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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。 | |||
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。 | |||
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。 | |||
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。 | |||
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。 | |||
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。 | |||
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)。 | |||
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)。 | |||
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。 | |||
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。 | |||
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。 | |||
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。 | |||
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。 | |||
T36008 |
Nebentan potassium
YM598 |
Endothelin Receptor | GPCR/G Protein |
Nebentan potassium (YM598) 是一种具有口服活性和选择性的非肽类内皮素受体 (ETA receptor) 拮抗剂。Nebentan potassium 抑制肺动脉高压,可用于研究神经系统疾病和心血管疾病。 | |||
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。 | |||
T64084 |
Clazosentan
VML 588,AXV-034343,Ro 61-1790 |
Endothelin Receptor | GPCR/G Protein |
Clazosentan (Ro 61-1790) 是一种特异性内皮素 A (ETA)受体拮抗剂,抑制 ET-1 介导的血管痉挛。Clazosentan 可用于研究神经系统疾病和心血管疾病。 | |||
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。 | |||
T22791 |
FR 139317
|
Others | Others |
highly potent and selective ETA endothelin receptor antagonist | |||
T30572 |
BQ 485
BQ485,BQ-485 |
Others | Others |
BQ 484 is an endothelin (ET) 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
|
Others | Others |
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]. | |||
T69816 |
ATZ-1993
|
Others | Others |
ATZ-1993 is an Endothelin Receptor Antagonist. | |||
T69791 |
Fandosentan
|
Others | Others |
Fandosentan is an endothelin receptor antagonist. | |||
T28343 |
PD-156707
PD156707 |
Others | Others |
PD-156707 is a selective antagonist of endothelin A receptor. | |||
T15232 |
TBC3711
Endothelin Mordulator 1 |
Others | Others |
TBC3711 is an endothelin receptor modulator. It is used for the research of endothelin-mediated disorders. | |||
T27725 |
Kendomycin
TAN-2162,TAN 2162,TAN2162 |
Others | Others |
Kendomycin is a proteasome inhibitor and endothelin receptor antagonist. It induces apoptosis in lymphoma. | |||
T70454 |
Cgs 27830
|
Others | Others |
Cgs 27830 is an Endothelin Receptor Antagonist. | |||
T24081 |
WS 009B
WS-009B,FR 901367,WS009B |
Others | Others |
WS 009B is an antagonist of the endothelin receptor. | |||
T28683 |
SB234551
SB 234551,SB-234551 |
Others | Others |
SB234551 is a selective antagonist of endothelin ETA receptor. | |||
T24053 |
WS 009A
WS009 A,FR 901366,WS009A,WS-009A |
Others | Others |
WS 009A is an antagonist of the endothelin receptor. | |||
T70727 |
BQ-610
|
Others | Others |
BQ-610 is an Endothelin A receptor antagonist. | |||
T69338 |
TBC 3711
|
Others | Others |
TBC 3711 is an endothelin a receptor antagonist. | |||
T27776 |
L-749329
L749329,L 749329 |
Others | Others |
L-749329 is a ligand of ET(A) and ET(B) endothelin receptor. | |||
T70452 |
PD 151242
|
Others | Others |
PD 151242 is an endothelin receptor antagonist. | |||
T30515 |
BMS-346567
BMS346567,BMS 346567 |
Others | Others |
BMS-346567 is a potent and selective dual angiotensin II and endothelin receptor antagonist. |
Cat. No. | Product Name | Species | Expression System |
---|---|---|---|
TMPY-03860 |
Endothelin B Receptor Protein, Human, Recombinant (mFc)
ET-B,endothelin receptor type B,ETB,ETBR,E... |
Human | HEK293 Cells |
Endothelin B Receptor Protein, Human, Recombinant (mFc) is expressed in HEK293 mammalian cells with mFc tag. The predicted molecular weight is 34.4 kDa and the accession number is P24530-1. | |||
TMPY-00181 |
Endothelin B Receptor Protein, Human, Recombinant (His)
ETBR,ET-B,ET-BR,ETB,HSCR2,endothelin receptor |
Human | HEK293 Cells |
Endothelin B Receptor Protein, Human, Recombinant (His) is expressed in HEK293 mammalian cells with His tag. The predicted molecular weight is 9.5 kDa and the accession number is P24530-1. | |||
TMPY-02717 |
GPR37 Protein, Human, Recombinant (His)
hET(B)R-LP,PAELR,G protein-coupled receptor 37 ( |
Human | HEK293 Cells |
GPR37 (cathepsin Z) is an orphan receptor that belongs to the G-protein coupled receptor 1 family. G protein-coupled receptors are a large protein family comprised of transmembrane receptors that sense molecules outside the cell and activate inside signal transduction pathways and, ultimately, cellular responses. They only exist in eukaryotes, including yeast, choanoflagellates, and animals. These receptors are bonded and activated by light-sensitive compounds, odors, pheromones, hormones, and n... | |||
TMPH-01294 |
EDNRA Protein, Human, Recombinant (His)
ET-A,Endothelin-1 receptor,hET-AR,ETA-R,ET... |
Human | P. pastoris (Yeast) |
Receptor for endothelin-1. Mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. The rank order of binding affinities for ET-A is: ET1 > ET2 >> ET3. |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
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。 |