orphan

Orphan GPCR SP9155 agonist P550 (mouse, rat) (26RFa (mouse, rat)) is an RFamide peptide family member with an orexigenic effect, acting as the cognate ligand for the mouse orphan receptor GPR103, also known as SP9155 or AQ27.

Orphan GPCR SP9155 agonist P550 (mouse, rat) acetate (Orphan GPCR SP9155 agonist P550 ) is a member of the RFamide peptide family with orexigenic effects.

Orphanin FQ(1-11) TFA, a fragment of orphanin FQ or nociceptin (OFQ/N), acts as a powerful NOP receptor (ORL-1; OP4) agonist with a K i of 55 nM. It lacks affinity for μ, δ, κ1, and κ3 receptors (K i >1000 nM), demonstrating specificity, and exhibits analgesic properties in CD-1 mice [1] [2].

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.

Orphanin FQ(1-11) acetate(178249-41-7 free base) is a peptide fragment containing amino acids 1-11 of Nociceptin. Orphanin FQ(1-11) acetate(178249-41-7 free base) 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) acetate(178249-41-7 free base) displays analgesic properties in CD-1 mice.

Nociceptin (Orphanin FQ) is a 17-amino-acid polypeptide that is structurally related to the opioid peptide dynorphin A.

Neuropeptide S (Rat) acetate is an endogenous ligand of a previously orphan G-protein-coupled receptor now named NPS receptor. Neuropeptide S (Rat) acetate can be used for the research of nervous system disease [1].

Urotensin II, mouse acetate (9047-55-6 free base) is an endogenous ligand for the orphan GPR14 or SENR. It is a potent vasoconstrictor.

Obestatin is a 23 amino acid peptide hormone with a conserved C-terminal glycine residue and amidation site that is formed by cleavage of the ghrelin and obestatin prepropeptide.1It binds to the orphan receptor GPR39 (Kd= 1 nM) and stimulates cAMP production in CHO and HEK293 cells overexpressing human GPR39. Obestatin inhibits contraction of isolated mouse jejunum muscle strips induced by ghrelin .In vivo, obestatin (12.5-1,000 nmol/kg) suppresses food intake in a time- and dose-dependent manner and reduces body weight gain and gastric emptying in mice. Obestatin (0.22 g per animal) also reduces food intake and glucose response without affecting plasma insulin responses in fasted high-fat diet fed mice.2 1.Zhang, J.V., Ren, P.C., Avsian-Kretchmer, O., et al.Obestatin, a peptide encoded by the ghrelin gene, opposes ghrelin's effects on food intakeScience310(5750)996-999(2005) 2.Subasinghage, A.P., Green, B.D., Flatt, P.R., et al.Metabolic and structural properties of human obestatin {1-23} and two fragment peptidesPeptides31(9)1697-1705(2010)

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-54 (10-1,000 nM) inhibits insulin secretion from isolated mouse pancreatic β-cells in the presence of 2.8 mM, but not 11.1 mM, glucose.2 Kisspeptin-54 (1-5 nmol, i.c.v.) increases serum levels of luteinizing hormone (LH) and follicular stimulating hormone (FSH) in mice, an effect which is reversed by the gonadotropin releasing hormone (GNRH) antagonist acycline.3References1. Kotani, M., Detheux, M., Vandenbogaerde, A.L., et al. The metastasis suppressor gene KiSS-1 encodes kisspeptins, the natural ligands of the orphan G protein-coupled receptor GPR54. J. Biol. Chem. 276(37), 34631-34636 (2001).2. Vikman, J., and Ahrén, B. Inhibitory effect of kisspeptins on insulin secretion from isolated mouse islets. Diabetes Obes. Metab. 11(Suppl 4), 197-201 (2009).3. Gottsch, M.L., Cunningham, M.J., Smith, J.T., et al. A role for kisspeptins in the regulation of gonadotropin secretion in the mouse. Endocrinology 145(9), 4073-4077 (2004). 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-54 (10-1,000 nM) inhibits insulin secretion from isolated mouse pancreatic β-cells in the presence of 2.8 mM, but not 11.1 mM, glucose.2 Kisspeptin-54 (1-5 nmol, i.c.v.) increases serum levels of luteinizing hormone (LH) and follicular stimulating hormone (FSH) in mice, an effect which is reversed by the gonadotropin releasing hormone (GNRH) antagonist acycline.3 References1. Kotani, M., Detheux, M., Vandenbogaerde, A.L., et al. The metastasis suppressor gene KiSS-1 encodes kisspeptins, the natural ligands of the orphan G protein-coupled receptor GPR54. J. Biol. Chem. 276(37), 34631-34636 (2001).2. Vikman, J., and Ahrén, B. Inhibitory effect of kisspeptins on insulin secretion from isolated mouse islets. Diabetes Obes. Metab. 11(Suppl 4), 197-201 (2009).3. Gottsch, M.L., Cunningham, M.J., Smith, J.T., et al. A role for kisspeptins in the regulation of gonadotropin secretion in the mouse. Endocrinology 145(9), 4073-4077 (2004).

Urotensin II-related peptide acetate are endogenous ligands of the orphan G-protein-coupled receptor GPR14, now known as UT. Urotensin II and URP exert a wide spectrum of biological effects on peripheral tissues including the cardiovascular system, airway smooth muscle, kidneys, and endocrine glands, while central administration elicits complex behavioral and cardiovascular responses, highlighting their physiological and pharmacological significance.

Apelin-12 is a highly potent C-terminal fragment of a polypeptide that exhibits a strong affinity towards the orphan receptor APJ. It plays a role in maintaining body fluid balance and regulating feeding control in the central nervous system. Additionally, Apelin-12 functions as an inhibitor of HIV-1 entry through the APJ receptor and demonstrates neuroprotective properties.

Apelin-12 acetate possesses a high affinity to orphan receptor APJ receptor. Apelin-12 acetate inhibits the JNK and p38 MAPK signaling pathway of the apoptosis-related MAPKs family, thus offering protection to neurons.

Apelin-36(human) TFA, an endogenous agonist of the orphan G protein-coupled receptor APJ, exhibits a potent EC50 of 20 nM and high affinity (pIC5 50 = 8.61) for human APJ receptors in HEK 293 cells. It is involved in significant cardiovascular and metabolic activities. Furthermore, Apelin-36(human) TFA can inhibit the entry of certain HIV-1 and HIV-2 strains into NP2/CD4 cells expressing the APJ receptor. [1] [2] [3] [4]

Apelin-36(rat, mouse) TFA, an endogenous agonist for the orphan G protein-coupled receptor APJ, exhibits a strong affinity for APJ receptors with an IC 50 of 5.4 nM and effectively inhibits cAMP production with an EC 50 of 0.52 nM. Moreover, it obstructs the invasion of certain HIV-1 and HIV-2 strains into NP-2/CD4 cells that express the APJ receptor [1] [2].

Apelin-17(human, bovine) TFA is an endogenous agonist of the orphan G protein-coupled receptor APJ, demonstrating affinity for human APJ receptors on HEK 293 cells with a pIC50 value of 9.02. It also blocks the entry of certain HIV-1 and HIV-2 strains into NP2/CD4 cells that express the APJ receptor [1] [2] [3].

Orexin B, rat, mouse (Rat orexin B) TFA, an endogenous agonist for orexin receptors, binds to and activates the orphan G protein-coupled receptors OX1-R and OX2-R, playing a crucial role in stimulating food intake, increasing energy expenditure, and regulating sleep-wake cycles [1] [2] [3].

Urotensin II, mouse acetate, serves as an endogenous ligand for the orphan G-protein-coupled receptor GPR14 or SENR and acts as a potent vasoconstrictor. Its physiological function extends to the central nervous system [1].

Melanin Concentrating Hormone, salmon TFA (MCH (salmon) TFA), is a 19-amino-acid neuropeptide discovered in the pituitary gland of teleost fish; it regulates food intake, energy balance, sleep states, and cardiovascular functions, and acts as a ligand for the orphan G protein-coupled receptors SLC-1/GPR24 and MCHR2.

Nocistatin, an endogenous neuropeptide, serves as a ligand for the orphan opioid receptor-like receptor and functionally antagonizes the neuropeptide nociceptin/orphanin FQ (Noc/OFQ). It inhibits 5-HT release through a G i/o protein-mediated pathway and blocks nociceptin-induced allodynia and hyperalgesia [1] [2].

NocII TFA, an orphan neuropeptide, stimulates locomotor activity in mice [1].

Neuromedin S (human), a 33-amino acid neuropeptide, serves as an endogenous ligand for the orphan G-protein coupled receptor (GPCR) FM-4/TGR-1, and acts on the neuromedin U (NMU) receptor 2 (NMUR2) to regulate body weight homeostasis [1].

'(Des-Bromo)-Neuropeptide B (1-23) (human)' is an agonist for orphan G-protein-coupled receptors, exhibiting a K i of 1.2 nM for GPR7 (NPBW1) and 341 nM for GPR8 (NPBW2) respectively [1].

VPM-p15, a synthetic peptide agonist targeting the adhesion G protein-coupled receptor (GPCR) G2 (ADGRG2)—an orphan GPCR implicated in male infertility—facilitates cAMP accumulation in HEK293 cells expressing human ADGRG2, demonstrating efficacy with an EC50 value of 1.41 µM.