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。 | |||
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。 | |||
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)。 | |||
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。 | |||
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。 | |||
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。 | |||
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. | |||
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. | |||
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. | |||
T11719L |
JMV 2959
|
Others | Others |
JMV 2959 is an antagonist of growth hormone secretagogue receptor type 1a (GHS-R1a) (IC50: 32 nM). | |||
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。 | |||
T22283 |
Capromorelin
卡普瑞林,CP 424,391,CP 424391-18 |
Others | Others |
Capromorelin, a member of the growth hormone secretagogue (GHS) class of drugs, is a ghrelin receptor agonist and a novel therapy for stimulation of appetite in dogs with Ki value of 7 nM for hGHS-R1a and EC50 value of 3 nM for rat pituicyte. Capromorelin | |||
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. | |||
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... | |||
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。 | |||
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) | |||
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... | |||
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。 | |||
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。 |