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T21874
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CID 2745687
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GPR |
Endocrinology/Hormones;
GPCR/G Protein |
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CID 2745687 是可逆的、特异性 GPR35竞争性拮抗剂（Ki:12.8 nM）。 |
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TP1051L
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Protein Kinase C Peptide Substrate acetate
Protein Kinase C Peptide Substrate acetate(120253-69-2 free base)
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Others |
Others |
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Protein Kinase C Peptide Substrate acetate(120253-69-2 free base) 以依赖于第二信使和特定衔接蛋白的方式靶向特定细胞间隔物，以响应激活 g 蛋白偶联受体、酪氨酸激酶受体或酪氨酸激酶偶联受体的细胞外信号。 |
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T50088
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N-phenylthiophene-2-carboximidamide
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Others |
Others |
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N-phenylthiophene-2-carboximidamide 是一种噻吩衍生物，可以作为蛋白酪氨酸激酶（PTKs）的抑制剂和 G 蛋白偶联受体（GPCR）的配体发挥作用。 |
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TP1074L
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Neuropeptide FF acetate(99566-27-5 free base)
NPFF acetate
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Neuropeptide Y Receptor |
GPCR/G Protein;
Neuroscience |
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Neuropeptide FF acetate(99566-27-5 free base) (NPFF acetate) 是属于 RF 酰胺家族的八肽。 NPFF 与 G 蛋白偶联受体 NPFF (1) 和 NPFF (2) 相互作用。 |
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T9857L
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Vasopressin acetate
Vasopressin acetate (11000-17-2 Free base)
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Endogenous Metabolite |
Metabolism |
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Vasopressin acetate 是一种环状九肽，在下丘脑中枢合成。 Vasopressin acetate 作为一种神经递质，通过与特定的 G 蛋白偶联受体结合发挥其作用。 |
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T38807L
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[Lys8, Lys9]-Neurotensin (8-13) acetate
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Neurotensin Receptor |
GPCR/G Protein |
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[Lys8, Lys9]-Neurotensin (8-13) acetate 是一种神经降压素类似物，通过激活 G 蛋白偶联受体 NTS1 和 NTS2 发挥镇痛作用，hNTS1 和 hNTS2 受体的 Ki 值分别为 0.33 nM 和 0.95 nM。 |
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TP1914L1
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BAM (8-22) acetate
BAM (8-22) acetate(412961-36-5 free base)
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Others |
Others |
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BAM (8-22) acetate 是脑啡肽原 A 的蛋白水解产物。BAM (8-22) acetate 可激活 Mas 相关的 G 蛋白偶联受体 (Mrgprs)、MrgprC11 和 hMrgprX1，并以 Mrgpr 依赖性方式诱导小鼠抓挠。 |
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T38651
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Lauryl maltose neopentyl glycol
LMNG
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Lauryl maltose neopentyl glycol (LMNG) 是一种能溶解和稳定膜蛋白的洗涤剂。Lauryl maltose neopentyl glycol 能从膜上提取完整的膜蛋白，从而改善G 蛋白偶联受体和呼吸系统复合物等膜蛋白的稳定性。Lauryl maltose neopentyl glycol 具有增溶作用。 |
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T38287
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C3a Receptor Agonist
C3a receptor agonist 1,C3a受体激动剂,Complement 3a Receptor Agonist
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Complement System |
Immunology/Inflammation |
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C3a Receptor Agonist (C3a receptor agonist 1) 结合免疫系统补体途径中的G 蛋白偶联C3a 受体(C3aRs)。在肠缺血再灌注损伤模型中，C3aR 的激活可防止中性粒细胞动员。C3aRs 在成年小鼠的神经祖细胞和未成熟神经元上表达。C3a 在体外刺激神经祖细胞的分化。 |
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T9857
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Vasopressin
antidiuretic hormone (ADH),argipressin,arginine vasopressin (AVP)
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Endogenous Metabolite |
Metabolism |
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Vasopressin (argipressin) 是一种由下丘脑神经元合成的环状九肽，是肽原激素合成中的一种激素。Vasopressin 参与下丘脑-垂体-肾上腺轴调节过程，增加无溶质水从肾小管的滤液中重新吸收回循环中的量，收缩小动脉提高压强，增强促肾上腺皮质激素释放因子的刺激作用调节垂体促肾上腺皮质激素分泌。Vasopressin 在神经传导过程中可作为神经递质，与特定的 G 蛋白偶联受体结合发挥作用。 |
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TP1051
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Protein Kinase C Peptide Substrate
PRKCE,Peptide Epsilon,PKCε
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Protein Kinase C Peptide Substrate targets specific cell spacers ina manner that is dependent on second messengers and specific adaptor proteins in response to extracellular signals that activate g protein-coupled receptors, tyrosine Kinase receptors, or |
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T26200
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Somatostatin RC 102
Somatostatin RC102,Somatostatin-RC-102,Somatostatin RC-102
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Somatostatin RC 102 is a peptide hormone. It regulates the endocrine system and affects neurotransmission and cell proliferation via interaction with G protein-coupled somatostatin receptors and inhibition of the release of numerous secondary hormones. |
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T39165
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Treprostinil palmitil
Treprostinil palmitil,INS-1009
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Treprostinil Palmitil (TP), a prodrug of the DP1 and EP2 agonist Treprostinil (UT-15), exhibits EC50 values of 0.6 and 6.2 nM, respectively. It is a pure prodrug without any inherent binding affinity for G-protein coupled receptors, including prostanoid receptors. |
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T38807
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[Lys8, Lys9]-Neurotensin (8-13)
JMV438,[Lys8, Lys9]-Neurotensin (8-13)
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[Lys8, Lys9]-Neurotensin (8-13) (JMV438) is a Neurotensin analog that elicits analgesic effects by activating the G protein-coupled receptors NTS1 and NTS2. The compound has K i values of 0.33 nM and 0.95 nM for hNTS1 and hNTS2 receptors, respectively. |
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T80197
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Vasopressin Dimer (parallel) (TFA)
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Vasopressin Receptor |
GPCR/G Protein |
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Vasopressin Dimer (parallel) TFA为Vasopressin的平行二聚体，能够激活G蛋白偶联受体V1aR、V1bR、V2R及OTR四种。 |
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T39976
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MS67
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MS67 is a potent and selective degrader of the WD40 repeat domain protein 5 (WDR5) with a dissociation constant (Kd) of 63 nM. It exhibits no activity against protein methyltransferases, kinases, G-protein-coupled receptors (GPCRs), ion channels, and transporters. Notably, MS67 demonstrates significant anticancer properties. |
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T83547
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(Des-Bromo)-Neuropeptide B (1-23) (human)
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'(Des-Bromo)-Neuropeptide B (1-23) (human)' 是一种作用于orphan G-protein coupled receptor的激动剂，对GPR7 (NPBW1) 的Ki值为1.2 nM，而对GPR8 (NPBW2) 的Ki值则为341 nM。 |
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T62444
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NBI-27914
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NBI-27914 是一种有效的、选择性的 CRFR1 拮抗剂。其中 CRF 受体 CRFR1 和 CRFR2 是 G 蛋白偶联受体超家族的成员。 |
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T80198
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Vasopressin Dimer (anti-parallel) (TFA)
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Vasopressin Receptor |
GPCR/G Protein |
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Vasopressin Dimer (anti-parallel) TFA为Vasopressin的反平行二聚体形式，能够激活G蛋白偶联受体V1aR、V1bR、V2R和OTR四种。 |
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T68247
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PSB-KD107
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PSB-KD107 is an agonist of the Cannabinoid-Activated Orphan G‑Protein-Coupled Receptor GPR18. PSB-KD107 displayed significantly higher potency and efficacy than THC, determined in a GPR18-dependent β-arrestin recruitment assay, and were found to be selective versus the CB-sensitive receptors CB1, CB2, and GPR55. |
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T80876
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Vasomera
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Vasomera是一種穩定的長效血管活性腸肽（VIP）激動劑，主要作用於G蛋白偶聯的VPAC2受體，適用於與肌肉營養不良症相關的心肌病研究。 |
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T77789
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Oleoyl-L-alpha-lysophosphatidic acid sodium salt
LPA sodium salt
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Oleoyl-L-alpha-lysophosphatidic acid sodium salt为必需的细胞膜生物合成代谢物，可通过与G蛋白偶联受体（GPCR）（即LPA受体）相互作用来介导信号传导，是LPA1和LPA2受体的内源性激动剂。 |
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TP2194
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Neuropeptide Y (scrambled)
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Others |
Others |
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Neuropeptide Y (NPY) is a 36-amino acid neuropeptide that exerts its activity via G-protein-coupled receptors. NPY is widely distributed in the peripheral and central nervous systems. It modulates a variety of physiological processes, e.g. the central reg |
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T69207
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Chelerythrine hydroxide
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Chelerythrine hydroxide is the salt form of Chelerythrine, a benzophenanthridine alkaloid present in the plant Chelidonium majus (greater celandine). It is a potent, selective, and cell-permeable protein kinase C inhibitor in vitro. And an efficacious antagonist of G-protein-coupled CB1 receptors.]This molecule also exhibits anticancer qualities and it has served as a base for many potential novel drugs against cancer. |
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T76423
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Neuropeptide AF (cattle)
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Neuropeptide AF (cattle)是一种RFamide家族的酰胺化十八肽，主要作用于Mas相关基因受体A4 (MrgprA4) (Mas-related G-protein-coupled Receptor (MRGPR))和MrgprC11，其EC50分别约为60 nM和300 nM。此外，该化合物还能激活G蛋白偶联受体NPFF1 (Neuropeptide Y Receptor) 和NPFF2，EC50范围分别为25-325 nM和1-5 nM。Neuropeptide AF (cattle)具有显著的抗阿片及疼痛调节功能。 |
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T35804
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C16 Lactosylceramide (d18:1/16:0)
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C16 Lactosylceramide is an endogenous bioactive sphingolipid. It forms membrane microdomains with Lyn kinase and the αi subunits of inhibitory G protein-coupled receptors (GPCRs), suggesting a role in cell signaling. Plasma levels of C16 lactosylceramide are elevated in insulin-resistant cattle. C16 Lactosylceramide is also upregulated in a mouse model of Niemann-Pick type C1 disease, a neurodegenerative cholesterol-sphingolipid lysosomal storage disorder. |
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T75862
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BAM(8-22) TFA
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BAM(8-22) TFA 作为前脑啡肽 A 的蛋白水解切割产物，有效激活 Mas 相关 G 蛋白偶联受体（Mrgprs）、MrgprC11 及 hMrgprX1，并能在小鼠中通过 Mrgpr 依赖机制诱发抓挠行为。 |
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T28838
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SPM-242
SPM 242
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SPM-242 is an orthosteric agonist of Sphingosine 1-phosphate (S1P) and a bitopic antagonist. S1P is a lysophospholipid signaling molecule that regulates important biological functions, including vascular development and lymphocyte trafficking, by activat |
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T71963
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(−)-WIN 55,212-3 mesylate
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(−)-WIN 55,212-3 mesylate is an aminoalkylindole derivative which acts as a competitive neutral antagonist of the human cannabinoid CB2 receptor, blocking both the stimulating action of CP 55,940 and the inverse agonism of SR 144528. (−)-WIN 55,212-3 neither antagonizes nor mimics the effects of Δ9-THC on rat cerebellar membranes, which presumably express the CB1 receptor. (−)-WIN 55,212-3 also weakly antagonizes the melatonin MT1 and muscarinic M4 receptors but has no effect on several other G ... |
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T75925
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Orexin B, rat, mouse TFA
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Orexin B, rat, mouse (Rat orexin B) TFA，作为一种内源性促进食欲的(Orexin receptor)激动剂，通过结合并激活两个亲密相关的孤儿G蛋白偶联受体OX1-R和OX2-R，促进食物摄入和能量消耗，并在睡眠-觉醒调节中扮演关键角色。 |
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T76262
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Cagrilintide
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Cagrilintide为一种处于研发阶段的新型长效酰化胰岛素类似物，兼具非选择性胰岛素受体(AMYR)与降钙素G蛋白偶联受体(CTR)的激动剂功能。该化合物能显著降低体重并减少食物摄入，展现出针对肥胖疾病的研究潜力。 |
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T36080
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Rivenprost
ONO-4819
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Prostaglandin E2 activates four distinct G protein-coupled receptors, EP1-4. Rivenprost is a potent and selective agonist for the EP4 receptor (Ki = 0.7, 56, 620, and >10,000 nM for EP4, EP3, EP2, and EP1, respectively). It has been used to promote EP4-mediated bone formation, prevent bone loss related to osteoporosis, drive osteoblast differentiation, and stabilize bone implants.[1][2][3][4][5] Rivenprost has also been used to support wound healing.[6] |
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T36982
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CXCR3 Antagonist 6c
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CXCR3 antagonist 6c is an antagonist of chemokine (C-X-C motif) receptor 3 (CXCR3).1It inhibits calcium mobilization induced by chemokine (C-X-C motif) ligand 11 (CXCL11) in HEK293 cells expressing the human receptor (IC50= 0.06 μM). It is selective for CXCR3 over a panel of 14 human G protein-coupled receptors at 10 μM. CXCR3 antagonist 6c inhibits CXCR3-mediated migration of isolated human T cells (IC50= ~100 nM).
1.Cole, A.G., Stroke, I.L., Brescia, M.-R., et al.Identification and initial eva... |
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T75970
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Melanin Concentrating Hormone, salmon TFA
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Melanin Concentrating Hormone, salmon TFA (MCH (salmon) TFA) 是在硬骨鱼的垂体中发现的 19 个氨基酸组成的神经肽，它调节食物摄入，能量平衡，睡眠状态和心血管系统。Melanin Concentrating Hormone, salmon TFA (MCH (salmon) TFA) 是 SLC-1/GPR24和 MCHR2的配体。 |
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T69612
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PSB-KD477
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PSB-KD477 is an Agonist of the Cannabinoid-Activated Orphan G-Protein-Coupled Receptor GPR18. PSB-KD477 displayed significantly higher potency and efficacy than THC, determined in a GPR18-dependent β-arrestin recruitment assay, and were found to be selective versus the CB-sensitive receptors CB1, CB2, and GPR55. Structure-activity relationships were steep, and indole substitution was crucial for biological activity. These first selective agonists, which are structurally distinct from the lipidic... |
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T37283
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1-Palmitoyl Lysophosphatidic Acid (sodium salt)
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1-Palmitoyl lysophosphatidic acid (1-Palmitoyl LPA) is a LPA analog containing palmitic acid at the sn-1 position. LPA binds to one of five different G protein-coupled receptors (GPCRs) to mediate a variety of biological responses including cell proliferation, smooth muscle contraction, platelet aggregation, neurite retraction, and cell motility. In addition to playing a role in the aforementioned biological responses, 1-palmitoyl LPA enhances the action of β-lactam antibiotics (ampicillin, pipe... |
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T37669
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CAY10498
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The A1, A2A, A2B, and A3 adenosine receptors (ARs) are ubiquitous G protein-coupled receptors. The four AR subtypes have been implicated in several areas of therapeutic interest such as stroke and other ischemic conditions, as well as inflammation, neurodegenerative diseases, diabetes, and sleep regulation. A3 AR antagonists are of interest as therapeutic agents in glaucoma agents and inflammation. CAY10498 is a potent and selective A3 AR antagonist exhibiting a Ki of 37 nM with 60 and 200-fold ... |
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T75784
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Apelin-36(rat, mouse) TFA
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Apelin-36(rat, mouse) TFA 是一种内源性孤儿 G 蛋白偶联受体 APJ 激动剂。Apelin-36(rat, mouse) TFA 与 APJ 受体结合，IC50为 5.4 nM，显著抑制 cAMP 的产生，EC50为 0.52 nM。Apelin-36(rat, mouse) TFA 阻断 HIV-1和 HIV-2毒株进入表达 APJ 的 NP-2/CD4 细胞。 |
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T75785
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Apelin-17(human, bovine) TFA
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Apelin-17(human, bovine) TFA 是一种内源性孤儿 G 蛋白偶联受体 APJ 激动剂。Apelin-17(human, bovine) TFA 与在 HEK 293 细胞中表达的人 APJ 受体结合 (pIC50)。Apelin-17(human, bovine) TFA 阻断 HIV-1和 HIV-2毒株进入表达 APJ 的 NP-2/CD4 细胞。 |
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T75708
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Argipressin diacetate
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Argipressin (diacetate) (AVP (diacetate)，又称antidiuretic hormone (ADH)) 是一种由垂体后叶分泌的含9个氨基酸的神经肽。通过作用于三种G蛋白偶联受体(GPCRs)，Avpr1a (V1a)、Avpr1b (V1b) 及Avpr2 (V2)，它调控体液平衡、渗透压及心血管系统的生理功能，并可能对中枢代谢过程产生重要影响。 |
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T38336
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W140 (trifluoroacetate salt)
W140 (trifluoroacetate salt)
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Sphingosine-1-phosphate (S1P) is a bioactive lipid that exhibits a broad spectrum of biological activities including cell proliferation, survival, migration, cytoskeletal organization, and morphogenesis. It exerts its activity by binding to five distinct G protein-coupled receptors, S1P1/EDG-1, S1P2/EDG-5, S1P3/EDG-3, S1P4/EDG-6, and S1P5/EDG-8. W140 is an inactive enantiomer of W146, a selective S1P1 antagonist (Ki = 77 nM), that binds to the S1P1 receptor with a Ki of 4.6 μM (2a = W146; 2b = W... |
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T35794
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Kisspeptin-54 (human) (trifluoroacetate salt)
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Kisspeptin-54 is a peptide ligand of the orphan G protein-coupled receptor GPR54 (Kis = 1.81 and 1.45 nM for rat and human receptors, respectively).1 It is a 54 amino acid peptide encoded by the metastasis suppressor gene KISS-1. Kisspeptin-54 induces calcium mobilization in CHO-K1 cells expressing rat and human receptors (EC50s = 1.39 and 5.47 nM, respectively). It also induces arachidonic acid release in CHO cells expressing rat and human GPR54 in a concentration-dependent manner. Kisspeptin-5... |
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T75783
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Apelin-36(human) TFA
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Apelin-36(human) TFA 是一种内源性孤儿 G 蛋白偶联受体 APJ 激动剂，EC50为 20 nM。Apelin-36(human) TFA 对 HEK 293 细胞表达的人 APJ 受体有很高的亲和力 (pIC50=8.61)。Apelin-36(human) TFA 与两种主要的生物活性有关：心血管和代谢。Apelin-36(human) TFA 抑制 HIV-1和 HIV-2进入表达 APJ 的 NP2/CD4细胞。 |
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T38365
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CAY10597
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The biological effects of prostaglandin D2 (PGD2) are transduced by at least two 7-transmembrane G protein-coupled receptors, designated DP1 and CRTH2/DP2. In humans, CRTH2/DP2 is expressed on Th2 cells, eosinophils, and basophils where it mediates the chemotactic activity of PGD2. CAY10597, as a racemic mixture, is a potent CRTH2/DP2 receptor antagonist that binds to the human receptor with a Ki value of 37 nM. The R enantiomer is slightly more potent exhibiting Ki values of 23 and 22 nM at the... |
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T37187
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D-erythro/L-threo Lysosphingomyelin (d18:1)
D-erythro/L-threo Lysosphingomyelin (d18:1)
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Lysosphingomyelin is an endogenous bioactive sphingolipid and a constituent of lipoproteins.1,2It is produced by the removal of the acyl group from sphingomyelin by a deacylase and acts as a precursor in the biosynthesis of sphingosine-1-phosphate . D-erythroLysosphingomyelin is an agonist of the S1P receptors S1P1, S1P2, and S1P3(EC50s = 167.7, 368.1, and 482.6 nM, respectively, for the human receptors).3It is also an agonist of the orphan receptor ovarian cancer G protein-coupled receptor 1 (O... |
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T80240
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Ala-parafluoroPhe-Arg-Cha-Cit-Tyr-NH2
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Ala-parafluoroPhe-Arg-Cha-Cit-Tyr-NH2是一类具有生物活性的肽，作为蛋白酶激活受体1 (PAR-1) 的选择性激动剂，其特异性优于PAR-2。该肽通过HEK293细胞进行的基于细胞的钙信号传导测定确认了其对PAR-1的高特异性，并可用于研究PAR-1在体内的激活。PAR-1除了介导凝血酶的多种细胞作用外，还与PAR-4协作，参与调控凝血酶诱导的被分类为“凝血型”的肝细胞癌。 |
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T36578
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Boc-Lys(Ac)-AMC
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Commendamide (N-acyl-3-hydroxypalmitoyl-glycine) is a newly discovered GPCR G2A/GPR132 agonist (EC50=11.8 μM) that isolated from Bacteroides vulgatus. [1]
G2A/GPR132 belongs to the guanine nucleotide-binding protein (G protein)-coupled receptor (GPCR) superfamily. GPR132/G2A is first reported to be a transcriptional target for BCR-ABL tyrosine kinase attenuating B-cell expansion in vitro and arresting cells at G2 during mitosis. It has been involved in autoimmune disease and atherosclerosis. [1]... |
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T37441
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KMN-80
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The prostaglandin E receptor 4 (EP4) is one of four G protein-coupled receptors that mediate the actions of prostaglandin E2 . Binding of PGE2 to the EP4 receptor causes an increase in intracellular cyclic AMP, which plays important roles in bone formation and resorption, cancer, and atherosclerosis. KMN-80 is a substituted γ-lactam (pyrrolidinone) derivative of PGE1 that acts as a selective and potent agonist of EP4 with an IC50 value of 3 nM (IC50 = 1.4 μM for EP3 and > 10 μM for all other pro... |
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T74142
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Angiotensin II human TFA
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Angiotensin II human (Angiotensin II) TFA 作为肾素/血管紧张素系统中关键的生物活性肽，扮演着血管收缩剂的角色并在调节人体血压中发挥中心作用。其主要通过与 G 蛋白偶联受体 (GPCRs)、血管紧张素 II 1型受体 (AT1R) 和血管紧张素 II 2型受体 (AT2R) 的相互作用来介导效应，包括刺激交感神经系统、增加醛固酮的生物合成和肾脏功能。此外，Angiotensin II human TFA 促进血管平滑肌细胞的生长和 I 型及 III 型胶原在成纤维细胞中的合成，导致血管壁与心肌增厚及纤维化，并诱导细胞凋亡。还通过LOX-1依赖的氧化还原敏感路径诱导内皮细胞中的毛细血管形成。 |
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T83697
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PAMP-12 (human, mouse, rat, porcine, bovine) TFA
Proadrenomedullin N-terminal 12 Peptide,PAMP (9-20)
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Proadrenomedullin N-terminal 12 peptide (PAMP-12) 是一种内源性肽段，源自人体肾上腺髓质，对应人类PAMP-20的9-20氨基酸，涉及降低血压。它是MAS相关G蛋白偶联受体家族成员X2 (MRGPRX2) 的激动剂。在表达人MRGPRX2的CHO细胞中，PAMP-12抑制forskolin诱导的cAMP积累（EC50 = 57.2 nM），特异性诱导表达MRGPRX2的CHO细胞的钙离子动员（EC50 = 41 nM），而在表达MRGPRX1、MRGPRX3或MRGPRX4的细胞中则无此效应（在1 µM浓度下）。PAMP-12还能作为烟碱型乙酰胆碱受体（nAChRs）的拮抗剂，抑制carbachol诱导的儿茶酚胺释放（IC50 = 1.3 µM）及钙和钠的流入（IC50分别为0.39 µM和0.87 µM），但不抑制组胺诱导的儿茶酚胺释放或钙和钠的流入（IC50 >1 µM），在初级牛肾上腺嗜铬细胞中有此表现。当以10至50 nmol/kg剂量给予正常血压大鼠时，PAMP-12能降低平均动脉血压。 |
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