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。 | |||
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)。 | |||
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。 | |||
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)。 | |||
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。 | |||
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。 | |||
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。 | |||
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。 | |||
T10988L |
Degarelix acetate(214766-78-6 free base)
|
GNRH Receptor | GPCR/G Protein |
Degarelix acetate(214766-78-6 free base) 是促性腺激素释放激素受体 (GnRHR) 的竞争性可逆拮抗剂。 | |||
TP1307 |
Buserelin Acetate (57982-77-1 free base)
布舍瑞林,Buserelin Acetate |
GNRH Receptor | GPCR/G Protein |
Buserelin Acetate (57982-77-1 free base) (Buserelin Acetate) 是促性腺激素释放激素受体 (GnRHR) 的激动剂。 | |||
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 | |||
T17301 |
opigolix
|
Others | Others |
Opigolix is a Gonadotropin-releasing hormone receptor antagonist. | |||
T10988 |
Degarelix
|
GNRH Receptor | GPCR/G Protein |
Degarelix is a competitive and reversible gonadotropin-releasing hormone receptor (GnRHR) antagonist. | |||
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。 | |||
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. | |||
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。 | |||
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 | |||
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。 | |||
T68701 | Abarelix acetate | ||
Abarelix acetate is a synthetic third generation gonadotropin-releasing hormone receptor (GnRHR) antagonist. It increases histamine release from rat peritoneal mast cells in vitro and from a human skin model ex vivo. In vivo, abarelix decreases plasma luteinizing hormone (LH) levels six hours post-treatment in castrated rats, with levels returning to baseline within 24 hours.3 Abarelix (2 mg/kg) also transiently decreases plasma testosterone levels in intact rats, with levels returning to baseli... | |||
T72990 |
BAY 1214784
|
||
BAY 1214784是一种针对人促性腺激素释放激素受体(hGnRH-R)的高效、选择性口服活性拮抗剂,属于螺二氢吲哚衍生物化合物。该化合物能显著降低血浆促黄体激素水平,最高可达49%,同时显示出较低的药代动力学变异性和良好的耐受性,表现出研究子宫肌瘤的潜力。 | |||
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... | |||
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... | |||
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。 |