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

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

目錄號(hào): HY-P1033 純度: 99.92%
COA 產(chǎn)品使用指南 技術(shù)支持

[Pyr1]-Apelin-13 是一種高效的,選擇性的內(nèi)源性 apelin 受體激動(dòng)劑。

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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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Customer Review

Other Forms of [Pyr1]-Apelin-13:

MCE 顧客使用本產(chǎn)品發(fā)表的 1 篇科研文獻(xiàn)

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

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

細(xì)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]
體外研究
(In Vitro)

[Pyr1]-apelin-13 包裹在 lipoPEG 顆粒 (lipoPEG-PA13) 中,可在生理?xiàng)l件下實(shí)現(xiàn)持續(xù)和延長(zhǎng)的藥物釋放[1]

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

體內(nèi)研究
(In Vivo)

[Pyr1]-apelin-13 納米載體在壓力過(guò)載引起的心力衰竭小鼠模型中表現(xiàn)出[Pyr1]-apelin-13 在預(yù)防心功能障礙方面的可持續(xù)長(zhǎng)期作用[1]。[Pyr1]apelin-13 (1,5 μg) 改善大鼠的運(yùn)動(dòng)活動(dòng)并減少疼痛癥狀、空腔大小和 caspase-3 水平。[Pyr1]apelin-13 (1,5 μg) 顯著增加熱縮爪潛伏期。與 SCI 后第二周的 SCI 動(dòng)物相比,5 μg 劑量的[Pyr1]apelin-13 也會(huì)顯著降低縮爪閾值[2]

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

分子量

1533.80

Formula

C69H108N22O16S

CAS 號(hào)
性狀

固體

顏色

White to off-white

Sequence Shortening

{Glp}-RPRLSHKGPMPF

中文名稱

[Pyr1]-愛(ài)帕琳肽-13

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.

儲(chǔ)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)

溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn): 

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

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)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
查看完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液;一旦配成溶液,請(qǐng)分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(nèi)使用,-20°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(nèi)使用。

* 備注:如您選擇水作為儲(chǔ)備液,請(qǐng)稀釋至工作液后,再用 0.22 μm 的濾膜過(guò)濾除菌后使用。

  • 摩爾計(jì)算器

  • 稀釋計(jì)算器

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

質(zhì)量
=
濃度
×
體積
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動(dòng)物實(shí)驗(yàn):

以下溶解方案,請(qǐng)直接配制工作液。建議現(xiàn)用現(xiàn)配,在短期內(nèi)盡快用完。 以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比; 如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過(guò)加熱和/或超聲的方式助溶。

  • 方案 一

    請(qǐng)依序添加每種溶劑: PBS

    Solubility: 100 mg/mL (65.20 mM); 澄清溶液; 超聲助溶

動(dòng)物溶解方案計(jì)算器
請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息:

給藥劑量

mg/kg

動(dòng)物的平均體重

g

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

由于實(shí)驗(yàn)過(guò)程有損耗,建議您多配一只動(dòng)物的量
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
該產(chǎn)品水溶性佳,請(qǐng)具體參考實(shí)測(cè) 水 / PBS / Saline 中的溶解度數(shù)據(jù)。
您所需的儲(chǔ)備液濃度超過(guò)該產(chǎn)品的實(shí)測(cè)溶解度,如有需要,請(qǐng)與 MCE 中國(guó)技術(shù)支持聯(lián)系。
純度 & 產(chǎn)品資料

純度: 99.92%

參考文獻(xiàn)

完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液;一旦配成溶液,請(qǐng)分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(nèi)使用,-20°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)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

* 備注:如您選擇水作為儲(chǔ)備液,請(qǐng)稀釋至工作液后,再用 0.22 μm 的濾膜過(guò)濾除菌后使用。

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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產(chǎn)品名稱:
[Pyr1]-Apelin-13
目錄號(hào):
HY-P1033
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