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32

抑制剂 & 化合物

2

天然产物

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Cat. No. Product Name Target Signaling Pathways
T17103 TM-N1324

Others; GHSR GPCR/G Protein; Others
TM-N1324 是一种 GPR39 激动剂。 TM-N1324 在没有和存在 Zn2+ 的情况下分别以 280 nM 和 9 nM 的高效率和效力激活人 GPR39。 TM-N1324 对鼠 GPR39 表现出相似的效力,EC50 分别为 180 nM 和 5 nM。
TQ0022 Capromorelin Tartrate

卡普瑞林酒石酸盐,CP 424391-18

GHSR GPCR/G Protein
Capromorelin Tartrate (CP 424391-18) 是口服有活性的 growth hormone secretagogue receptor 有效激动剂,能够作用于 hGHS-R1a(Ki:7 nM)。
T4648 TC-G-1008

GPR39-C3

GHSR GPCR/G Protein
TC-G-1008 (GPR39-C3) 是一种口服有活性的 GPR39激动剂,可作用于大鼠受体(EC50: 0.4 nM)和人类受体(EC50:0.8 nM)的。
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)。
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。
T7112 Ibutamoren Mesylate

MK-0677,伊布莫仑甲磺酸盐,MK-677

GHSR GPCR/G Protein
Ibutamoren Mesylate (MK-0677) 是非肽段类生长激素促分泌素受体 (GHSR) 激动剂,也是一种口服有活性的生长激素 (GH) 促分泌素。
T1088 Repaglinide

AG-EE 388 ZW,AG-EE 623ZW,瑞格列奈

Potassium Channel; PPAR DNA Damage/DNA Repair; Membrane transporter/Ion channel; Metabolism
Repaglinide (AG-EE 623ZW) 是一种能够用于2 型糖尿病的胰岛素促分泌剂。
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。
T11719 JMV 2959 hydrochloride (925238-89-7 free base)

JMV 2959 hydrochloride

GHSR GPCR/G Protein
JMV 2959 hydrochloride (925238-89-7 free base) 是一种生长激素促分泌素受体 1a 型 (GHS-R1a) 拮抗剂,在 LLC-PK1 细胞中的 IC50 为 32±3 nM。
TP2328L CJC-1295 acetate(863288-34-0 free base)

DAC:GRF acetate

GHSR GPCR/G Protein
CJC-1295 acetate(863288-34-0 free base) (DAC:GRF acetate) 是生长激素释放激素 (GHRH)(也称为生长激素释放因子 (GRF))和生长激素促分泌素 (GHS) 的合成类似物。
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。
T11798 L-692429

MK-0751

GHSR; GPCR19 GPCR/G Protein
L-692429 (MK-0751) 是一种有效的非肽基生长激素促分泌素 (GHS) 激动剂,是一种苯并内酰胺的衍生物,可逆转糖皮质激素对 GH 分泌的抑制。L-692429 对 G 蛋白偶联受体 (G protein-coupled receptor)具有很高的亲和力,可用于研究肢端肥大症和肥胖。
T32435 L 163255

L-163255,L163255,L163,255,L-163,255,L 163,255

L 163255 is a type of growth hormone secretagogue (GHS).
T32507 L-739943

L 739943,L739943

L-739943 is a growth hormone secretagogue.
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.
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.
T31734 BMS-604992

EX1314,EX-1314 HCl,EX-1314,BMS604992,EX-1314 hydrochloride, BMS-604992,EX 1314

EX-1314 (BMS-604992) is a growth hormone secretagogue receptor (GHSR) agonist.
T30513 BMS-317180

BMS317180

BMS-317180 is a potent, novel, orally effective growth hormone secretagogue (GHS) that shows an excellent safety profile in preclinical studies. The compound was advanced into clinical development.
T19548 Repaglinide D5

AG-EE 623ZW D5,瑞格列奈 D5

Others Others
Repaglinide D5 is deuterium labeled Repaglinide. Repaglinide is an insulin secretagogue for treatment type-2 diabetes mellitus.
T11719L JMV 2959

Others Others
JMV 2959 is an antagonist of growth hormone secretagogue receptor type 1a (GHS-R1a) (IC50: 32 nM).
TP1261 Alexamorelin Met 1

(D-Mrp)-Ala-Trp-(D-Phe)

Alexamorelin Met 1 is one of the metabolites of alexamorelin. The heptapeptide Ala-His-D-2-methyl-Trp-Ala-Trp-D-Phe-Lys-NH2 (Alexamorelin) is a synthetic molecule which inhibits growth hormone secretagogue binding in vitro.
T38959 BMS-604992 dihydrochloride

EX-1314 dihydrochloride,BMS-604992 dihydrochloride

BMS-604992 (EX-1314) dihydrochloride is a selective and orally active small-molecule agonist of the growth hormone secretagogue receptor (GHSR). It exhibits high-affinity binding (k i = 2.3 nM) and potent functional activity (EC 50 = 0.4 nM). Furthermore, BMS-604992 dihydrochloride has been shown to stimulate food intake in rodents.
T40876 BMS-604992 free base

BMS-604992 free base,EX-1314 free base

BMS-604992 (EX-1314) free base is a selective, orally active small-molecule growth hormone secretagogue receptor (GHSR) agonist. It exhibits high-affinity binding (k i = 2.3 nM) and potent functional activity (EC 50 = 0.4 nM). Moreover, BMS-604992 free base has the ability to stimulate food intake in rodents.
T76318 GHRF, porcine

GHRF, porcine 是一种生长激素释放激素 (GHRH) 多肽 (porcine)。GHRF, porcine 与 GHRHR 受体结合并促进生长激素的释放。
TP1768 Exendin-3

Exendin-3 is a biologically active peptides isolated from venoms of the Gila monster lizards, Heloderma horridurn . Exendin-3 is a pancreatic secretagogue, which is a member of the glucagon family. It is found in the venom of Heloderma horridurn, which i
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)
T22036 Arylquin 1

Arylquin 1 是一种前列腺-凋亡-反应-4(Par-4)促分泌剂,靶向波形蛋白诱导 Par-4 分泌。Arylquin 1 通过诱导溶酶体膜通透性 (LMP) 诱导癌细胞非凋亡性细胞死亡。
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。
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。
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...
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。

化合物

TM-N1324
Cat.No: T17103
Synonym:
Target: Others, GHSR
Capromorelin Tartrate
Cat.No: TQ0022
Synonym: 卡普瑞林酒石酸盐,CP 424391-18
Target: GHSR
TC-G-1008
Cat.No: T4648
Synonym: GPR39-C3
Target: GHSR
PF-5190457
Cat.No: T16508
Synonym: PF-05190457
Target: GHSR
Anamorelin
Cat.No: T10319
Synonym: RC-1291,阿拉莫林,ONO-7643
Target: GHSR
Ibutamoren Mesylate
Cat.No: T7112
Synonym: MK-0677,伊布莫仑甲磺酸盐,MK-677
Target: GHSR
Repaglinide
Cat.No: T1088
Synonym: AG-EE 388 ZW,AG-EE 623ZW,瑞格列奈
Target: Potassium Channel, PPAR
AnaMorelin hydrochloride
Cat.No: T7225
Synonym: RC-1291 hydrochloride,阿拉莫林盐酸盐,ONO-7643 hydrochloride
Target: GHSR
JMV 2959 hydrochloride (925238-89-7 free base)
Cat.No: T11719
Synonym: JMV 2959 hydrochloride
Target: GHSR
CJC-1295 acetate(863288-34-0 free base)
Cat.No: TP2328L
Synonym: DAC:GRF acetate
Target: GHSR
Relamorelin
Cat.No: T34281
Synonym: BIM28131,RM 131,BIM-28131,BIM-28163,BIM 28163,BIM28163,BIM 28131
Target: GHSR
L-692429
Cat.No: T11798
Synonym: MK-0751
Target: GHSR, GPCR19
L 163255
Cat.No: T32435
Synonym: L-163255,L163255,L163,255,L-163,255,L 163,255
Target:
L-739943
Cat.No: T32507
Synonym: L 739943,L739943
Target:
SM-130686
Cat.No: T28812
Synonym: SM 130686,SM130,686,SM 130,686
Target:
PF-04628935
Cat.No: T28366
Synonym: PF 04628935,PF 4628935,PF4628935,PF04628935,PF-4628935
Target:
BMS-604992
Cat.No: T31734
Synonym: EX1314,EX-1314 HCl,EX-1314,BMS604992,EX-1314 hydrochloride, BMS-604992,EX 1314
Target:
BMS-317180
Cat.No: T30513
Synonym: BMS317180
Target:
Repaglinide D5
Cat.No: T19548
Synonym: AG-EE 623ZW D5,瑞格列奈 D5
Target: Others
JMV 2959
Cat.No: T11719L
Synonym:
Target: Others
Alexamorelin Met 1
Cat.No: TP1261
Synonym: (D-Mrp)-Ala-Trp-(D-Phe)
Target:
BMS-604992 dihydrochloride
Cat.No: T38959
Synonym: EX-1314 dihydrochloride,BMS-604992 dihydrochloride
Target:
BMS-604992 free base
Cat.No: T40876
Synonym: BMS-604992 free base,EX-1314 free base
Target:
GHRF, porcine
Cat.No: T76318
Synonym:
Target:
Exendin-3
Cat.No: TP1768
Synonym:
Target:
AZ-GHS-22
Cat.No: T37412
Synonym:
Target:
Arylquin 1
Cat.No: T22036
Synonym:
Target:
Macimorelin acetate
Cat.No: T68276
Synonym: EP-1572 acetate ; AEZS-130 acetate,AEZS-130 acetate,EP-1572 acetate
Target:
des-​Gln14-​Ghrelin TFA
Cat.No: T75928
Synonym:
Target:
Relamorelin acetate
Cat.No: T39236
Synonym: Relamorelin acetate,RM-131 acetate,BIM-28131acetate
Target:
JMV3002
Cat.No: T35793
Synonym: JMV3002
Target:
Relamorelin TFA
Cat.No: T75262
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
TN1128 Bruceine E

Others Others
Bruceine E 是从 B. javanica 种子中分离得到的,具有降血糖作用。 Bruceine E 可用于作为胰岛素促分泌剂的研究。
TN2050 Peonidin-3-O-glucoside chloride

Peonidin 3-Glucoside Chloride

Free radical scavengers oxidation-reduction
Peonidin-3-O-glucoside chloride (Peonidin 3-Glucoside Chloride) 是一种具有自由基清除活性的花青素,可用于作为胰岛素促分泌剂的研究。

天然产物

Bruceine E
Cat.No: TN1128
Synonym:
Target: Others
Peonidin-3-O-glucoside chloride
Cat.No: TN2050
Synonym: Peonidin 3-Glucoside Chloride
Target: Free radical scavengers
TargetMol Loading
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