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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。
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.

化合物

Darusentan
Cat.No: T5458
Synonym: Lu-135252,达卢生坦
Target: Endothelin Receptor
Ro 46-2005
Cat.No: T3194
Synonym:
Target: Endothelin Receptor
Macitentan
Cat.No: T2561
Synonym: 马西替坦,ACT-064992
Target: Apoptosis, Endothelin Receptor
Sparsentan
Cat.No: T5355
Synonym: RE-021,DARA-a
Target: RAAS, Endothelin Receptor
Sulfisoxazole
Cat.No: T0750
Synonym: NU-445,磺胺二甲异唑,Sulfafurazole,磺胺异恶唑
Target: Endothelin Receptor, Antibacterial, Antibiotic, Autophagy
CYM5442
Cat.No: T2026
Synonym:
Target: S1P Receptor, LPL Receptor
RO 46-8443
Cat.No: T3474
Synonym:
Target: Endothelin Receptor
Zibotentan
Cat.No: T6258
Synonym: ZD4054
Target: Apoptosis, Endothelin Receptor
BQ-123
Cat.No: T6792
Synonym: BQ123
Target: Endothelin Receptor
Bosentan
Cat.No: T6264
Synonym: Actelion,波生坦,Ro 47-0203,Benzenesulfonamide
Target: Endothelin Receptor
Avosentan
Cat.No: TQ0282
Synonym: SPP-301,Ro 67-0565,阿伏生坦
Target: Endothelin Receptor
Ambrisentan
Cat.No: T1655
Synonym: BSF-208075,BSF 208075,安倍生坦,LU 208075
Target: Endothelin Receptor
Atrasentan
Cat.No: TQ0259
Synonym: A-147627,(+)-A 127722,阿曲生坦,ABT-627
Target: Endothelin Receptor
Bosentan (hydrate)
Cat.No: T6265
Synonym: 波生坦水合物,Bosentan Hydrate,Benzenesulfonamide,Actelion,Ro 47-0203
Target: Endothelin Receptor
Sitaxsentan sodium
Cat.No: T6672
Synonym: 西他生坦钠,TBC11251 sodium salt,TBC11251,Thelin,Sitaxentan sodium
Target: Endothelin Receptor
Aprocitentan
Cat.No: T7817
Synonym: 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
Target: Endothelin Receptor
Atrasentan hydrochloride
Cat.No: TQ0270
Synonym: (+)-A 127722 hydrochloride,ABT-627 hydrochloride,盐酸阿曲生坦,A-147627 hydrochloride
Target: Endothelin Receptor
IRL 2500
Cat.No: T15596
Synonym:
Target: Endothelin Receptor
Sitaxsentan
Cat.No: T12924
Synonym: TBC-11251,IPI 1040
Target: Endothelin Receptor
Edonentan
Cat.No: T31605
Synonym: BMS207940,BMS-207940,BMS 207940
Target: Endothelin Receptor
BMS 182874 hydrochloride
Cat.No: T21790
Synonym:
Target: Endothelin Receptor
Nebentan potassium
Cat.No: T36008
Synonym:
Target:
IRL-1038 acetate
Cat.No: TP2262L
Synonym: IRL-1038 acetate(144602-02-8 Free base)
Target: Endothelin Receptor
SB-209670
Cat.No: T34541
Synonym: SB 209670
Target: Endothelin Receptor
Ac-Endothelin-1 (16-21), human acetate
Cat.No: T22540L
Synonym:
Target: Others
IRL-1620 acetate
Cat.No: T15595L
Synonym: IRL-1620 acetate(142569-99-1 free base)
Target: Endothelin Receptor
BMS 182874
Cat.No: T26841
Synonym: BMS182874,BMS-182874
Target: Endothelin Receptor
Urantide acetate(669089-53-6 free base)
Cat.No: TP2106L
Synonym:
Target: Neurotensin Receptor
Sacubitril hemicalcium salt
Cat.No: T4200
Synonym: AHU-377 (hemicalcium salt),LCZ696中间体,AHU377 calcium salt
Target: Neprilysin
BQ 485
Cat.No: T30572
Synonym: BQ485,BQ-485
Target:
FR 139317
Cat.No: T22791
Synonym:
Target: Others
ABT-546
Cat.No: T10225
Synonym: A-216546
Target: Others
CI 1020
Cat.No: T22663
Synonym:
Target: Others
[Ala1,​3,​11,​15]​-​Endothelin TFA
Cat.No: TP1512
Synonym:
Target:
Sulfisoxazole diethanolamine
Cat.No: T61498
Synonym:
Target:
PD-156707
Cat.No: T28343
Synonym: PD156707
Target:
Fandosentan
Cat.No: T69791
Synonym:
Target:
Kendomycin
Cat.No: T27725
Synonym: TAN-2162,TAN 2162,TAN2162
Target:
Cgs 27830
Cat.No: T70454
Synonym:
Target:
TBC 3711
Cat.No: T69338
Synonym:
Target:
BQ-610
Cat.No: T70727
Synonym:
Target:
L-749329
Cat.No: T27776
Synonym: L749329,L 749329
Target:
BMS-346567
Cat.No: T30515
Synonym: BMS346567,BMS 346567
Target:
TBC3711
Cat.No: T15232
Synonym: Endothelin Mordulator 1
Target: Others
ATZ-1993
Cat.No: T69816
Synonym:
Target:
WS 009A
Cat.No: T24053
Synonym: WS009 A,FR 901366,WS009A,WS-009A
Target:
SB234551
Cat.No: T28683
Synonym: SB 234551,SB-234551
Target:
WS 009B
Cat.No: T24081
Synonym: WS-009B,FR 901367,WS009B
Target:
IRL-1038
Cat.No: TP2262
Synonym:
Target: Others
PD 151242
Cat.No: T70452
Synonym:
Target:
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