GHSR
Growth hormone secretagogue receptor; Ghrelin receptor
GHSR (Growth hormone secretagogue receptor) is a seven transmembrane G protein-coupled receptor with high expression in the anterior pituitary, pancreatic islets, thyroid gland, heart and various regions of the brain. Two types of GHS-R are accepted to be present, GHS-R1a and GHS-R1b.
Ghrelin is a gastric polypeptide displaying strong GH-releasing activity by activation of the GHS-R1a located in the hypothalamus-pituitary axis. GHS-R1a is a G-protein-coupled receptor that, upon the binding of ghrelin or synthetic peptidyl and non-peptidyl ghrelin-mimetic agents known as GHS, preferentially couples to Gq, ultimately leading to increased intracellular calcium content. Beside the potent GH-releasing action, ghrelin and GHS influence food intake, gut motility, sleep, memory and behavior, glucose and lipid metabolism, cardiovascular performances, cell proliferation, immunological responses and reproduction.
GHSR アイソフォーム特異的製品
All Product Categories
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GHSR 関連製品 (76)
関連製品 (76)
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抗体 (3)
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GHSR Isoform Comparison
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Anamorelin
(Anamorelin)
0 Images別名: RC-1291; ONO-7643Anamorelin (RC-1291) is an orally active Ghrelin receptor agonist with an EC50 of 0.74 nM. Anamorelin can promote appetite, increase body weight, and stimulate the secretion of growth hormone and insulin-like growth factor-1. Anamorelin can be used in the research of anorexia and cancer cachexia.
- Ibutamoren Mesylate (Ibutamoren (Mesylate))
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LEAP-2
0 Images別名: Human liver expressed antimicrobial peptide-2LEAP-2 (Human liver expressed antimicrobial peptide-2) is a GHS-R1a antagonist, with an IC50 of 6.0 nM. LEAP-2 suppresses the orexigenic effect of ghrelin. LEAP-2 attenuates ghrelin-induced growth hormone (GH) release and reduces basal food intake. LEAP-2 exhibits antimicrobial activity against microbial model organisms. LEAP-2 can be used for the study of obesity and infection.
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Anamorelin hydrochloride
0 Images別名: RC-1291 hydrochloride; ONO-7643 hydrochlorideAnamorelin (RC-1291) hydrochloride is an orally active Ghrelin receptor agonist with an EC50 of 0.74 nM. Anamorelin hydrochloride can promote appetite, increase body weight, and stimulate the secretion of growth hormone and insulin-like growth factor-1. Anamorelin hydrochloride can be used in the research of anorexia and cancer cachexia.
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PF-5190457
(PF-5190457)
0 Images別名: PF-05190457PF-5190457 (PF-05190457) is a potent and selective ghrelin receptor inverse agonist with a pKi of 8.36.
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(S)-PF-5190457
0 Images製品番号: HY-12584A純度: 99.27%別名: (S)-PF-05190457(S)-PF-5190457 ((S)-PF-05190457) is the S-enantiomer of PF-5190457 (HY-12584). PF-5190457 (PF-05190457) is a potent and selective ghrelin receptor inverse agonist with a pKi of 8.36.
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KARI 101
0 Images製品番号: HY-186165CAS 番号: 3061559-97-2KARI 101 is a blood-brain barrier permeable acid sphingomyelinase (ASM) inhibitor. KARI 101 directly inhibits ASM activity and reduces ceramide production. KARI 101 induces Ca2+ mobilization, activates AMPK and triggers GHSR1α internalization. KARI 101 can be used for the research of Alzheimer's disease.
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Ibutamoren
0 Images別名: MK-677 free base; MK-0677 free baseIbutamoren (MK-677 free base; MK-0677 free base) is an orally active non-peptide growth hormone secretagogue receptor agonist. Ibutamoren activates signal cascades by mimicking endogenous ligands, triggers pulsatile release of growth hormone from the pituitary gland, and increases serum levels of IGF-1 and insulin-like growth factor-binding protein 3. Ibutamoren not only increases the frequency of growth hormone pulses in male individuals, but also promotes elevated bone formation markers in female individuals with postmenopausal osteoporosis. The combination of Ibutamoren with Alendronate sodium hydrate (HY-11101) significantly increases bone mineral density at the femoral neck. However, Ibutamoren may cause mild, reversible adverse reactions such as increased appetite, fluid retention, and elevated fasting blood glucose. Ibutamoren has been widely used in studies related to idiopathic growth hormone deficiency, sarcopenia, Alzheimer's disease, and osteoporosis.
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JMV 2959
0 ImagesJMV 2959 is a growth hormone secretagogue receptor type 1a (GHS-R1a) antagonist with an IC50 of 32 nM.
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Relamorelin TFA
0 Images別名: RM-131 TFA; BIM-28131 TFARelamorelin (RM-131) TFA, a pentapeptide ghrelin analog, is a selective ghrelin/growth hormone secretagogue receptor (GHSR) agonist with a Ki of 0.42 nM for GHS-1a receptor. Relamorelin TFA is centrally penetrant. Relamorelin TFA increases growth hormone levels and accelerates gastric emptying. Relamorelin TFA has the potential for cachexia, gastroparesis, and gastric/intestinal dysmobility disorders research.
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Macimorelin acetate
0 Images別名: EP-1572 acetate; AEZS-130 acetate
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des-Gln14-Ghrelin
0 Imagesdes-Gln14-Ghrelin is a second endogenous ligand for the growth hormone secretagogue receptor. a). des-Gln14-ghrelin potently induces increases in [Ca2+]i in CHO-GHSR62 cells, with an EC50 of 2.4 nM.
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AZP-531
0 ImagesAZP-531 is an analogue of unacylated ghrelin designed to improve glycaemic control and reduce weight.
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Meranzin hydrate
0 ImagesMeranzin hydrate is an orally active antidepressant and GHSR modulator. Meranzin hydrate significantly upregulates the expression levels of brain-derived neurotrophic factor and p-mTOR in the hippocampus via the ghrelin-growth hormone secretagogue receptor pathway. Meranzin hydrate regulates blood oxygen level-dependent signals in the hippocampus-thalamus-basal ganglia circuit, attenuates reward system activation, and promotes the normalization of related hormone levels. Meranzin hydrate effectively ameliorates depression-like behaviors and gastrointestinal hypomotility, and can be used in research related to depression and major depressive disorder.
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KARI 201 hydrochloride
0 ImagesKARI 201 hydrochloride is a selective, brain penetrant pand competitive acid sphingomyelinase (ASM) inhibitor with an IC50 of 338.3?nM. KARI 201 hydrochloride is a ghrelin receptor agonist. KARI 201 hydrochloride improves neuropathological features of Alzheimer's disease.
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JMV 2959 hydrochloride
0 Images製品番号: HY-U00433ACAS 番号: 2448414-54-6JMV 2959 hydrochloride is a growth hormone secretagogue receptor type 1a (GHS-R1a) antagonist with an IC50 of 32±3 nM in LLC-PK1 cells.
