Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T5458 |
Darusentan
Lu-135252,达卢生坦 |
Endothelin Receptor | GPCR/G Protein |
Darusentan (Lu-135252) 是内皮素受体 A (ET-A) 受体选择性拮抗剂,能够作用于 ET-A 受体(Ki:1.4 nM)及ET-B 受体(Ki:184 nM),对 ETA 受体的选择性大于 ETB 受体的100以上。它在大鼠主动脉血管平滑肌细胞膜中竞争结合放射性标记的内皮素(Ki:13 nM)。 | |||
T3194 |
Ro 46-2005
|
Endothelin Receptor | GPCR/G Protein |
Ro 46-2005是新型非肽类内皮素拮抗剂,能够抑制人血管平滑肌细胞(ETA 受体)(IC50:220 nM)。 | |||
T2561 |
Macitentan
马西替坦,ACT-064992 |
Apoptosis; Endothelin Receptor | Apoptosis; GPCR/G Protein |
Macitentan (ACT-064992) 是一种内皮素受体拮抗剂,用于治疗肺动脉高压。 | |||
T5355 |
Sparsentan
RE-021,DARA-a |
RAAS; Endothelin Receptor | Endocrinology/Hormones; GPCR/G Protein |
Sparsentan (DARA-a) 是一种具有高度选择的血管紧张素 II (Ki:0.8 nM)和内皮素 A 受体(Ki:9.3 nM)的双重拮抗剂。 | |||
T0750 |
Sulfisoxazole
NU-445,磺胺二甲异唑,Sulfafurazole,磺胺异恶唑 |
Endothelin Receptor; Antibacterial; Antibiotic; Autophagy | Autophagy; GPCR/G Protein; Microbiology/Virology |
Sulfisoxazole (Sulfafurazole) 是一种内皮素受体拮抗剂,是磺胺类抗生素。它靶向内皮素受体 A,抑制乳腺癌外显子释放。 | |||
T2026 |
CYM5442
|
S1P Receptor; LPL Receptor | GPCR/G Protein |
CYM5442 是高选择性和口服活性的鞘氨醇 1-磷酸受体激动剂,EC50为 1.35 nM。它激活依赖 S1P1的 p42/p44-MAPK 磷酸化,具有视网膜神经保护作用,可轻松穿过中枢神经系统。 | |||
T3474 |
RO 46-8443
|
Endothelin Receptor | GPCR/G Protein |
Ro 46-844 是选择性非肽内皮素受体拮抗剂。它对ETB(IC50: 34-69 nM) 的选择性比ETA 受体 (IC50: 6800 nM) 高的100倍以上。 | |||
T6258 |
Zibotentan
ZD4054 |
Apoptosis; Endothelin Receptor | Apoptosis; GPCR/G Protein |
Zibotentan (ZD4054) 是一种选择性的,具有口服活性的内皮素 A (ETA) 受体拮抗剂,Ki 为 13 nM。它具有抗癌作用,可研究去势抵抗性前列腺癌。 | |||
T6792 |
BQ-123
BQ123 |
Endothelin Receptor | GPCR/G Protein |
BQ-123 是高效的内皮素 A(ETA)受体选择性拮抗剂,其IC50=7.3 nM,Ki=25 nM。它能够降低高血压大鼠血压,抑制内皮素-1 介导的人肺动脉平滑肌细胞增殖。 | |||
T6264 |
Bosentan
Actelion,波生坦,Ro 47-0203,Benzenesulfonamide |
Endothelin Receptor | GPCR/G Protein |
Bosentan (Benzenesulfonamide) 是 endothelin-1 (ET)拮抗剂,在人的 SMC 细胞中,它能够作用于 ETA 受体(Ki:4.7 nM)和 ETB 受体(Ki:95 nM)。 | |||
TQ0282 |
Avosentan
SPP-301,Ro 67-0565,阿伏生坦 |
Endothelin Receptor | GPCR/G Protein |
Avosentan 是有效的内皮素受体(ETA)拮抗剂。 | |||
T1655 |
Ambrisentan
BSF-208075,BSF 208075,安倍生坦,LU 208075 |
Endothelin Receptor | GPCR/G Protein |
Ambrisentan (BSF 208075) 是 ET A 型受体选择性拮抗剂。 | |||
TQ0259 |
Atrasentan
A-147627,(+)-A 127722,阿曲生坦,ABT-627 |
Endothelin Receptor | GPCR/G Protein |
Atrasentan (ABT-627) 是内皮素受体 (endothelin receptor) 拮抗剂,能够抑制 ETA 的活性(IC50:0.0551 nM)。 | |||
T6265 |
Bosentan (hydrate)
波生坦水合物,Bosentan Hydrate,Benzenesulfonamide,Actelion,Ro 47-0203 |
Endothelin Receptor | GPCR/G Protein |
Bosentan hydrate (Ro 47-0203) 是endothelin-1 (ET)竞争性拮抗剂,在人SMC 细胞中,它能够作用于 ETA 受体(Ki:4.7 nM)和 ETB 受体(Ki:95 nM)。 | |||
T6672 |
Sitaxsentan sodium
西他生坦钠,TBC11251 sodium salt,TBC11251,Thelin,Sitaxentan sodium |
Endothelin Receptor | GPCR/G Protein |
Sitaxsentan sodium (TBC11251 sodium salt) 是 endothelin A receptor 选择性拮抗剂。 | |||
T7817 |
Aprocitentan
ACT-132577,N-[5-(4-溴苯基)-6-[2-[(5-溴-2-嘧啶基)氧基]乙氧基]-4-嘧啶基]氨基磺酰胺 |
Endothelin Receptor | GPCR/G Protein |
Aprocitentan (ACT-132577) 是一种 Macitentan 的主要活性代谢物。它是 ETA/ETB 的双重拮抗剂,其 pA2值分别为 6.7 和 5.5,IC50分别为 3.4 nM 和 987 nM。 | |||
TQ0270 |
Atrasentan hydrochloride
(+)-A 127722 hydrochloride,ABT-627 hydrochloride,盐酸阿曲生坦,A-147627 hydrochloride |
Endothelin Receptor | GPCR/G Protein |
Atrasentan hydrochloride (ABT-627 hydrochloride) 是内皮素 A 受体选择性拮抗剂,抑制内皮素 A 受体活性的IC50为 0.0551 nM。 | |||
T15596 | IRL 2500 | Endothelin Receptor | GPCR/G Protein |
IRL 2500 是内皮素受体的拮抗剂,对内皮素 A 受体和内皮素 B 受体的 IC50 分别为 1.3 和 94 nM。 | |||
T12924 |
Sitaxsentan
TBC-11251,IPI 1040 |
Endothelin Receptor | GPCR/G Protein |
Sitaxsentan (TBC-11251) 是选择性内皮素A (ETA) 受体拮抗剂。内皮素是一种有效的血管收缩剂。Sitaxsentan 阻断内皮素与其受体的结合,从而消除内皮素的有害作用。 | |||
T31605 |
Edonentan
BMS207940,BMS-207940,BMS 207940 |
Endothelin Receptor | GPCR/G Protein |
Edonentan 是一种有效的内皮素A(ETA)受体拮抗剂,可用于研究心脏衰竭。 | |||
T21790 |
BMS 182874 hydrochloride
|
Endothelin Receptor | GPCR/G Protein |
BMS 182874 hydrochloride 是一种非肽内皮素 (El) 受体拮抗剂。 | |||
T36008 |
Nebentan potassium
|
||
Nebentan potassium (YM598) is a potent, selective and orally active non-peptide endothelin ETA receptor antagonist through the modification of Bosentan . Nebentan potassium inhibits [125I] endothelin-1 binding to cloned human endothelin ETA and ETB receptor, with Ki of 0.697 nM and 569 nM, respectively[1]. YM598 can ameliorate the progression of cor pulmonale and myocardial infarction in vivo[2]. Nebentan potassium inhibits the specific binding of [125I] endothelin-1 to endothelin ETA and ETB re... | |||
TP2262L |
IRL-1038 acetate
IRL-1038 acetate(144602-02-8 Free base) |
Endothelin Receptor | GPCR/G Protein |
IRL-1038 acetate 是一种有效的 ETB 内皮素受体拮抗剂。 | |||
T34541 |
SB-209670
SB 209670 |
Endothelin Receptor | GPCR/G Protein |
SB-209670是一种选择性内皮素受体拮抗剂,能够抑制大鼠血管内皮和血管平滑肌中ET(B)受体的活性。 | |||
T22540L |
Ac-Endothelin-1 (16-21), human acetate
|
Others | Others |
Ac-Endothelin-1 (16-21), human acetate 是内皮素家族的主要肽,已被证明在血管和非血管组织中具有多种生物活性。 C-末端片段是 ET 家族肽中高度保守的序列,已显示可区分称为 ETA 和 ETB 的两种 ET 受体亚型,因为它仅激活后者。 | |||
T15595L |
IRL-1620 acetate
IRL-1620 acetate(142569-99-1 free base) |
Endothelin Receptor | GPCR/G Protein |
IRL-1620 acetate 是一种有效的特异性内啡肽 B 受体 (ETB) 激动剂,Ki 为 16 pM,相比于ETA,其Ki 为 19 μM。 | |||
T26841 |
BMS 182874
BMS182874,BMS-182874 |
Endothelin Receptor | GPCR/G Protein |
BMS 182874 是一种口服有效的高选择性内皮素受体 endothelin receptor ETA 拮抗剂,对 ETA 的 IC50 值为0.150 μM,对 ETA 的 Ki 值为0.055 μM。BMS 182874 能够在大鼠高血压模型中降低 Deoxycorticosterone acetate 诱导的动脉压,可用于研究心血管疾病。 | |||
TP2106L |
Urantide acetate(669089-53-6 free base)
|
Neurotensin Receptor | GPCR/G Protein |
Urantide acetate(669089-53-6 free base) 是一种选择性和竞争性的 urotensin-II (UT) 受体拮抗剂 (pKB = 8.3)。体外阻断 hU-II 诱导的胸主动脉收缩。对去甲肾上腺素或内皮素 1 诱导的收缩或乙酰胆碱诱导的松弛没有影响。在钙动员测定(在表达 hUT 受体的 CHO 细胞中)中表现为部分激动剂。 | |||
T4200 |
Sacubitril hemicalcium salt
AHU-377 (hemicalcium salt),LCZ696中间体,AHU377 calcium salt |
Neprilysin | Metabolism |
Sacubitril hemicalcium salt (AHU377 calcium salt) 是一种有效的 NEP 抑制剂,IC50=5 nM。它是研究心力衰竭药物 LCZ696 的组分之一。 | |||
T30572 |
BQ 485
BQ485,BQ-485 |
||
BQ 484 is an endothelin (ET) receptor antagonist. | |||
T22791 |
FR 139317
|
Others | Others |
highly potent and selective ETA endothelin receptor antagonist | |||
T10225 |
ABT-546
A-216546 |
Others | Others |
ABT-546 (A-216546) is a potent, highly selective, and active endothelin ETA receptor antagonist with a Ki of 0.46 nM for [125I]endothelin-1 binding to cloned human endothelin ETA. | |||
T22663 | CI 1020 | Others | Others |
endothelin-A receptor (ETA) antagonist | |||
TP1512 |
[Ala1,3,11,15]-Endothelin TFA
|
||
[Ala1,3,11,15]-Endothelin (TFA) is a highly selective for endothelin A (ETA) and endothelin B (ETB) receptor.[Ala1,3,11,15]-Endothelin is a selective ETB endothelin receptor agonist (IC50 values are 0.33 and 2200 nM for displacing [125I]-ET-1 from ET | |||
T61498 | Sulfisoxazole diethanolamine | ||
Sulfisoxazole diethanolamine, also known as Sulfafurazole diethanolamine, is a sulfonamide antibacterial compound with an oxazole substituent. It acts as an endothelin receptor antagonist, specifically targeting endothelin receptor A with an IC50 value of 0.60 μM and endothelin receptor B with an IC50 value of 22 μM. Additionally, Sulfisoxazole diethanolamine has been found to inhibit the release of breast cancer exosomes by specifically targeting endothelin receptor A [1] [2]. | |||
T28343 |
PD-156707
PD156707 |
||
PD-156707 is a selective antagonist of endothelin A receptor. | |||
T69791 |
Fandosentan
|
||
Fandosentan is an endothelin receptor antagonist. | |||
T27725 |
Kendomycin
TAN-2162,TAN 2162,TAN2162 |
||
Kendomycin is a proteasome inhibitor and endothelin receptor antagonist. It induces apoptosis in lymphoma. | |||
T70454 |
Cgs 27830
|
||
Cgs 27830 is an Endothelin Receptor Antagonist. | |||
T69338 | TBC 3711 | ||
TBC 3711 is an endothelin a receptor antagonist. | |||
T70727 |
BQ-610
|
||
BQ-610 is an Endothelin A receptor antagonist. | |||
T27776 |
L-749329
L749329,L 749329 |
||
L-749329 is a ligand of ET(A) and ET(B) endothelin receptor. | |||
T30515 |
BMS-346567
BMS346567,BMS 346567 |
||
BMS-346567 is a potent and selective dual angiotensin II and endothelin receptor antagonist. | |||
T15232 |
TBC3711
Endothelin Mordulator 1 |
Others | Others |
TBC3711 is an endothelin receptor modulator. It is used for the research of endothelin-mediated disorders. | |||
T69816 | ATZ-1993 | ||
ATZ-1993 is an Endothelin Receptor Antagonist. | |||
T24053 |
WS 009A
WS009 A,FR 901366,WS009A,WS-009A |
||
WS 009A is an antagonist of the endothelin receptor. | |||
T28683 |
SB234551
SB 234551,SB-234551 |
||
SB234551 is a selective antagonist of endothelin ETA receptor. | |||
T24081 |
WS 009B
WS-009B,FR 901367,WS009B |
||
WS 009B is an antagonist of the endothelin receptor. | |||
TP2262 |
IRL-1038
|
Others | Others |
ETB endothelin receptor antagonist | |||
T70452 |
PD 151242
|
||
PD 151242 is an endothelin receptor antagonist. |