 0.6520 mL
30 mM 0.0217 mL 0.1087 mL 0.2173 mL 0.5433 mL
40 mM 0.0163 mL 0.0815 mL 0.1630 mL 0.4075 mL
50 mM 0.0130 mL 0.0652 mL 0.1304 mL 0.3260 mL
60 mM 0.0109 mL 0.0543 mL 0.1087 mL 0.2717 mL

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

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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产品名称:
[Pyr1]-Apelin-13
目录号:
HY-P1033
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