Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
TP1288 |
Fertirelin
|
Others | Others |
Fertirelin 是 GnRH 和 LH-RH 的类似物,可用于研究牛滤泡囊肿。 它是促性腺激素释放激素激动剂。 | |||
T1494 |
Alarelin Acetate
阿拉瑞林,Alarelin |
GNRH Receptor | GPCR/G Protein |
Alarelin Acetate 是一种合成的GnRH 激动剂。 | |||
T27837 |
Linzagolix
|
GNRH Receptor | GPCR/G Protein |
Linzagolix 是一种口服有活性的非多肽GnRH 拮抗剂。可用于研究子宫肌瘤、子宫腺肌症、子宫内膜异位症。 | |||
T3630 |
Relugolix
RVT-601,瑞卢戈利,TAK-385 |
GNRH Receptor | GPCR/G Protein |
Relugolix (RVT-601) 是口服有活性的非肽性促性腺激素释放激素的拮抗剂。同 TAK-013 相比,它对人和猴子的受体具有高亲和力和强拮抗活性,它们的 IC50值分别为0.33 nM 和0.32 nM。它可用于研究性激素依赖性疾病,如子宫肌瘤、子宫内膜异位症、前列腺癌等。 | |||
T11174 |
(R)-Elagolix
恶拉戈利,NBI-56418 |
GNRH Receptor | GPCR/G Protein |
(R)-Elagolix (NBI-56418) 是口服具有活性的、选择性高的非肽类促性腺激素释放激素受体短期有效拮抗剂 (KD = 54 pM)。 | |||
T5520 |
Cetrorelix Acetate
醋酸西曲瑞克,Cetrorelix |
GNRH Receptor | GPCR/G Protein |
Cetrorelix Acetate 是一种GnRH 受体的强效拮抗剂(IC50:1.21 nM)。 | |||
T4102 |
Goserelin acetate
醋酸戈舍瑞林,Fertilan,ICI-118630 acetate,Zoladex |
Apoptosis; GNRH Receptor | Apoptosis; GPCR/G Protein |
Goserelin acetate (Fertilan) 是一种促性腺激素释放激素 (GnRH/LHRH) 十肽类似物,能作为GnRH 激动剂。它可研究乳腺癌、上皮性卵巢癌和前列腺癌。 | |||
T5031 |
Elagolix sodium
NBI-56418 sodium,恶拉戈利钠 |
GNRH Receptor | GPCR/G Protein |
Elagolix sodium (NBI-56418 sodium) 是人GnRH 受体拮抗剂,其IC50=0.25 nM,Ki=3.7 nM。 | |||
T10217L |
Abarelix
R3827,阿巴瑞克,PPI 149 |
GNRH Receptor | GPCR/G Protein |
Abarelix (PPI 149) 是一种促性腺激素释放激素 (GnRH) 拮抗剂,用于前列腺癌研究。 | |||
T5520L |
Cetrorelix diacetate
NS-75A,醋酸西曲瑞克,SB-075 acetate,SB-075 diacetate,Cetrorelix acetate,NS-75A diacetate |
GNRH Receptor | GPCR/G Protein |
Cetrorelix diacetate (NS-75A) 是GnRH 受体的强效拮抗剂(IC50:1.21 nM)。 | |||
T21308 |
Histrelin
Supprelin LA,组氨瑞林,Histrelin Acetate |
Others | Others |
Histrelin (Supprelin LA) 是促性腺激素释放激素 (GnRH) 的九肽类似物,具有增加的效力。它被认为是 GnRH 激动剂。 Histrelin 用于治疗对激素敏感的男性前列腺癌和女性子宫肌瘤。 | |||
T22025 |
AG 045572
|
P450; GNRH Receptor | GPCR/G Protein; Metabolism |
AG 045572 是一种有效的 GnRH 受体拮抗剂,对人类和大鼠的 GnRH receptor 具有抑制作用, Ki 值分别为 6.0 nM 和 3.8 nM。AG 045572 通过 CYP3A 代谢并抑制睾酮。 | |||
TP2337 |
Ganirelix Acetate
|
GNRH Receptor | GPCR/G Protein |
Ganirelix Acetate 是一种促性腺激素释放激素 (GnRH) 受体拮抗剂。 | |||
TP1896L1 |
Kisspeptin 234 acetate(1145998-81-7 free base)
|
GPR; Kisspeptin | Endocrinology/Hormones; GPCR/G Protein |
Kisspeptin 234 acetate(1145998-81-7 free base) 是Kisspeptin 受体 (KISS1, GPR54) 拮抗剂; 是Kisspeptin-10 类似物。它抑制 Kisspeptin-10 对磷酸肌醇 (IP) (IC50 = 7 nM) 的刺激和促性腺激素释放激素 (GnRH) 的释放。 | |||
T23412 |
T 98475
|
Others | Others |
gonadotropin-releasing hormone (GnRH, LHRH) receptor antagonist,orally active | |||
T37003 |
GnRH antagonist 2
|
||
GnRH antagonist 2 (formula I) is a potent GnRH receptor antagonist with valuable applications in endometriosis research[1]. | |||
T10475 |
BAY-784
|
Others | Others |
BAY-784 is a gonadotropin-releasing hormone receptor (GnRH-R) antagonist (IC50s: 21 and 24 nM for human and rat GnRH-R). | |||
T76351 | [D-Ala6]-LH-RH | ||
[D-Ala6]-LH-RH,一种黄体激素释放激素(LHRH)模拟物,充当GnRH受体的激动剂。 | |||
T76350 |
[D-Glp1,D-Phe2,D-Trp3,6]-LH-RH
|
||
[D-Glp1,D-Phe2,D-Trp3,6]-LH-RH 是一种黄体激素释放激素 (LHRH) 类似物,可作为 GnRH 受体拮抗剂。 | |||
TP1896 |
Kisspeptin 234
|
||
kisspeptin receptor (KISS1, GPR54) antagonist; kisspeptin-10 analog. Inhibits kisspeptin-10 stimulation of inositol phosphate (IP) (IC50 = 7 nM) and release of gonadotrophin-releasing hormone (GnRH). | |||
T76348 |
[D-Lys6]-LH-RH
|
||
[D-Lys6]-LH-RH 是一种黄体激素释放激素 (LHRH) 类似物,可作为GnRH 受体激动剂。 | |||
T28795 |
SKI2496
SKI 2496,SKI-2496 |
||
SKI2496 is a potent and orally bioavailableantagonist of Gonadotropin-Releasing Hormone Receptor (hGnRHR IC50 = 0.46 nM; max. LH inh. inh. (%, h)= 84%, 12h; LH inh. (24h) = 76%.). SKI2496 exhibits more selective antagonistic activity toward the human GnRH | |||
T69383 |
NBI-42902
|
||
NBI-42902 is a potent inhibitor of peptide radioligand binding to the human GnRH receptor (K(i) = 0.56 nm). Tritiated NBI-42902 binds with high affinity (K(d) = 0.19 nm) to a single class of binding sites and can be displaced by a range of peptide and nonpeptide GnRH receptor ligands. In vitro experiments demonstrate that NBI-42902 is a potent functional, competitive antagonist of GnRH stimulated IP accumulation, Ca(2+) flux, and ERK1/2 activation. It did not stimulate histamine release from rat... | |||
TP1936 |
RFRP-3(human)
RFRP 3 (human) |
||
Agonist of the NPFF1 receptor (IC50 = 0.7 nM for inhibition of forskolin-induced cAMP production). Homolog of gonadotropin-inhibitory hormone (GnIH); inhibits activity of gonadotropin-releasing hormone (GnRH) neurons. | |||
T70309 | Dicetrorelix pamoate | ||
Dicetrorelix pamoate is a synthetic decapeptide with gonadotropin-releasing hormone (GnRH) antagonistic activity. GnRH induces the production and release of luteinizing hormone (LH) and follicle stimulating hormone (FSH) from the gonadotrophic cells of the anterior pituitary. Due to a positive estradiol (E2) feedback at midcycle, GnRH liberation is enhanced resulting in an LH-surge. This LH-surge induces the ovulation of the dominant follicle, resumption of oocyte meiosis and subsequently lutein... | |||
T76436 |
[MePhe7]-Neurokinin B
|
||
[MePhe7]-Neurokinin B为NK-3受体(NK3R)激动剂,具有3 nM的IC50值。通过激活神经激肽3受体,[MePhe7]-Neurokinin B能够调节脉冲促性腺激素释放激素(GnRH)的分泌,成为调控该过程的潜在调节剂。 | |||
T70775 |
Zoptarelin doxorubicin
|
||
Zoptarelin doxorubicin, also known as AEZS-108, is an LHRH agonist. Zoptarelin doxorubicin is a peptide agonist of the gonadotropin releasing hormone-1 receptor (GnRH-1R) that is conjugated to the anthracycline antibiotic doxorubicin with potential antineoplastic activity. Zoptarelin doxorubicin binds to GnRH-1Rs, which may be highly expressed on endometrial and ovarian tumor cell membrane surfaces, and is internalized. Once inside the cell, the doxorubicin moiety of this agent intercalates in... | |||
T81485 |
Phoenixin-14 TFA
PNX-14 TFA |
||
Phoenixin-14 (PNX-14) TFA 是具抗焦虑、心脏保护及神经保护效果的穿透大脑屏障神经肽。它通过上调GnRH受体mRNA调控垂体促性腺激素分泌,并促进胰岛素释放。此外,Phoenixin-14 TFA保护小鼠免受缺血/再灌注(IR)伤害,通过降低ROS、提高GSH减缓氧化应激。 | |||
T76048 |
TAK-683 acetate
|
||
TAK-683 acetate是一种高效的KISS1R激动剂(IC50=170 pM),改善了代谢稳定性。作为九肽metastin的类似物,对人和大鼠的EC50值分别为0.96 nM和1.6 nM。该化合物通过消耗下丘脑GnRH,能够降低血浆FSH、LH、睾酮水平,展示了对研究激素依赖性前列腺癌的潜力。 | |||
T69492 |
Ozarelix
|
||
Ozarelix is a fourth generation GnRH antagonist, induces apoptosis in hormone refractory androgen receptor negative prostate cancer cells modulating expression and activity of death receptors. Mechanistically, LHRH antagonists exert rapid inhibition of luteinizing hormone and follicle stimulating hormone with an accompanying rapid decrease in sex hormones and would therefore be expected to be effective in a variety of hormonally dependent disease states including ovarian cancer, prostate cancer,... | |||
T76047 |
TAK-683 TFA
|
||
TAK-683 TFA是一种高效的全KISS1R激动剂(IC50=170 pM),拥有较好的代谢稳定性,是九肽metastin的类似物,对KISS1R有激动效应,其对人和大鼠EC50值分别为0.96 nM和1.6 nM。TAK-683 TFA能够降低下丘脑GnRH水平,进而减少血浆FSH、LH、睾酮的浓度,显示出对激素依赖性前列腺癌研究的可能性。 | |||
T35794 |
Kisspeptin-54 (human) (trifluoroacetate salt)
|
||
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-5... |