Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T25394 |
ETB067
ETB-067,ETB 067 |
||
ETB067, an H-89 analog, acts as a PKA and AKT1 inhibitor with specificity on no longer inhibiting CAMK2B and neither affecting viability of mice nor causing any detectable tissue damage at the dose given. | |||
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。 | |||
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。 | |||
T73099 |
Etbicyphat
Trimethylopropane phosphate |
||
Etbicyphat (Trimethylopropane phosphate)作为一种GABA(A)受体竞争性拮抗剂展现出显著效果。通过诱发海马体CA1神经元的类似癫痫的活动并与GABA(A)-benzodiazepine受体结合,Etbicyphat的作用机制得到了阐述。 | |||
T10595 |
BQ-788
BQ788 |
Endothelin Receptor | GPCR/G Protein |
BQ-788 是一种具有选择性和有效性的 ETB 受体拮抗剂,具有潜在的高血压活性,抑制 ET-1 与 ETB 受体结合,抑制外源性 ET-1 诱导的冠状动脉灌注压升高。 | |||
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。 | |||
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。 | |||
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。 | |||
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。 | |||
T19309L1 |
Endothelin 1 (swine, human) acetate
Endothelin 1 (swine, human) acetate(117399-94-7 free base) |
Endothelin Receptor | GPCR/G Protein |
Endothelin 1 (swine, human) acetate(117399-94-7 free base) 是一种合成肽,其序列为人和猪内皮素 1。它是一种有效的内源性血管收缩剂,通过两种类型的受体 ETA 和 ETB 起作用。 | |||
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... | |||
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。 | |||
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)。 | |||
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)。 | |||
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)。 | |||
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。 | |||
T12382 | PD-159020 | Others | Others |
PD-159020 is a non-selective antagonist of ETA/ETB(hETA and hETB with IC50s of 30 and 50 nM , respectively). | |||
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。 | |||
TP2120 |
Sarafotoxin S6c
|
||
Highly selective ETB endothelin receptor agonist (Ki values are 0.29 and 28000 nM at ETB and ETA receptors respectively). | |||
T14068 |
A-192621
|
Others | Others |
A-192621 is a potent, nonpeptide, orally active and selective endothelin B (ETB) receptor antagonist with an IC50 of 4.5 nM and a Ki of 8.8 nM. A-192621 promotes apoptosis in PASMCs and it also causes elevation of arterial blood pressure and an elevation | |||
T10595L |
BQ-788 sodium salt
|
Others | Others |
BQ-788 sodium salt is a potent and selective antagonist of ETB receptor(ETB receptors with an IC50 of 1.2 nM in human Girrardi heart cells). | |||
TP1706 |
BQ-3020 TFA (143113-45-5 free base)
BQ-3020 TFA |
||
BQ-3020 (TFA) is a selective ETB receptor agonist that inhibits [125I] et-1 binding to the ETB receptor in the cerebellum with a 0.2nm IC50, causing vasoconstriction. | |||
T15595 |
IRL-1620
|
Others | Others |
IRL-1620 is an effective and selective agonist of endothelin receptor type B (ETB) (Ki: 16 pM). | |||
T17064 |
Tezosentan
RO 610612 |
Others | Others |
Tezosentan is an antagonist of the endothelin receptor (pA2s: 9.5, 7.7 for ETA and ETB receptors, respectively). | |||
T9621 |
N-(6-chloro-5-(2-Methoxyphenoxy)-2-(pyridin-4-yl)pyriMidin-4-yl)-5-Methylpyridine-2-sulfonamide
|
Others | Others |
N-(6-chloro-5-(2-Methoxyphenoxy)-2-(pyridin-4-yl)pyriMidin-4-yl)-5-Met 抑制内皮素与CHO 细胞膜上人ETA 受体和人ETB 受体的的结合,IC50分别为268nM 和 1810nM。 | |||
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 | |||
TP2262 |
IRL-1038
|
Others | Others |
ETB endothelin receptor antagonist | |||
T36007 |
Nebentan
|
||
Nebentan (YM598) is a potent, selective and orally active non-peptide endothelin ETA receptor antagonist through the modification of Bosentan . Nebentan 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 inhibits the specific binding of [125I] endothelin-1 to endothelin ETA and ETB receptors in a concentration dep... | |||
TP2099 |
[Ala1,3,11,15]-Endothelin
|
||
Selective ETB endothelin receptor agonist (IC50 values are 0.33 and 2200 nM for displacing [125I]-ET-1 from ETB and ETA receptors respectively). | |||
TP1465 |
IRL-1620 TFA (142569-99-1 free base)
IRL-1620 TFA |
||
IRL-1620 (TFA) is a potent selective endothelin receptor B (ETB) agonist with a Ki value of 16pm. | |||
T10351 |
Aprocitentan D4
ACT-132577 D4 |
Others | Others |
Aprocitentan D4 (ACT-132577 D4) is a deuterium-labeled Aprocitentan. Aprocitentan is a major and pharmacologically active metabolite of Macitentan. Aprocitentan is a dual ETA/ETB antagonist (IC50s: 3.4 nM and 987 nM; pA2s: 6.7 and 5.5). | |||
T75771 |
BQ-3020 TFA
|
||
BQ-3020 (TFA) 是一种选择性的内皮素受体 B (ETBreceptor) 激动剂,抑制小脑 [125I]ET-1 与 ETB 受体结合,IC50值为 0.2 nM。BQ-3020 (TFA) 可导致血管收缩。 | |||
T11935 |
Macitentan (n-butyl analogue)
|
Others | Others |
Macitentan n-butyl analogue, a derivative of Macitentan, functions as an orally active dual antagonist targeting both endothelin ETA and ETB receptors. This compound shows promise for treating idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH), leveraging its non-peptide structure for potential therapeutic applications. | |||
T27647 |
J-104132
L753037,L 753037,J104132,J 104132,L-753037 |
||
J-104132 is a potetn and selective endothelin A/B receptor antagonist (Ki: cloned human ETA = 0.034 nM; cloned human ETB = 0.104 nM) . In vitro, J-104132 is a potent antagonist of ET-1-induced accumulation of [3H]inositol phosphates in Chinese hamster ova | |||
T75772 |
[Ala1,3,11,15]-Endothelin (53-63) (TFA)
|
||
[Ala1,3,11,15]-Endothelin (53-63) (TFA) 是一种ETB 激动剂。[Ala1,3,11,15]-Endothelin (53-63) (TFA) 对 ETB 具有选择性,IC50值范围为 0.33 nM 至 0.61 nM。[Ala1,3,11,15]-Endothelin (53-63) (TFA) 可用于血管收缩的研究。 | |||
T19309 |
Endothelin 1 (swine, human)
|
Others | Others |
Endothelin 1 (swine, human), a synthetic peptide mirroring the sequence of both human and swine Endothelin 1, functions as a robust endogenous vasoconstrictor by interacting with two receptor types, ETA and ETB. | |||
T11934 |
Macitentan-d4
Macitentan D4,ACT-064992 D4 |
Endothelin Receptor | GPCR/G Protein |
Macitentan-d4 (ACT-064992 D4) 是一种 Macitentan 氘代物,可被当作非多肽 ETA 和 ETB (内皮素受体)双拮抗剂。Macitentan-d4 比 Macitentan 毒性更低,半衰期更长,可用于研究由内皮素受体介导介导的疾病。 | |||
T75249 |
IRL-1620 TFA
|
||
IRL-1620 (TFA) 是高效,选择性的内啡肽受体 (endothelin receptor) B 型激动剂,Ki 值为 16 pM。 | |||
T78096 |
BQ-3020 ammonium
|
Endothelin Receptor | GPCR/G Protein |
BQ-3020 ammonium 是一种内皮素受体(endothelin receptor)(ETB receptor) 激动剂。它在阻断[125I]ET-1与猪小脑ETB受体的结合实验中显示出IC50值为0.2 nM。此外,BQ-3020 ammonium能够引致兔肺动脉血管收缩以及猪膀胱颈的松弛,因此可作为心血管疾病研究的工具。 | |||
T36878 |
Sclerotiorin
|
||
Sclerotiorin is a natural product isolated primarily from Penicillium species. It inhibits soybean lipoxygenase-1 with an IC50 value of 4.2 μM. Sclerotiorin also exhibits a number of other activities including inhibition of cholesterol ester transfer protein (IC50 = 19.4 μM),, inhibition of Grb2-Shc interaction (IC50 = 22 μM),, and antagonism of endothelin receptors (IC50 = 114 and 152 μM for human ETA and ETB, respectively). | |||
T75807 |
Sarafotoxin S6a TFA
|
||
Sarafotoxin S6a TFA 是一种 Sarafotoxin 类似物,是一种内皮素受体 (endothelin receptor) 激动剂,具有与 Endothelin-3 相似的 ETA/ETB 选择性。Sarafotoxin S6a TFA 诱导猪冠状动脉的 EC50值为 7.5 nM。 | |||
T22540 |
Ac-Endothelin-1 (16-21), human
|
Others | Others |
ENDOTHELIN-1 (ET-1), the principal peptide of the endothelin family, has been shown to have a variety of biological activities in both vascular and nonvascular tissues. The C-terminal fragment, which is a highly conserved sequence in the peptides of t | |||
T76081 |
Endothelin 1 (swine, human), Alexa Fluor 488-labeled
|
||
Endothelin 1 (swine, human), Alexa Fluor 488-labeled 是标记了488 荧光的 Endothelin 1 合成肽。Endothelin 1 (swine, human) 是具有人和猪内皮素 1 序列的合成肽,是有效的内源性血管收缩剂。Endothelin 1 通过两种类型受体 ETA 和 ETB 发挥作用。 | |||
T75731 |
Endothelin 1 (swine, human) (TFA)
|
||
Endothelin 1 (swine, human) (TFA) 是具有人和猪内皮素 1 序列的合成肽,是有效的内源性血管收缩剂。Endothelin 1 通过两种类型受体 ETA 和 ETB 发挥作用。 | |||
T73820 |
Bosentan-d4
|
||
Bosentan-d4 是 Bosentan 的氘代物。Bosentan 是一种有效的endothelin-1 (ET)拮抗剂,在人的 SMC 细胞中,作用于ETA 和ETB 受体,Ki 值分别为 4.7 nM 和 95 nM。 | |||
T30501 |
BMS-193884
BMS193884,BMS 193884 |
||
BMS-193884 is an oral endothelin antagonist for the treatment of congestive heart failure (CHF) and pulmonary arterial hypertension. |