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

DAMGO 是 一种选择性的 μ-阿片受体 (μ-OPR) 激动剂,Kd 值为 3.46 nM。

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Custom Peptide Synthesis

DAMGO Chemical Structure

DAMGO Chemical Structure

CAS No. : 78123-71-4

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Customer Review

Other Forms of DAMGO:

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

DAMGO is a μ-opioid receptor (μ-OPR ) selective agonist with a Kd of 3.46 nM for native μ-OPR[1].

IC50 & Target

μ Opioid Receptor/MOR

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
CHO EC50
0.088 μM
Compound: DAMGO
Agonist activity at human mu opioid receptor expressed in CHO cells by cAMP assay
Agonist activity at human mu opioid receptor expressed in CHO cells by cAMP assay
[PMID: 31147104]
CHO EC50
110 nM
Compound: DAMGO
Agonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding by scintillation counting
Agonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding by scintillation counting
[PMID: 21351746]
CHO EC50
110 nM
Compound: DAMGO
Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding after 60 mins
Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding after 60 mins
[PMID: 17433695]
CHO EC50
110 nM
Compound: DAMGO
Activity at human mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay
Activity at human mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay
[PMID: 16392810]
CHO EC50
19 nM
Compound: DAMGO
Agonist activity at mouse mu opioid receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP formation incubated for 8 min followed by forskolin stimulation by ELISA
Agonist activity at mouse mu opioid receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP formation incubated for 8 min followed by forskolin stimulation by ELISA
[PMID: 31782922]
CHO EC50
19 nM
Compound: DAMGO
Agonist activity at mouse mu opioid receptor-1 expressed in CHO cell membranes assessed as [35S]GTPgammaS binding incubated for 60 mins by scintillation spectroscopic analysis
Agonist activity at mouse mu opioid receptor-1 expressed in CHO cell membranes assessed as [35S]GTPgammaS binding incubated for 60 mins by scintillation spectroscopic analysis
[PMID: 27556704]
CHO EC50
19.7 nM
Compound: DAMGO
Agonist activity at human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay
Agonist activity at human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay
[PMID: 30996778]
CHO IC50
2.5 nM
Compound: DAMGO
Agonist activity at human MOR expressed in CHO cells assessed as induction of membrane potential change measured every 3 secs for 30 secs by fluorescent membrane potential assay
Agonist activity at human MOR expressed in CHO cells assessed as induction of membrane potential change measured every 3 secs for 30 secs by fluorescent membrane potential assay
[PMID: 26789491]
CHO EC50
2.66 nM
Compound: DAMGO
Activity at CCK2R-MOPR coexpressed in CHO cells co-transfected with delta-6-Galphaqi4-myr assessed as intracellular calcium release by FLIPR
Activity at CCK2R-MOPR coexpressed in CHO cells co-transfected with delta-6-Galphaqi4-myr assessed as intracellular calcium release by FLIPR
[PMID: 19113864]
CHO EC50
23 nM
Compound: DAMGO
Agonist activity at human MOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
Agonist activity at human MOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
[PMID: 32435376]
CHO EC50
25.5 nM
Compound: DAMGO
Agonist activity at human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay
Agonist activity at human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay
[PMID: 32530286]
CHO IC50
3 nM
Compound: DAMGO
Binding affinity against rat mu-opioid receptor expressed in CHO cells by competitive inhibition of 1 nM [3H]DAMGO
Binding affinity against rat mu-opioid receptor expressed in CHO cells by competitive inhibition of 1 nM [3H]DAMGO
[PMID: 9873480]
CHO EC50
30 nM
Compound: DAMGO
Agonist activity at human MOR expressed in CHO cell membranes after 60 mins by [35S]GTP-gamma-S binding assay
Agonist activity at human MOR expressed in CHO cell membranes after 60 mins by [35S]GTP-gamma-S binding assay
[PMID: 27096047]
CHO EC50
32.6 nM
Compound: DAMGO
Agonist activity at human mu opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
Agonist activity at human mu opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
[PMID: 24657054]
CHO ED50
34 nM
Compound: DAMGO
Agonist activity at human recombinant mu opioid receptor expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 3 hrs by liquid scintillation counting analysis
Agonist activity at human recombinant mu opioid receptor expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 3 hrs by liquid scintillation counting analysis
[PMID: 23618710]
CHO EC50
35.3 nM
Compound: DAMGO, MOP
Partial agonist activity at human MOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting
Partial agonist activity at human MOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting
[PMID: 21866885]
CHO EC50
40 nM
Compound: DAMGO
Agonist activity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay
Agonist activity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay
[PMID: 18380425]
CHO ED50
42 nM
Compound: DAMGO
Agonist activity at human recombinant mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 3 hrs by liquid scintillation counting
Agonist activity at human recombinant mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 3 hrs by liquid scintillation counting
[PMID: 19627147]
CHO ED50
42 nM
Compound: DAMGO
Agonist activity at human mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S assay
Agonist activity at human mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S assay
[PMID: 17625813]
CHO EC50
45.06 nM
Compound: DAMGO
Activity at monocloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay
Activity at monocloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay
[PMID: 19199782]
CHO EC50
5.6 nM
Compound: DAMGO
Agonist activity at mouse cloned mu opioid receptor expressed in CHO cells after 60 mins by [35S]GTPgammaS binding assay
Agonist activity at mouse cloned mu opioid receptor expressed in CHO cells after 60 mins by [35S]GTPgammaS binding assay
[PMID: 24103580]
CHO EC50
55 nM
Compound: DAMGO
Activity at human cloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay
Activity at human cloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay
[PMID: 19027293]
CHO EC50
55 nM
Compound: DAMGO
Agonist activity at human mu opioid receptor expressed in CHO cell membrane by [35S]GTPgammaS binding assay
Agonist activity at human mu opioid receptor expressed in CHO cell membrane by [35S]GTPgammaS binding assay
[PMID: 17935988]
CHO EC50
55 nM
Compound: DAMGO
Agonist activity at human mu opioid receptor expressed in CHO cell membrane assessed as stimulation of [35S]GTPgammaS binding after 60 mins by liquid scintillation counting
Agonist activity at human mu opioid receptor expressed in CHO cell membrane assessed as stimulation of [35S]GTPgammaS binding after 60 mins by liquid scintillation counting
[PMID: 23434225]
CHO EC50
55 nM
Compound: DAMGO
Agonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 60 mins by scintillation counting
Agonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 60 mins by scintillation counting
[PMID: 23142613]
CHO EC50
55 nM
Compound: DAMGO
Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [33S]GTPgammaS binding after 60 mins by scintillation counting
Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [33S]GTPgammaS binding after 60 mins by scintillation counting
[PMID: 22439881]
CHO EC50
6.86 nM
Compound: DAMGO, MOP
Partial agonist activity at human DOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting
Partial agonist activity at human DOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting
[PMID: 21866885]
CHO EC50
7.2 nM
Compound: DAMGO
Agonist activity at human MOR expressed in CHO cell membranes incubated for 1 hr by [35S]-GTPgammaS coupling assay
Agonist activity at human MOR expressed in CHO cell membranes incubated for 1 hr by [35S]-GTPgammaS coupling assay
[PMID: 31834798]
CHO EC50
7.5 nM
Compound: DAMGO
Agonist activity at human MOR expressed in CHO cells assessed as increase in intracellular Ca2+ level after 30 mins by microplate reader analysis
Agonist activity at human MOR expressed in CHO cells assessed as increase in intracellular Ca2+ level after 30 mins by microplate reader analysis
[PMID: 25783191]
CHO EC50
7.57 nM
Compound: DAMGO
Agonist activity at human MOR expressed in CHO cells by [35S]GTPgammaS binding assay
Agonist activity at human MOR expressed in CHO cells by [35S]GTPgammaS binding assay
[PMID: 25248680]
CHO EC50
81 nM
Compound: DAMGO
Agonist activity at rat mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay
Agonist activity at rat mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay
[PMID: 25221662]
CHO EC50
9.61 nM
Compound: DAMGO
Agonist activity at human MOR expressed in CHO cells assessed as increase in intracellular Ca2+ level after 30 mins by cytosensor micrometer
Agonist activity at human MOR expressed in CHO cells assessed as increase in intracellular Ca2+ level after 30 mins by cytosensor micrometer
[PMID: 25783191]
CHO-K1 IC50
0.02 μM
Compound: DAMGO
Displacement of [3H]Diprenorphine from human recombinant mu opioid receptor expressed in CHOK1 cells after 60 mins
Displacement of [3H]Diprenorphine from human recombinant mu opioid receptor expressed in CHOK1 cells after 60 mins
[PMID: 23403082]
HEK293 IC50
0.005 μM
Compound: DAMGO
Agonist activity at human mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP production after 30 mins by HTRF assay
Agonist activity at human mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP production after 30 mins by HTRF assay
[PMID: 25087049]
HEK293 IC50
0.0051 μM
Compound: DAMGO
Agonist activity at human MOR expressed in HEK293 cells assessed as inhibition of forskolin-induced adenylyl cyclase-mediated cAMP accumulation after 30 mins by HTRF assay
Agonist activity at human MOR expressed in HEK293 cells assessed as inhibition of forskolin-induced adenylyl cyclase-mediated cAMP accumulation after 30 mins by HTRF assay
[PMID: 27776274]
HEK293 IC50
19.3 nM
Compound: DAMGO
Agonist activity at human MOR expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation by EIA method
Agonist activity at human MOR expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation by EIA method
[PMID: 27607020]
HEK293 EC50
3.04 nM
Compound: DAMGO
Agonist activity at FLAG-tagged mu-type opioid receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by liquid scintillation counting analysis
Agonist activity at FLAG-tagged mu-type opioid receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by liquid scintillation counting analysis
[PMID: 23477419]
HEK293 EC50
3.04 nM
Compound: DAMGO
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
3.18 nM
Compound: DAMGO
Agonist activity at human MOR expressed in HEK293 cell membrane assessed as inhibition of forskolin-induced cAMP accumulation by by liquid scintillation counting
Agonist activity at human MOR expressed in HEK293 cell membrane assessed as inhibition of forskolin-induced cAMP accumulation by by liquid scintillation counting
[PMID: 21978284]
HEK293 EC50
378 nM
Compound: DAMGO
Agonist activity at GFP-fused mu opioid receptor (unknown origin) expressed in HEK293 cells assessed as recruitment of beta-arrestin-2 after 10 mins by BRET assay
Agonist activity at GFP-fused mu opioid receptor (unknown origin) expressed in HEK293 cells assessed as recruitment of beta-arrestin-2 after 10 mins by BRET assay
[PMID: 24613457]
HEK293 IC50
4.3 x 10-10 M
Compound: DAMGO
Displacement of [3H]DAMGO from human recombinant mu-opioid receptor expressed in HEK293 cells measured after 120 mins by scintillation counting method
Displacement of [3H]DAMGO from human recombinant mu-opioid receptor expressed in HEK293 cells measured after 120 mins by scintillation counting method
[PMID: 27876250]
HEK293-A EC50
1 nM
Compound: DAMGO
Activation of human mu opioid receptor expressed in HEK293a cells by [35S]GTP-gamma-S binding assay
Activation of human mu opioid receptor expressed in HEK293a cells by [35S]GTP-gamma-S binding assay
[PMID: 17616524]
体外研究
(In Vitro)

DAMGO (1-10 μM) 显著减少 CXCL12 激活的神经元 Akt 和 ERK1/2 活性并抑制其促进的神经元存活,但不下调 CXCR4 蛋白表达; (1 μM) 有效抑制前列腺素 E2 (PGE2) 诱导的 TTX 抗性电压门控钠电流增加[2]. [3].

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

体内研究
(In Vivo)

DAMGO(iv, 0.5-2 mg/kg)可对体重200-225 g的雄性Sprague-Dawley大鼠受伤的足爪产生明显的抗损伤作用,且呈剂量依赖性,产生有效且持久的镇痛作用[4][1234]

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

分子量

513.59

Formula

C26H35N5O6

CAS 号
性状

固体

颜色

White to off-white

Sequence

Tyr-{d-Ala}-Gly-{Me-Phe}-Gly-ol

Sequence Shortening

Y-{d-Ala}-G-{Me-Phe}-G-ol

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Sealed storage, away from moisture and light

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)

溶解性数据
细胞实验: 

H2O 中的溶解度 : ≥ 100 mg/mL (194.71 mM)

DMSO 中的溶解度 : 33.33 mg/mL (64.90 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.9471 mL 9.7354 mL 19.4708 mL
5 mM 0.3894 mL 1.9471 mL 3.8942 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 and light)。-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:

请根据您的 实验动物和给药方式 选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用
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: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (4.87 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

    生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
  • 方案 二

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (4.87 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中,混合均匀。

    2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。
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: 99.90%

参考文献
Cell Assay
[2]

Neurons (9 days in vitro) are treated with DAMGO (10 μM) for 24 h in their original culture dish, subsequently transferred to a dish containing Mg2+-free saline with glycine (15 μM), and exposed to NMDA (100 μM) and/or CXCL12 (20 nM) in absence of glia. After treatments, neurons are moved back into the original culture dishes containing glia. Neuronal death is evaluated after 24 h. Hoechst 33342 (3 μg/mL) combined with cleaved caspase-3 (1:100) staining is used to identify normal and apoptotic cells[2].

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

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 and light)。-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
DMSO / H2O 1 mM 1.9471 mL 9.7354 mL 19.4708 mL 48.6770 mL
5 mM 0.3894 mL 1.9471 mL 3.8942 mL 9.7354 mL
10 mM 0.1947 mL 0.9735 mL 1.9471 mL 4.8677 mL
15 mM 0.1298 mL 0.6490 mL 1.2981 mL 3.2451 mL
20 mM 0.0974 mL 0.4868 mL 0.9735 mL 2.4338 mL
25 mM 0.0779 mL 0.3894 mL 0.7788 mL 1.9471 mL
30 mM 0.0649 mL 0.3245 mL 0.6490 mL 1.6226 mL
40 mM 0.0487 mL 0.2434 mL 0.4868 mL 1.2169 mL
50 mM 0.0389 mL 0.1947 mL 0.3894 mL 0.9735 mL
60 mM 0.0325 mL 0.1623 mL 0.3245 mL 0.8113 mL
H2O 80 mM 0.0243 mL 0.1217 mL 0.2434 mL 0.6085 mL
100 mM 0.0195 mL 0.0974 mL 0.1947 mL 0.4868 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:
DAMGO
目录号:
HY-P0210
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