Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
TP1071 |
Nociceptin
Orphanin FQ,孤菲肽 |
Opioid Receptor | Endocrinology/Hormones; GPCR/G Protein; Neuroscience |
Nociceptin (Orphanin FQ) 是一种 17 个氨基酸的多肽,是 nociceptin 受体的内源性配体,具有缓解疼痛的作用。 | |||
T23076L |
Nociceptin (1-7) acetate
|
Opioid Receptor | Endocrinology/Hormones; GPCR/G Protein; Neuroscience |
Nociceptin (1-7) acetate 是一种有效的阿片受体样受体 1 (ORL1) 受体激动剂。 Nociceptin (1-7) 与 nociceptin 结合可降低痛觉过敏并具有镇痛活性。 | |||
TP1793L |
Nociceptin (1-13) amide TFA
|
Opioid Receptor | Endocrinology/Hormones; GPCR/G Protein; Neuroscience |
Nociceptin (1-13) amide TFA (178064-02-3 free base) 是一种有效的 Opioid receptor-like1 (ORL1) receptor 激动剂,对小鼠输精管的 pEC50 为 7.9,与大鼠前脑膜结合的 Ki 为 0.75 nM。 | |||
TP1885L1 |
[(pF)Phe4]Nociceptin(1-13)NH2 acetate
|
Opioid Receptor | Endocrinology/Hormones; GPCR/G Protein; Neuroscience |
[(pF)Phe4]Nociceptin(1-13)NH2 acetate 是一种选择性 NOP 受体激动剂,pKi 为 10.68,pEC50 为 9.31。 [(pF)Phe4]Nociceptin(1-13)NH2 acetate 对 δ、κ 和 μ 阿片受体具有高选择性(>3000 倍)。 | |||
T23076 |
Nociceptin(1-7)
Nociceptin (1-7) |
Others | Others |
Bioactive metabolite of nociceptin, antagonist of nociceptin-induced hyperalgesia | |||
TP1986 |
[Arg14,Lys15]Nociceptin
|
||
Highly potent and selective NOP receptor agonist (EC50 = 1 nM). Displays > 875-fold selectivity over opioid receptors (IC50 values are 0.32, 280, > 10000 and 1500 for NOP, μ, δ and κ receptors respectively). Longer lasting and 30-fold more potent than noc | |||
TP1793 |
Nociceptin (1-13), amide
|
Opioid Receptor | Endocrinology/Hormones; GPCR/G Protein; Neuroscience |
Nociceptin (1-13), amide 是一种 ORL1 (OP4) 受体激动剂,与大鼠前脑膜结合的 Ki 为 0.75 nM,对小鼠输精管的 pEC50 为 7.9。 | |||
TP1987 |
[Nphe1]Nociceptin(1-13)NH2
|
||
Selective and competitive nociceptin receptor antagonist, devoid of any agonist activity. Binds selectively to recombinant nociceptin receptors (pKi = 8.4), and competitively antagonizes the actions of nociceptin in vitro and in vivo. | |||
TP1885 |
[(pF)Phe4]Nociceptin(1-13)NH2
|
||
Highly potent and selective nociceptin/orphanin FQ receptor (OP4) agonist peptide (pKi = 10.68; pEC50 = 9.80). Displays > 8000-fold selectivity over δ, κ, and μ opioid receptors and has relatively long lasting pronociceptive, hypotensive, negative inotrop | |||
TP1988 |
[Phe1Ψ(CH2-NH)Gly2]Nociceptin(1-13)NH2
|
||
Potent agonist of the nociceptin (ORL1) receptor, demonstrated both in vitro and in vivo. Selective, competitive antagonism at the nociceptin receptor has also been reported (pA2 = 7.02 and 6.75 in the guinea pig ileum and mouse vas deferens respectively) | |||
T75908 |
Nociceptin(1-7) TFA
|
||
Nociceptin(1-7) 是 Nociceptin 的 N 端生物活性片段。Nociceptin(1-7) 是一种有效的ORL1(NOP)受体激动剂,具有缓解疼痛活性。Nociceptin(1-7) 联合 Nociceptin 可降低体内对痛觉的敏感。 | |||
T75896 |
[Arg14,Lys15]Nociceptin TFA
|
||
[Arg14,Lys15]Nociceptin TFA 是一种高效、选择性的 NOP (ORL1; OP4)受体激动剂,EC50为 1 nM。[Arg14,Lys15]Nociceptin TFA 对阿片受体具有较高的选择性,对 NOP、μ、δ 和 κ 受体的 IC50值分别为 0.32、280、>10000 和 1500 nM。 | |||
T75909 |
[Nphe1]Nociceptin(1-13)NH2 TFA
|
||
[Nphe1]Nociceptin(1-13) NH2 TFA 是一种 Nociceptin/orphanin FQ (NC)内源性配体,是一种选择性和竞争性的 ociceptin receptor 拮抗剂,不具有激动剂活性。[Nphe1]nociceptin(1-13)NH2 选择性结合重组 nociceptin 受体(pKi=8.4),拮抗 nociceptin 对 CHO 细胞中 cAMP 积累的抑制作用(pA2=6.0)。[Nphe1]Nociceptin(1-13)NH2 有可能作为一种止痛试剂。 | |||
T75906 |
Nociceptin (1-13), amide TFA
|
||
Nociceptin (1-13), amide TFA 是一种有效的阿片受体 ORL1 (OP4)受体激动剂,对小鼠输精管 pEC50值为 7.9,与大鼠前脑膜结合的 Ki 值为 0.75 nM。 | |||
T2071 |
MCOPPB triHydrochloride
MCOPPB trihydrochlride,MCOPPB 3HCl |
Opioid Receptor | Endocrinology/Hormones; GPCR/G Protein; Neuroscience |
MCOPPB triHydrochloride (MCOPPB 3HCl) 是一种伤害感受肽受体激动剂,pKi 为10.07。 | |||
TP1940L1 |
Ac-RYYRIK-NH2 acetate
|
Opioid Receptor | Endocrinology/Hormones; GPCR/G Protein; Neuroscience |
Ac-RYYRIK-NH2 acetate 是 nociceptin/orphanin FQ(noc/OFQ) 受体的激动剂,影响自发运动活动。 它是转染在 CHO 细胞中的 ORL1 的部分激动剂,可拮抗大鼠脑膜和切片中 noc/OFQ 对 [35S]-GTPgammaS 与 G 蛋白结合的刺激。 | |||
T28728 |
SCH-486757
SCH 486757,SCH486757 |
Opioid Receptor | Endocrinology/Hormones; GPCR/G Protein; Neuroscience |
SCH-486757是一种伤害感受素-1(NOP1)和孤儿素 FQ 肽受体激动剂,可用于研究咳嗽。 | |||
TP1941L1 |
Ac-RYYRWK-NH2 acetate
|
Opioid Receptor | Endocrinology/Hormones; GPCR/G Protein; Neuroscience |
Ac-RYYRWK-NH2 acetate 是一种有效的伤害感受素受体 (NOP) 的部分激动剂,它是内源性 ORL1 受体激动剂。 | |||
T15799 |
LY2940094
LY-2940094 |
Opioid Receptor | Endocrinology/Hormones; GPCR/G Protein; Neuroscience |
LY2940094 (LY-2940094) 是一种口服有效的选择性 NOP 受体拮抗剂,可降低动物模型的自身给药酒精依赖,对 NOP 受体具有高亲和力,Ki 为 0.105 nM,和拮抗活力,Kb 为 0.166 nM。 | |||
TP1882L1 |
Orphanin FQ(1-11) acetate(178249-41-7 free base)
|
Opioid Receptor | Endocrinology/Hormones; GPCR/G Protein; Neuroscience |
Orphanin FQ(1-11) acetate(178249-41-7 free base) 含有 Nociceptin 氨基酸 1-11 的肽片段。 ORL1/KOR-3 受体的强效激动剂 (Ki = 55 nM);对阿片受体无亲和力,包括 μ、δ、κ1 和 κ3 受体 (Ki >1000 nM)。在 CD-1 小鼠中显示镇痛特性。 | |||
T23475 |
Trap-101 hydrochloride
Trap 101 |
Others | Others |
nociceptin/orphanin FQ (NOP) receptor antagonist | |||
T21999 | (±)-J 113397 | ||
(±)-J-113397 是一种有效的、高选择性的非肽基ORL1 受体拮抗剂,对人克隆 ORL1 的Ki 为 1.8 nM。在体外,J-113397 抑制 nociceptin/orphanin FQ 刺激的GTPγS 与表达 ORL1 的 CHO 细胞结合,IC50值为 5.3 nM。J-113397 可用于研究 nociceptin/orphanin FQ 的生理作用。 | |||
T24831 |
SR8993
SR 8993,SR-8993 |
||
SR8993 is a highly selective, brain-penetrant agonist of the nociceptin receptor. | |||
T76420 |
Nocistatin
|
||
Nocistatin 是一种神经肽,是孤儿类阿片受体的内源性配体。 Nocistatin 还是神经肽伤害感受肽或孤啡肽 FQ (Noc/OFQ) 的功能性拮抗剂。Nocistatin 通过 Gi/o 蛋白介导途径抑制 5-HT 释放。Nocistatin 阻断 Nociceptin 诱导的异常性疼痛和痛觉过敏。 | |||
T27939 |
LY2940094 tartrate
LY2940094,LY 2940094,LY-2940094 tartrate,LY-2940094 |
||
LY-2940094, a nociceptin receptor antagonist, is used potentially for the treatment of major depressive disorder and alcoholism. | |||
TP2277 |
Nocistatin(human)
Nocistatin (human) |
Others | Others |
Blocker of nociceptin-induced allodynia and hyperalgesia | |||
TP2276 |
Nocistatin (bovine)
|
Others | Others |
endogenous peptide used to block nociceptin-induced allodynia and hyperalgesia | |||
T12120 |
MT-7716 hydrochloride
W-212393 hydrochloride |
Others | Others |
MT-7716 hydrochloride is a selective agonist of non-peptide nociceptin receptor (NOP) | |||
T40510 |
Ac-RYYRWK-NH2 TFA
Ac-RYYRWK-NH2 TFA |
||
Ac-RYYRWK-NH2 is a highly effective and specific partial agonist for the nociceptin receptor (NOP). It demonstrates a remarkable affinity for rat cortical membranes ORL1, with [3H]Ac-RYYRWK-NH2 exhibiting a Kd value of 0.071 nM. However, it shows negligible affinity towards μ-, κ-, or δ-opioid receptors. | |||
T83685 |
UFP101 TFA
|
||
UFP101是一种合成肽类物质,作为nociceptin受体的拮抗剂(Ki为0.06 nM,测试于表达人类受体的CHO细胞中)。它对nociceptin受体的选择性高于κ-opioid受体(Ki为204 nM,测试于表达大鼠受体的CHO细胞中)。UFP101能抑制表达于CHO细胞膜的nociceptin受体释放GTPγS(EC50为1.86 nM)。通过脑室内给药,UFP101(10 nmol/每只动物)能延长小鼠尾巴甩动试验中的尾巴撤回潜伏期。在由盲肠结扎和穿刺诱发的小鼠败血症模型中,UFP101(0.003、0.03及0.3 mg/kg)能提高生存率。 | |||
T12120L |
MT-7716 free base
W-212393 |
Others | Others |
MT-7716 free base is a selective non-peptide agonist of nociceptin receptor (NOP). It is used for promising potential treatment drugs for alcohol abuse and relapse prevention. | |||
T26918 |
BU08028
BU 08028,BU-08028 |
||
BU08028 is a mu opioid peptide (MOP) receptor and nociceptin-orphanin FQ peptide (NOP) receptor agonist. | |||
TP1940 |
Ac-RYYRIK-NH2
|
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High affinity ligand for the NOP site (Ki = 1.5 nM). Antagonizes nociceptin-stimulated GTP binding in rat brain and the chronotropic effect of nociceptin on rat cardiomyocytes. However, displays potent agonist properties in vivo, inhibiting locomotor acti | |||
TP2105 |
UFP-101
|
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Potent, selective and competitive silent antagonist for the NOP opioid receptor. Binds to NOP with high affinity (pKi = 10.24) and displays > 3000-fold selectivity over δ, μ and κ opioid receptors. Antinociceptive and opposes the action of nociceptin in v | |||
T81658 |
Nocistatin(human) TFA
|
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Nocistatin (human) TFA 可以抑制因疼痛刺激而引发的痛觉过敏与异常,并可减轻由前列腺素prostaglandin E2所致的疼痛。 | |||
T26673 |
AT-076
AT 076 |
||
AT-076 is a noncompetitive antagonist of the κ-opioid receptor (Ki = 1.14 nM) and nociceptin receptor (Ki = 1.75 nM) and a competitive antagonist of the μ-opioid receptor (Ki = 1.67 nM) and δ-opioid receptor (Ki = 19.6 nM). | |||
T21345 | MCOPPB | ||
MCOPPB is a potent and selective agonist for the nociceptin receptor with a pKi of 10.07, much weaker activity at other opioid receptors. In animal studies, MCOPPB produces potent anxiolytic effects, with no inhibition of motor or memory function, and onl | |||
T62805 | SB-612111 hydrochloride | ||
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。 | |||
T36376 | SB-612111 | ||
SB-612111 is a novel and potent human opiate receptor-like orphan receptor (ORL-1) antagonist with a high affinity for hORL-1 (Ki=0.33 nM). SB-612111 exhibits selectivity for μ-, κ- and δ-receptors with Ki values of 57.6 nM, 160.5 nM and 2109 nM, respecticely. SB-612111 effectively antagonizes the pronociceptive action of Nociceptin in an acute pain model[1]. [1]. Paola F Zaratin, et al. Modification of Nociception and Morphine Tolerance by the Selective Opiate Receptor-Like Orphan Receptor Anta... | |||
TP1882 |
Orphanin FQ(1-11)
Orphanin FQ (1-11) |
||
Orphanin FQ(1-11) is a peptide fragment containing amino acids 1-11 of Nociceptin. Orphanin FQ(1-11) is a potent agonist of the ORL1/KOR-3 receptor (Ki = 55 nM) and displays no affinity for opioid receptors, including μ, δ, κ1 and κ3 receptors (Ki >1000 nM). Orphanin FQ(1-11) displays analgesic properties in CD-1 mice. | |||
T75897 |
Orphanin FQ(1-11) TFA
|
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Orphanin FQ(1-11) TFA 是孤儿蛋白 FQ 或 nociceptin (OFQ/N) 片段,是一种有效的NOP 受体 (ORL-1; OP4) 激动剂,Ki 为 55 nM。Orphanin FQ(1-11) TFA 对 μ,δ,κ1 和 κ3 受体没有亲和力 (Ki>1000 nM)。Orphanin FQ(1-11) TFA 在 CD-1 小鼠中具有缓解疼痛作用。 | |||
T75907 |
Ac-RYYRIK-NH2 TFA
|
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Ac-RYYRIK-NH2 TFA 作为高效的ORL1部分激动剂,充当ORL1的内源性配体,在CHO细胞中表现出较低的解离常数(Kd=1.5 nM)。该化合物以特异性方式激活G蛋白,作为竞争性拮抗剂,抑制noc/OFQ对大鼠脑膜和脑切片上 [35S]-GTPγS 结合G蛋白的作用。 | |||
T83709 |
LIH383 TFA
Phe-Gly-Gly-Phe-Met-Arg-Arg-Lys-NH2 |
||
LIH383是一种趋化因子(C-X-C motif) 受体7 (CXCR7)的多肽激动剂,属于趋化因子和阿片肽清除受体。它专一性激活CXCR7 (EC50 = 0.61 nM),在3 µM浓度时,相比μ-、δ-、κ-阿片受体以及诺氨酸阿片肽(NOP)受体的β-arrestin招募实验中表现出高选择性。LIH383(3 µM)通过阻止U87-ACKR3细胞中,由非选择性阿片受体激动剂dynorphin A诱导的CXCR7对阿片肽的摄取,发挥作用。 |