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  2. GPCR/G Protein Neuronal Signaling
  3. Opioid Receptor
  4. Endomorphin 1

Endomorphin 1  (Synonyms: 內(nèi)嗎啡肽 1)

目錄號(hào): HY-P0185 純度: 99.92%
COA 產(chǎn)品使用指南

Endomorphin 1，一種高度選擇性的，高親和力的 μ-opioid 受體激動(dòng)劑 (Ki: 1.11 nM)，對(duì) kappa3結(jié)合位點(diǎn)具有高親和力，Ki 值為 20 到 30 nM 之間。Endomorphin 1 具有鎮(zhèn)痛特性。

MCE 的所有產(chǎn)品僅用作科學(xué)研究或藥證申報(bào)，我們不為任何個(gè)人用途提供產(chǎn)品和服務(wù)

Custom Peptide Synthesis

Endomorphin 1 Chemical Structure

Endomorphin 1 Chemical Structure

CAS No. : 189388-22-5

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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in Water ￥672
In-stock
5 mg ￥500
In-stock
10 mg ￥700
In-stock
25 mg ￥1400
In-stock
50 mg   詢價(jià)  
100 mg   詢價(jià)  

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Customer Review

Other Forms of Endomorphin 1:

MCE 顧客使用本產(chǎn)品發(fā)表的 2 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

Endomorphin 1, a high affinity, highly selective agonist of the μ-opioid receptor (Ki: 1.11 nM), displays reasonable affinities for kappa3 binding sites, with Ki value between 20 and 30 nM. Endomorphin 1 has antinociceptive properties[1][2][4].

IC50 & Target

μ Opioid Receptor/MOR

1.11 nM (Ki)

細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
CHO EC50
0.001 nM
Compound: 1, Endomorphin-1
Activity at mu opioid receptor assessed as increase in calcium level in CHO cells by aequorin luminescence based calcium assay
Activity at mu opioid receptor assessed as increase in calcium level in CHO cells by aequorin luminescence based calcium assay
[PMID: 17266203]
CHO EC50
932 nM
Compound: 1, Endomorphin-1
Activity at delta opioid receptor assessed as increase in calcium level in CHO cells by aequorin luminescence based calcium assay
Activity at delta opioid receptor assessed as increase in calcium level in CHO cells by aequorin luminescence based calcium assay
[PMID: 17266203]
CHO-K1 IC50
3.2 nM
Compound: 1
Agonist activity at MOP receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins
Agonist activity at MOP receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins
[PMID: 23022277]
HEK293 EC50
14.4 nM
Compound: 1, EM-1
Agonist activity at mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by liquid scintillation counter
Agonist activity at mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by liquid scintillation counter
[PMID: 22724433]
HEK293 EC50
61 nM
Compound: EM-1
Agonist activity at mu opioid receptor (unknown origin) expressed in human HEK293 cells assessed as increase in cAMP accumulation using [3H]-cAMP as substrate measured after 30mins by liquid scintillation counting method
Agonist activity at mu opioid receptor (unknown origin) expressed in human HEK293 cells assessed as increase in cAMP accumulation using [3H]-cAMP as substrate measured after 30mins by liquid scintillation counting method
[PMID: 32199689]
SH-SY5Y IC50
65.4 nM
Compound: 1
Agonist activity at mu-opioid receptor in human SH-SY5Y cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by immunoassay
Agonist activity at mu-opioid receptor in human SH-SY5Y cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by immunoassay
[PMID: 22680612]
體外研究
(In Vitro)

Endomorphin 1 inhibits Forskolin (HY-15371) (1 μM) stimulated cyclic AMP formation with a pIC50 value of 8.03 in In CHOμ cells[5].
Endomorphin 1 (1-10 μM) increases interleukin-8 secretion in Caco-2 cells[6].
Endomorphin 1 (1 μM) inhibits excitatory transmission in adult rat substantia gelatinosa neurons[7].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
體內(nèi)研究
(In Vivo)

Endomorphin 1 (i.c.v.) shows antinociceptive properties in mice, with an ED50 value of 6.16 nM[2].
Endomorphin 1 (50 μg/kg, i.v.) alleviates myocardial ischemia/reperfusion injury (MIRI) by inhibiting the inflammatory response[3].

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

Animal Model: ICR mice[2].
Dosage: 6.16 nM (ED50)
Administration: Intracerebroventricularly (i.c.v.) injection
Result: Inhibited dose-dependently the tail-flick response.
Animal Model: Rats[3].
Dosage: 50 μg/kg
Administration: Intravenously following LAD ligation for 25 min, subsequently the LAD was reperfused for 120 min.
Result: Alleviated MIRI by reducing the production of free radicals.
Dncreased LDH and CK-MB activities.
Increased SOD activity and decreased MDA content.
Decreased IL-6 and TNF-α plasma content.
分子量

610.70

Formula

C34H38N6O5
CAS 號(hào)
性狀

固體

顏色

White to off-white

Sequence

Tyr-Pro-Trp-Phe-NH2
Sequence Shortening

YPWF-NH2
中文名稱

內(nèi)嗎啡肽 1
結(jié)構(gòu)分類
初始來(lái)源
運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.
儲(chǔ)存方式

Sealed storage, away from moisture and light, under nitrogen

Powder -80°C 2 years
-20°C 1 year

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

溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn)： 

DMSO 中的溶解度 : ≥ 50 mg/mL (81.87 mM; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響，請(qǐng)使用新開封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 1.6375 mL 8.1873 mL 16.3747 mL
5 mM 0.3275 mL 1.6375 mL 3.2749 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 and light, under nitrogen)。-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。

  • 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

只
由于實(shí)驗(yàn)過程有損耗，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
純度 & 產(chǎn)品資料
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 and light, under nitrogen)。-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
DMSO 1 mM 1.6375 mL 8.1873 mL 16.3747 mL 40.9366 mL
5 mM 0.3275 mL 1.6375 mL 3.2749 mL 8.1873 mL
10 mM 0.1637 mL 0.8187 mL 1.6375 mL 4.0937 mL
15 mM 0.1092 mL 0.5458 mL 1.0916 mL 2.7291 mL
20 mM 0.0819 mL 0.4094 mL 0.8187 mL 2.0468 mL
25 mM 0.0655 mL 0.3275 mL 0.6550 mL 1.6375 mL
30 mM 0.0546 mL 0.2729 mL 0.5458 mL 1.3646 mL
40 mM 0.0409 mL 0.2047 mL 0.4094 mL 1.0234 mL
50 mM 0.0327 mL 0.1637 mL 0.3275 mL 0.8187 mL
60 mM 0.0273 mL 0.1365 mL 0.2729 mL 0.6823 mL
80 mM 0.0205 mL 0.1023 mL 0.2047 mL 0.5117 mL
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：
Endomorphin 1
目錄號(hào)：
HY-P0185
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