Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
TP1174 |
Endothelin-2 (49-69), human
Human endothelin-2,Endothelin-2, human,Endothelin-2 (human, canine),人内皮素2 |
Others | Others |
Endothelin-2 (49-69), human (Human endothelin-2) 是一种由 21 个氨基酸组成的血管活性肽。它可与 G 蛋白连接的跨膜受体,ET-RA 和ET-RB 结合。 | |||
TP2143 |
Endothelin-2 (49-69), human TFA
Endothelin-2 (49-69) (human, canine) TFA,Human endothelin-2 TFA |
Others | Others |
Endothelin-2 (49-69), human (TFA) is a 21-amino acid vasoactive peptide that binds to ET-RA and ET-RB. | |||
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。 | |||
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。 | |||
T7391 |
SAR407899
|
ROCK; Rho | Cell Cycle/Checkpoint; Cytoskeletal Signaling; Stem Cells |
SAR407899 是一种选择性的 ATP 竞争性ROCK 抑制剂,对ROCK-2的IC50值为 135 nM,对人和大鼠ROCK-2的Ki 值分别为 36 和 41 nM。它是 Rho 激酶抑制剂,有效抑制 endothelin-1 诱导的肾阻力动脉收缩。 | |||
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。 | |||
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]. | |||
TP2246 |
Endothelin-1 (1-15), amide, human
|
Others | Others |
Endothelin-1 is one of the there isoforms of endothelin (identified as ET-1, -2, -3) with varying regions of expression and binding to at least four known endothelin receptors, ETA, ETB1, ETB2 and ETC. | |||
T36007 |
Nebentan
|
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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... | |||
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。 | |||
T38167 |
BE-24566B
|
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BE-24566B is a polyketide fungal metabolite originally isolated fromS. violaceusniger.1It is active againstB. subtilis,B. cereus,S. aureus,M. luteus,E. faecalis, andS. thermophilus(MICs = 1.56, 1.56, 1.56, 1.56, 3.13, and 3.13 μg/ml, respectively). BE-24566B is an endothelin (ET) receptor antagonist (IC50s = 11 and 3.9 μM for ETAand ETBreceptors, respectively).2 1.Kojiri, K., Nakajima, S., Fuse, A., et al.BE-24566B, a new antibiotic produced by Streptomyces violaceusnigerJ. Antibiot. (Tokyo)48(1... | |||
T73877 | BQ-123 TFA | ||
BQ-123 TFA 是一种高效、选择性内皮素 A(ETA)受体拮抗剂,IC50值为 7.3 nM,Ki 值为 25 nM。BQ-123 TFA 抑制内皮素-1 介导的人肺动脉平滑肌细胞增殖,降低高血压大鼠血压。 | |||
T76305 |
[Ala2] Endothelin-3, human
|
||
[Ala2] Endothelin-3, human 为ET-3的线性类似物,其结构中的Cys残基被Ala所替代。ET-3是由人体横纹肌肉瘤细胞系产生,且仅在此细胞系中表达的一种具有血管活性的肽。在非肌肉来源的肉瘤细胞系中不表达。该肽能够作为旁分泌因子,促进内皮细胞迁移。 | |||
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 | |||
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。 |