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Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T7748 |
Dermorphin TFA
皮啡肽三氟乙酸盐 |
Others; Opioid Receptor | Endocrinology/Hormones; GPCR/G Protein; Neuroscience; Others |
Dermorphin TFA 是在两栖类皮肤中发现的天然七肽,是 μ-阿片受体激动剂,可用于抑制神经痛。 | |||
T62767 |
Mu opioid receptor antagonist 3
|
Others | Others |
Mu opioid receptor antagonist 3 (compound 26) 是一种有效的、选择性的、能透过血脑屏障渗透性的μ 阿片受体 (MOR) 拮抗剂 (Ki: 0.24 nM, EC50: 0.54 nM)。Mu opioid receptor antagonist 2 对吗啡表现出明显的中枢神经系统拮抗活性,诱发戒断症状比 Naloxone 小。Mu opioid receptor antagonist 2 能够用于研究阿片类药物使用障碍 (OUD)。 | |||
T7404 |
Dermorphin
皮啡肽 |
Opioid Receptor | Endocrinology/Hormones; GPCR/G Protein; Neuroscience |
Dermorphin 是在两栖类皮肤中发现的天然七肽,是 μ-阿片受体激动剂,可用于抑制神经痛。 | |||
T62766 |
Mu opioid receptor antagonist 2
|
Others | Others |
Mu opioid receptor antagonist 2 (compound 25) 是一种有效的、选择性的、能透过血脑屏障渗透性的μ 阿片受体 (MOR) 拮抗剂 (Ki: 0.37 nM, EC50: 0.44 nM)。Mu opioid receptor antagonist 2 对吗啡表现出明显的中枢神经系统拮抗活性,诱发戒断症状比 Naloxone 小。Mu opioid receptor antagonist 2 能够用于研究阿片类药物使用障碍 (OUD)。 | |||
T62768 |
Mu opioid receptor antagonist 4
|
Others | Others |
Mu opioid receptor antagonist 4 (compound 31) 是一种有效的、选择性的、能透过血脑屏障渗透性的μ 阿片受体 (MOR) 拮抗剂 (Ki: 0.38 nM, EC50: 0.38 nM)。Mu opioid receptor antagonist 2 对吗啡表现出明显的中枢神经系统拮抗活性,诱发戒断症状比 Naloxone 小。Mu opioid receptor antagonist 2 能够用于研究阿片类药物使用障碍 (OUD)。 | |||
T79431 |
Mu opioid receptor antagonist 7
|
Opioid Receptor | Endocrinology/Hormones; GPCR/G Protein; Neuroscience |
Muopioid receptorantagonist 7 (compound 24) 是一种有效的CNS渗透性μOR (μ-阿片受体)拮抗剂,具有29 ± 3.0 nM的IC50。该化合物可用于研究疼痛和阿片类药物使用障碍。 | |||
T62673 |
Mu opioid receptor antagonist 5
|
Others | Others |
Mu opioid receptor antagonist 5 (compound NAP) 是一种选择性的、能够透过血脑屏障的 μ 阿片受体 (MOR) 拮抗剂 (EC50: 1.14 nM, Ki: 0.37 nM)。Mu opioid receptor antagonist 5 能够用于研究阿片类药物使用障碍 (OUD)。 | |||
T1242 |
Alvimopan
爱维莫潘 |
Opioid Receptor | Endocrinology/Hormones; GPCR/G Protein; Neuroscience |
Alvimopan (LY 246736) 是一种选择性和竞争性 μ 阿片受体拮抗剂,IC50值为 1.7 nM。它存在于肌间和黏膜下神经元以及人体肠道固有层的免疫细胞中,可用于术后肠梗阻的研究。 | |||
T27667 |
JNJ-20788560
JNJ 20788560 |
Opioid Receptor | Endocrinology/Hormones; GPCR/G Protein; Neuroscience |
JNJ-20788560 是一种δ阿片受体(DOR)激动剂,具有镇痛活性。它对 DOR 的选择性高于μ阿片受体(MOR)。 | |||
T1197 |
Trimebutine maleate
Debridat,Polibutin,马来酸曲美布汀 |
Calcium Channel; Opioid Receptor | Endocrinology/Hormones; GPCR/G Protein; Membrane transporter/Ion channel; Metabolism; Neuroscience |
Trimebutine maleate (Polibutin) 是一种外周 μ、δ 和 kappa 阿片受体激动剂,用作治疗慢性和急性腹痛的解痉药物。 | |||
T31081 |
CP-866087
CP 866087,UNII-MDH21334PI,CP-866,087,CP866087 |
Opioid Receptor | Endocrinology/Hormones; GPCR/G Protein; Neuroscience |
CP-866087 是一种新型、有效和选择性的μ阿片受体拮抗剂,用于研究女性性功能障碍。 | |||
T4407 |
SR17018
|
Opioid Receptor | Endocrinology/Hormones; GPCR/G Protein; Neuroscience |
SR17018 是一种 μ-阿片受体 (MOR) 激动剂,与 GTPγS 结合,EC50 为 97 nM。 | |||
T50091 |
1-(8-carbamimidamidooctyl)guanidine 2HCl
1,1'-(Octane-1,8-diyl)diguanidine 2HCl,1-(8-carbamimidamidooctyl)guanidine dihydrochloride |
Others | Others |
1,1'-(Octane-1,8-diyl)diguanidine dihydrochloride 是一种合成的阿片肽,来源于天然阿片肽脑啡肽。它是μ-阿片受体(MOR)的高效激动剂,Ki 为0.14 nM,是一种有效的MOR 激动剂。 | |||
T0102 |
Naloxone hydrochloride
盐酸纳洛酮,Naloxone HCl |
Opioid Receptor | Endocrinology/Hormones; GPCR/G Protein; Neuroscience |
Naloxone hydrochloride (Naloxone HCl) 是一种特异性、没有激动剂活性的opiate 拮抗剂。它是 mu、delta 和 kappa 阿片受体的竞争性拮抗剂。 | |||
T4411 |
DAMGO TFA (78123-71-4(Free base))
|
Opioid Receptor | Endocrinology/Hormones; GPCR/G Protein; Neuroscience |
DAMGO TFA (78123-71-4(Free base)) 是Mu-opioid 受体的强效选择性激动剂。它也是镇痛药。它刺激钙激活的腺苷酸环化酶相关 cAMP 的产生。通过 TGF-beta1 表达趋化因子和趋化因子受体。增加老鼠的食物摄入量。 | |||
T39529 |
AT-121 hydrochloride
|
Opioid Receptor | Endocrinology/Hormones; GPCR/G Protein; Neuroscience |
AT-121 hydrochloride 是一种 nociception 和 mu 阿片受体 (mu opioid receptor)的双重激动剂,Ki 值分别为 3.67 和 16.49 nM。AT-121 hydrochloride 是一种安全、无成瘾性且科缓解疼痛的化合物,具有抗伤害和止痛活性。 | |||
T10593 |
BPR1M97
|
Opioid Receptor | Endocrinology/Hormones; GPCR/G Protein; Neuroscience |
BPR1M97 是一种具有血脑屏障渗透性和有效性的 mu 阿片受体(MOP)和神经肽-啡肽 FQ(NOP)受体激动剂,对 MOP 的 Kis 值为1.8 nM,对 NOP 的Kis 值为 4.2 nM。BPR1M97 具有抗伤害作用和抗痛觉作用。 | |||
T7211 |
Tyr-Gly-Gly-Phe-Met-OH
Methionine enkephalin,蛋氨酸脑啡肽,Met-Enkephalin,[MET5]脑啡肽 |
Opioid Receptor | Endocrinology/Hormones; GPCR/G Protein; Neuroscience |
Tyr-Gly-Gly-Phe-Met-OH (Met-Enkephalin) 是天然存在的内源性阿片肽、metenkephalin 和 zeta-和 delta-阿片受体激动剂的合成形式,是 mu-阿片受体激动剂,具有潜在的镇痛、神经调节、免疫调节、抗炎、抗肿瘤作用以及镇痛、抗抑郁和胃肠运动调节活性。 | |||
T0918 |
Trimebutine
曲美布汀,Mebutin |
Opioid Receptor | Endocrinology/Hormones; GPCR/G Protein; Neuroscience |
Trimebutine (Mebutin) 是阿片受体激动剂,有抗毒蕈碱活性。它是解痉剂,可调节肠道和结肠运动,并通过抗毒蕈碱和弱μ-阿片受体激动剂作用缓解腹痛。 | |||
T7306 |
Valorphin
Valorphin TFAsalt |
Opioid Receptor | Endocrinology/Hormones; GPCR/G Protein; Neuroscience |
Valorphin (Valorphin TFAsalt) 是内源性血红蛋白 β 链第 33-39 位氨基酸残基,具有阿片类镇痛活性,与大鼠 mu-阿片受体结合,IC50 为 14 nM。它有抗肿瘤活性,也可用于缓解疼痛的研究。 | |||
T25194 |
BW 443C
BW443C,BW-443C,Tyr-arg-gly-(4-nitro-phe)-pro-NH2 |
Others | Others |
BW 443C is a selective agonist of mu-opioid receptor. | |||
T26918 |
BU08028
BU 08028,BU-08028 |
Others | Others |
BU08028 is a mu opioid peptide (MOP) receptor and nociceptin-orphanin FQ peptide (NOP) receptor agonist. | |||
T71189 |
RX 809055AX
|
Others | Others |
RX 809055AX is a long lasting opioid antagonist at mu and delta receptors. | |||
T70730 |
Oxycodegol phosphate
|
Others | Others |
Oxycodegol phosphate is a mu-opioid agonist used in the treatment of Moderate to Severe Chronic Low Back Pain | |||
T60415 |
DS34942424
|
Others | Others |
DS34942424 是一种没有μ 阿片受体激动剂活性的口服强效镇痛剂。 | |||
T1242L |
Alvimopan monohydrate
|
Others | Others |
Alvimopan monohydrate is a mu-opioid receptor antagonist that intended for the treatment of constipation in patients who take opiates for pain. | |||
T69121 |
Oxpheneridine
|
Others | Others |
Oxpheneridine is a mu opioid receptor agonist that possesses the spasmolytic activity and acts as a narcotic analgesic. | |||
T10926L |
CYT-1010 hydrochloride
|
Others | Others |
CYT-1010 hydrochloride is an mu-opioid receptor agonist. The EC50 for β-arrestin recruitment and cAMP production inhibition were 13.1 nM and 0.0053 nM, respectively. | |||
T71225 |
Oxicodegol HCl
|
Others | Others |
Oxicodegol HCl is a mu-opioid agonist used in the treatment of Moderate to Severe Chronic Low Back Pain | |||
T71224 |
Oxicodegol trifluoroacetate
|
Others | Others |
Oxicodegol trifluoroacetate is a mu-opioid agonist used in the treatment of Moderate to Severe Chronic Low Back Pain | |||
T10926 | CYT-1010 | Others | Others |
CYT-1010 is an mu-opioid receptor agonist. The EC50 for the inhibition of β-arrestin recruitment and cAMP production is 13.1 nM and 0.0053 nM, respectively. | |||
T62722 |
SC13
|
Others | Others |
SC13 是一种新型的 mitragynine 类似物,具有低效Muopioid receptor 激动作用,具有麻醉作用和较轻的不良反应。 | |||
T27027 |
CJ-15208
CJ15,208,CJ-15,208,CJ 15,208.c[Phe-D-Pro-Phe-Trp] |
Others | Others |
CJ-15208 is a potent and selective κ-opioid receptor antagonist from a fungus, Ctenomyces serratus ATCC15502 (IC50 are 47 nM for kappa, 260 nM for mu, and 2,600 nM for delta respectly). In the electrically-stimulated twitch response assay of rabbit vas de | |||
T40845 |
Methylnaltrexone iodide
Naltrexonium methiodide,碘化甲基纳曲酮; 碘甲纳曲酮 |
Others | Others |
Methylnaltrexone iodide, a quaternary derivative of Naltrexone, is an orally active and selective antagonist of the mu-opioid receptor. It acts peripherally in the gastrointestinal tract to antagonize the receptor. Furthermore, Methylnaltrexone iodide exhibits limited permeability across the blood-brain barrier. | |||
T75916 |
Dynorphin A TFA
|
||
Dynorphin A TFA, 作为一种内源性阿片肽,主要在中枢神经系统(CNS)中发挥抑制性神经传导的作用。该化合物不仅是kappa阿片受体(KOR)的高效激动剂,还能激活其他阿片受体,包括mu(MOR)和delta(DOR)。Dynorphin A TFA具有诱导神经元死亡的能力,因此在神经系统疾病的研究中具有应用价值。 | |||
T27934 |
LY255582
LY-255582,LY 255582 |
Opioid Receptor | Endocrinology/Hormones; GPCR/G Protein; Neuroscience |
LY255582 是一种具有选择性的中枢活性阿片受体拮抗剂,对 mu、delta 和 kappa 受体具有高亲和力 ,Ki 分别为 0.4 nM、5.2、2.0 nM。LY255582 可以抑制饮食相关的中脑边缘多巴胺水平的增加,并减少食物摄入的消耗。LY255582 常用于对肥胖的研究。LY255582是用于阿片受体介导的细胞信号传导研究的潜在化合物。 | |||
T78778 |
D3R/MOR antagonist 1
|
Dopamine Receptor | GPCR/G Protein; Neuroscience |
D3R/MOR antagonist 1 (Compound 114) 为D3R/MOR拮抗剂,其对D3R和MOR的Ki值分别为46.5 nM和691 nM。该化合物通过MOR的部分激动作用可能具有镇痛效果,同时通过D3R的拮抗作用有助于降低阿片类药物的滥用风险。 | |||
T36722 |
Deltorphin II (trifluoroacetate salt)
|
Others | Others |
Deltorphin II is a peptide agonist of δ2-opioid receptors.1,2It is selective for δ-opioid receptors over μ- and κ-opioid receptors in radioligand bindings assays (Kis = 0.0033, >1, and >1 μM, respectively) and induces [35S]GTPγS binding in mouse brain membrane preparations (EC50= 0.034 μM). Deltorphin II (0.12 mg/kg) decreases the infarction zone:risk zone ratio in a rat model of myocardial ischemia-reperfusion injury induced by coronary occlusion, an effect that can be reversed by the δ2-opioid... | |||
T62805 |
SB-612111 hydrochloride
|
Others | Others |
SB-612111 hydrochloride 是一种高效的、新型的阿片受体孤儿受体 (ORL-1) 拮抗剂,对 hORL-1 具有较高的亲和力,Ki 值为 0.33 nM。SB-612111 hydrochloride 能够作用于 μ-receptor (Ki: 57.6 nM),κ-receptor (Ki: 160.5 nM) 和 δ-receptor (Ki: 2109 nM)。SB-612111 hydrochloride 能有效拮抗 Nociceptin 在急性疼痛模型中的造成的痛觉作用。 |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
TN3367 |
Akuammidine
|
Opioid Receptor | Endocrinology/Hormones; GPCR/G Protein; Neuroscience |
Akuammidine shows anti-inflammatory and anti-asthmatic properties, it has opioid analgesic activity, it shows a preference for mu-opioid binding sites with Ki values of 0.6, 2.4 and 8.6 microM at mu-, delta- and kappa-opioid binding sites, respectively. | |||
TN3368 |
Akuammigine
|
Opioid Receptor; Adrenergic Receptor | Endocrinology/Hormones; GPCR/G Protein; Neuroscience |
Akuammigine has in vitro antimalarial activity. Akuammigine competitively antagonizes the effect of noradrenaline on postsynaptic alpha-adrenoceptors, yielding pA2 values of 4.68. Akuammidine also shows a preference for mu-opioid binding sites with Ki val |
Cat. No. | Product Name | Species | Expression System |
---|---|---|---|
TMPH-01719 |
OPRM1 Protein, Human, Recombinant (His)
Mu opioid receptor,OPRM1,Mu opiat... |
Human | E. coli |
OPRM1 Protein, Human, Recombinant (His) is expressed in E. coli expression system with N-10xHis tag. The predicted molecular weight is 47.6 kDa and the accession number is P35372. | |||
TMPJ-00513 |
LTF Protein, Human, Recombinant (His)
Lactoferroxin-A,Talalactoferrin,LTF,Lactotransferrin,Lactofe... |
Human | HEK293 Cells |
Lactotransferrin is a member of the transferrin family that transfer iron to the cells and control the level of free iron in the blood and external secretions. Lactotransferrin is a secreted protein and contains two transferrin-like domains. Lactotransferrin can be cleaved into the following four chains: Kaliocin-1, Lactoferroxin-A, Lactoferroxin-B, and Lactoferroxin-C. Lactoferroxin A, Lactoferroxin B, and Lactoferroxin C have opioid antagonist activity. Lactoferroxin A shows preference for mu-... | |||
TMPH-02020 |
RGS17 Protein, Human, Recombinant (GST)
Regulator of G-protein signaling 17,RGS17 |
Human | E. coli |
Regulates G protein-coupled receptor signaling cascades, including signaling via muscarinic acetylcholine receptor CHRM2 and dopamine receptor DRD2. Inhibits signal transduction by increasing the GTPase activity of G protein alpha subunits, thereby driving them into their inactive GDP-bound form. Binds selectively to GNAZ and GNAI2 subunits, accelerates their GTPase activity and regulates their signaling activities. Negatively regulates mu-opioid receptor-mediated activation of the G-proteins. R... |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
TMIJ-0213 |
Naloxone-d5 HCl
|
||
Naloxone-d5 HCl 是 Naloxone HCl 的氘代化合物。Naloxone HCl 的 CAS 号为 357-08-4。Naloxone hydrochloride 是一种特异性、没有激动剂活性的opiate拮抗剂。它是 mu、delta 和 kappa 阿片受体的竞争性拮抗剂。 |