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Search Results for " ghrelin "

40

抑制剂 & 化合物

4

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
TP2032	des-Gln14-Ghrelin des-Gln14-Ghrelin (rat)
	An endogenous ligand for the ghrelin receptor (GHS-R1a), produced by alternative splicing of the rat ghrelin gene. Potently induces Ca2+ release in cells expressing ghrelin receptors (EC50 = 2.4 nM) and stimulates GH release in vivo.
T40234	Ghrelin receptor full agonist-2
	Ghrelin receptor full agonist-2 is a highly potent Ghrelin receptor full agonist.
TP2241	[Des-octanoyl]-Ghrelin (human)	Others	Others
	[Des-octanoyl]-Ghrelin (human) is a Non-acylated, major circulating isoform of ghrelin.
TP2242	[Des-octanoyl]-Ghrelin (rat)	Others	Others
	[Des-octanoyl]-Ghrelin (rat) is a Non-acylated, major circulating isoform of ghrelin.
T75928	des-Gln14-Ghrelin TFA
	des-Gln14-Ghrelin TFA为生长激素促分泌受体的第二个内源性配体。该化合物能在CHO-GHSR62细胞中诱导[Ca2+]I的提升，其EC50值为2.4 nM。
T10319	Anamorelin RC-1291,阿拉莫林,ONO-7643	GHSR	GPCR/G Protein
	Anamorelin (ONO-7643) 是新型ghrelin receptor 激动剂，根据FLIPR 检测，得到其EC50=0.74 nM。
T16508	PF-5190457 PF-05190457	GHSR	GPCR/G Protein
	PF-5190457 是具有选择性的、有效的生长素释放肽受体选择性的反向激动剂(pKi:8.36)。
T7225	AnaMorelin hydrochloride RC-1291 hydrochloride,阿拉莫林盐酸盐,ONO-7643 hydrochloride	GHSR	GPCR/G Protein
	AnaMorelin hydrochloride (RC-1291 hydrochloride) 是生长素受体激动剂，根据 FLIPR 检测，得到 EC50=0.74 nM。
T23543	YIL 781	GHSR	GPCR/G Protein
	YIL 781是一种选择性ghrelin 受体拮抗剂(GHS-R1a) (Ki = 17 nM))，对运动素受体显示出较弱的亲和力(K = 6 μ M)。YIL 781通过阻断胃饥饿素分泌对体内和体外胰岛素分泌改善体内葡萄糖稳态。
TP1931L1	[D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P acetate [D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P acetate(96736-12-8 free base)	cholecystokinin	GPCR/G Protein
	[D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P acetate ([D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P acetate (96736-12-8 free base)) 是广谱神经肽反向激动剂和拮抗剂。 ghrelin 受体的强效完全反向激动剂(EC50 = 5.2 nM)；减少组成型生长素释放肽受体信号传导。它也是速激肽、缓激肽、CCK 和铃蟾肽受体的拮抗剂。在体外诱导细胞凋亡并抑制癌细胞生长。
T10319L	Anamorelin Fumarate ONO-7643 Fumarate,RC1291 Fumarate,富马酸阿拉莫林	Others	Others
	Anamorelin Fumarate is a novel ghrelin receptor agonist (EC50: 0.74 nM in the FLIPR assay).
T34281	Relamorelin BIM28131,RM 131,BIM-28131,BIM-28163,BIM 28163,BIM28163,BIM 28131	GHSR	GPCR/G Protein
	Relamorelin (RM-131)是一种具有选择性和有效性的生长素释放肽/生长激素促分泌素受体 (GHSR) 激动剂，是一种有效的生长素释放肽模拟物，对 GHS-1a 受体具有很高的亲和力。Relamorelin 是一种具有中枢渗透性的五肽，可增加生长激素水平，加速胃排空，具有研究恶病质的潜力。
T22898	L-692585 L-692,585	Others	Others
	ghrelin receptor (GHS-R1a) agonist
T23413	Tabimorelin hemifumarate	Others	Others
	orally active ghrelin receptor (GHS-R1a) agonist
T27443	GSK 894281 GSK894281,GSK-894281
	GSK 894281 is a ghrelin receptor agonist. It may produces myocardial degeneration/necrosis in rats.
T28812	SM-130686 SM 130686,SM130,686,SM 130,686
	SM-130,686 is a potent, orally-active agonist of the ghrelin/growth hormone secretagogue receptor (GHSR) and growth hormone secretagogue. It has around half the potency of the endogenous agonist ghrelin as a stimulator of growth hormone release.
TP2236	Cortistatin-8	Others	Others
	ghrelin receptor antagonist
TP1894	K-(D-1-Nal)-FwLL-NH2
	High affinity and potent ghrelin receptor inverse agonist (Ki values are 4.9 and 31 nM in COS7 and HEK293T cells, respectively). Blocks ghrelin receptor-mediated Gq- and G13-dependent signaling pathways.
T27451	GSK1614343 GSK-1614343,GSK 1614343
	GSK1614343 is an antagonist of ghrelin receptor.
T29174	YIL781 hydrochloride YIL 781,YIL-781,YIL781 HCl,YIL781
	YIL781 is a ghrelin receptor antagonist (GHS-R1a) (Ki = 17 nM) with no significant affinity for the motilin receptor (Ki = 6 μM).
T71632	TZP-102
	TZP-102 is a potent, oral, ghrelin receptor agonist that has been shown to improve diabetic gastroparesis symptoms.
TP1439	AZP-531
	Azp-531 is a disacylated ghrelin used to improve blood sugar control and weight loss.
T17202	Ulimorelin TZP-101	Others	Others
	Ulimorelin is a ghrelin receptor agonist (EC50: 29 nM and a Ki of 16 nM). Ulimorelin is a prokinetic agent and causes vasorelaxation through competitive antagonist action at α1-adrenoceptors.
T28366	PF-04628935 PF 04628935,PF 4628935,PF4628935,PF04628935,PF-4628935
	PF-04628935 is a potent antagonist/inverse agonist of the ghrelin receptor, growth hormone secretagogue receptor 1a (GHS-R1a) with an IC50 of 4.6 nM. PF-04628935 is orally bioavailable and brain penetrant.
T27493	GSK-894490A GSK 894490A
	GSK-894490A is an agonist of ghrelin receptor. GSK-894490A crosses the blood/brain barrier and elicit pro-cognitive effects.
T35787	Obestatin (human) (trifluoroacetate salt)
	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 manne...
T75948	K-(D-1-Nal)-FwLL-NH2 TFA
	K-(D-1-Nal)-FwLL-NH2 TFA is a potent and high-affinity inverse agonist of the ghrelin receptor, exhibiting Ki values of 4.9 nM in COS7 cells and 31 nM in HEK293T cells. This compound effectively inhibits ghrelin receptor-mediated Gq- and G13-dependent signaling pathways.
TP1931	[D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P
	Broad spectrum neuropeptide inverse agonist and antagonist. Potent full inverse agonist for the ghrelin receptor (EC50 = 5.2 nM); diminishes constitutive ghrelin receptor signaling. Also antagonist at tachykinin, bradykinin, CCK and bombesin receptors. In
T11448	GOAT-IN-1	Others	Others
	GOAT-IN-1 is an inhibitor of ghrelin O-acyltransferase (GOAT), which could be useful for the prophylaxis or treatment of diabetes, hyperlipidemia, non-alcoholic fatty liver, Alzheimer’s disease, Parkinson’s disease, cerebrovascular dementia, cerebral infa
T39236	Relamorelin acetate Relamorelin acetate,RM-131 acetate,BIM-28131acetate
	Relamorelin (RM-131) acetate is a pentapeptide ghrelin analog that acts as a selective agonist for the ghrelin/growth hormone secretagogue receptor (GHSR). It exhibits a high affinity for the GHS-1a receptor, with a Ki value of 0.42 nM. Notably, Relamorelin acetate can cross the blood-brain barrier and target the central nervous system. This compound effectively increases growth hormone levels and promotes faster gastric emptying. Due to these properties, Relamorelin acetate holds promise for it...
T35793	JMV3002 JMV3002
	Ghrelin is an endogenous ligand for the growth hormone secretagogue receptor that stimulates food intake and transduces signals to hypothalamic regulatory nuclei that control energy homeostasis. JMV3002 is a potent ghrelin receptor antagonist with an IC50 value of 1.1 nM in vitro. At 80 μg/kg, JMV3002 inhibits hexarelin-stimulated food intake by as much as 98% in rats. JMV3002 alone does not elicit growth hormone release nor does it inhibit hexarelin-stimulated growth hormone secretion when test...
T82961	ASB20123
	ASB20123 是一款融合了CNP/ghrelin序列的嵌合肽，具有促进骨骼生长的效能，适用于研究生长障碍和侏儒症。
T81625	Obestatin(human) TFA
	Obestatin(human) TFA, 同源于与ghrelin相同的前体多肽，是一种内源性肽。该化合物抑制大鼠食欲并降低体重增加。
T81287	RFRP-3 (rat)
	RFRP-3 (rat) 为一种神经肽，其抑制作用使促性腺激素分泌降低，同时显著提升生长激素释放激素mRNA及血浆生长激素水平。
T37412	AZ-GHS-22
	AZ-GHS-22 is an inverse agonist of the growth hormone secretagogue receptor 1a (GHS-R1a), which is also known as the ghrelin receptor.1It binds to GHS-R1a with an IC50value of 0.77 nM. AZ-GHS-22 decreases food intake in mice by 54% in the first two hours after administration of a 100 mg/kg dose. 1.McCoull, W., Barton, P., Brown, A.J.H., et al.Identification, optimization, and pharmacology of acylurea GHS-R1a inverse agonistsJ. Med. Chem.57(14)6128-6140(2014)
T75901	Obestatin(rat) TFA
	Obestatin(rat) TFA 是一个包含23个氨基酸的肽，由Ghrelin基因编码。该化合物能够抑制食欲和空肠收缩，并能减缓体重增加。同时，Obestatin(rat) TFA 作为G 蛋白偶联受体 39 (GPR39) 的内源性配体，发挥抗炎、抗心肌梗塞和抗氧化功能。
T75262	Relamorelin TFA
	Relamorelin (RM-131) TFA，一种生长素类似物，是一种选择性的生长素释放肽/生长激素促分泌素受体 (GHSR) 激动剂，对GHS-1a 受体的Ki 值为 0.42 nM。Relamorelin TFA 是一种五肽，具有中枢渗透性。Relamorelin TFA 增加生长激素水平，加速胃排空，具有用于恶病质、胃轻瘫和胃/肠运动障碍研究的潜力。
T68276	Macimorelin acetate EP-1572 acetate ; AEZS-130 acetate,AEZS-130 acetate,EP-1572 acetate
	Macimorelin (EP-1572) acetate，一种 GH 促分泌素，是一种具有口服活性的GHSR 激动剂。Macimorelin acetate 可刺激 GH 的释放。Macimorelin acetate 可用于成人生长激素缺乏症 (AGHD) 和癌症厌食-恶病质综合征 (CACS) 的研究。
T64475	FMOC-L-THR
	FMOC-L-THR (AZP-531) is an analogue of unacylated ghrelin designed to improve glycaemic control and reduce weight. The O-glycosidic linkage and the O-acetyl protection in this building block is stable to both piperidine and TFA, making it completely compatible with standard protocols in Fmoc solid phase peptide synthesis. The Tn antigen is a tumor-associated carbohydrate antigen that is not normally expressed in peripheral tissues or blood cells. Expression of this antigen, which is found in a m...
TP2215	Agouti-related Protein (AGRP) (25-82), human	Others	Others
	Agouti-related peptide (AgRP) is a neuropeptide produced in the brain by the AgRP/NPY neuron. It is only synthesized in NPY containing cell bodies located in the ventromedial part of the arcuate nucleus in the hypothalamus. The appetite-stimulating effect

化合物

des-Gln14-Ghrelin

Cat.No: TP2032

Synonym: des-Gln14-Ghrelin (rat)

Ghrelin receptor full agonist-2

Cat.No: T40234

[Des-octanoyl]-Ghrelin (human)

Cat.No: TP2241

Target: Others

[Des-octanoyl]-Ghrelin (rat)

Cat.No: TP2242

Target: Others

des-Gln14-Ghrelin TFA

Cat.No: T75928

Cat.No: T10319

Synonym: RC-1291,阿拉莫林,ONO-7643

Target: GHSR

Cat.No: T16508

Synonym: PF-05190457

Target: GHSR

AnaMorelin hydrochloride

Cat.No: T7225

Synonym: RC-1291 hydrochloride,阿拉莫林盐酸盐,ONO-7643 hydrochloride

Target: GHSR

Cat.No: T23543

Target: GHSR

[D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P acetate

Cat.No: TP1931L1

Synonym: [D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P acetate(96736-12-8 free base)

Target: cholecystokinin

Anamorelin Fumarate

Cat.No: T10319L

Synonym: ONO-7643 Fumarate,RC1291 Fumarate,富马酸阿拉莫林

Target: Others

Cat.No: T34281

Synonym: BIM28131,RM 131,BIM-28131,BIM-28163,BIM 28163,BIM28163,BIM 28131

Target: GHSR

Cat.No: T22898

Synonym: L-692,585

Target: Others

Tabimorelin hemifumarate

Cat.No: T23413

Target: Others

Cat.No: T27443

Synonym: GSK894281,GSK-894281

Cat.No: T28812

Synonym: SM 130686,SM130,686,SM 130,686

Cat.No: TP2236

Target: Others

K-(D-1-Nal)-FwLL-NH2

Cat.No: TP1894

Cat.No: T27451

Synonym: GSK-1614343,GSK 1614343

YIL781 hydrochloride

Cat.No: T29174

Synonym: YIL 781,YIL-781,YIL781 HCl,YIL781

Cat.No: T71632

Cat.No: TP1439

Cat.No: T17202

Synonym: TZP-101

Target: Others

Cat.No: T28366

Synonym: PF 04628935,PF 4628935,PF4628935,PF04628935,PF-4628935

Cat.No: T27493

Synonym: GSK 894490A

Obestatin (human) (trifluoroacetate salt)

Cat.No: T35787

K-(D-1-Nal)-FwLL-NH2 TFA

Cat.No: T75948

[D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P

Cat.No: TP1931

Cat.No: T11448

Target: Others

Relamorelin acetate

Cat.No: T39236

Synonym: Relamorelin acetate,RM-131 acetate,BIM-28131acetate

Cat.No: T35793

Synonym: JMV3002

Cat.No: T82961

Obestatin(human) TFA

Cat.No: T81625

Cat.No: T81287

Cat.No: T37412

Obestatin(rat) TFA

Cat.No: T75901

Relamorelin TFA

Cat.No: T75262

Macimorelin acetate

Cat.No: T68276

Synonym: EP-1572 acetate ; AEZS-130 acetate,AEZS-130 acetate,EP-1572 acetate

Cat.No: T64475

Agouti-related Protein (AGRP) (25-82), human

Cat.No: TP2215

Target: Others

Cat. No.	Product Name	Target	Signaling Pathways
T2O2721	L-Cysteine Thioserine,L-半胱氨酸,cysteine,半胱氨酸,L-(+)-Cysteine	Endogenous Metabolite	Metabolism
	L-Cysteine (L-(+)-Cysteine) 是人体非必需的含硫氨基酸。L-Cysteine 对蛋白质合成、解毒和多种代谢功能很重要。L-Cysteine 存在于指甲、皮肤和头发的主要蛋白质-角蛋白中，对胶原蛋白的生成、皮肤弹性和质地都很重要。L-Cysteine 是抗氧化剂谷胱甘肽的一种成分，在辅酶A、肝素和生物素等基本生化物质的代谢中起着重要作用，也是氨基酸牛磺酸的制造所必需的。
T80006	Emoghrelin	GHSR	GPCR/G Protein
	Emoghrelin是一种从Polygonum multiflorum（何首乌）提取的化合物，能够通过激活生长素释放肽受体来刺激生长激素的分泌。
T8141	L-Cysteine hydrochloride L-Cysteine HCl,L-半胱氨酸盐酸盐,L-半胱氨酸盐酸盐(无水物)	Others; Endogenous Metabolite	Metabolism; Others
	L-Cysteine hydrochloride (L-Cysteine HCl) 是一种条件必需氨基酸，是硫化氢 (H2S)、牛磺酸谷胱甘肽和等生物特性分子的前体。它能抑制胃饥饿素，抑制啮齿动物和人类的食欲。
TN5283	L-Cysteine hydrochloride hydrate L-Cysteine hydrochloride monohydrate,L-半胱氨酸盐酸盐一水物,L-半胱氨酸盐酸盐一水合物	Others; Endogenous Metabolite	Metabolism; Others
	L-Cysteine hydrochloride hydrate (L-Cysteine hydrochloride monohydrate) 是条件必需氨基酸，是硫化氢、谷胱甘肽和牛磺酸等生物活性分子的前体。它可以抑制胃饥饿素，抑制啮齿动物和人类的食欲。

天然产物

Cat.No: T2O2721

Synonym: Thioserine,L-半胱氨酸,cysteine,半胱氨酸,L-(+)-Cysteine

Target: Endogenous Metabolite

Cat.No: T80006

Target: GHSR

L-Cysteine hydrochloride

Cat.No: T8141

Synonym: L-Cysteine HCl,L-半胱氨酸盐酸盐,L-半胱氨酸盐酸盐(无水物)

Target: Others, Endogenous Metabolite

L-Cysteine hydrochloride hydrate

Cat.No: TN5283

Synonym: L-Cysteine hydrochloride monohydrate,L-半胱氨酸盐酸盐一水物,L-半胱氨酸盐酸盐一水合物

Target: Others, Endogenous Metabolite

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