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Search Results for " endothelin receptor "
Targets Recommended: Endothelin Receptor Endothelin Receptor

80

抑制剂 & 化合物

4

重组蛋白

1

同位素标记化合物

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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.

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
CYM5442
Cat.No: T2026
Synonym:
Target: S1P Receptor, LPL 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
BQ-123
Cat.No: T6792
Synonym: BQ123
Target: Endothelin Receptor
RO 46-8443
Cat.No: T3474
Synonym:
Target: Endothelin Receptor
Zibotentan
Cat.No: T6258
Synonym: ZD4054
Target: Apoptosis, 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
Bosentan (hydrate)
Cat.No: T6265
Synonym: 波生坦水合物,Bosentan Hydrate,Benzenesulfonamide,Actelion,Ro 47-0203
Target: Endothelin Receptor
Atrasentan
Cat.No: TQ0259
Synonym: A-147627,(+)-A 127722,阿曲生坦,ABT-627
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
BMS 182874 hydrochloride
Cat.No: T21790
Synonym:
Target: Endothelin Receptor
Edonentan
Cat.No: T31605
Synonym: BMS207940,BMS-207940,BMS 207940
Target: Endothelin Receptor
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
IRL-1620 acetate
Cat.No: T15595L
Synonym: IRL-1620 acetate(142569-99-1 free base)
Target: Endothelin Receptor
Nebentan potassium
Cat.No: T36008
Synonym: YM598
Target: Endothelin Receptor
Ac-Endothelin-1 (16-21), human acetate
Cat.No: T22540L
Synonym:
Target: Others
Clazosentan
Cat.No: T64084
Synonym: VML 588,AXV-034343,Ro 61-1790
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
FR 139317
Cat.No: T22791
Synonym:
Target: Others
BQ 485
Cat.No: T30572
Synonym: BQ485,BQ-485
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: Others
ATZ-1993
Cat.No: T69816
Synonym:
Target: Others
Fandosentan
Cat.No: T69791
Synonym:
Target: Others
PD-156707
Cat.No: T28343
Synonym: PD156707
Target: Others
TBC3711
Cat.No: T15232
Synonym: Endothelin Mordulator 1
Target: Others
Kendomycin
Cat.No: T27725
Synonym: TAN-2162,TAN 2162,TAN2162
Target: Others
Cgs 27830
Cat.No: T70454
Synonym:
Target: Others
WS 009B
Cat.No: T24081
Synonym: WS-009B,FR 901367,WS009B
Target: Others
SB234551
Cat.No: T28683
Synonym: SB 234551,SB-234551
Target: Others
WS 009A
Cat.No: T24053
Synonym: WS009 A,FR 901366,WS009A,WS-009A
Target: Others
BQ-610
Cat.No: T70727
Synonym:
Target: Others
TBC 3711
Cat.No: T69338
Synonym:
Target: Others
L-749329
Cat.No: T27776
Synonym: L749329,L 749329
Target: Others
PD 151242
Cat.No: T70452
Synonym:
Target: Others
BMS-346567
Cat.No: T30515
Synonym: BMS346567,BMS 346567
Target: Others
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.

重组蛋白

Endothelin B Receptor Protein, Human, Recombinant (mFc)
Cat.No: TMPY-03860
Species: Human
Expression System: HEK293 Cells
Endothelin B Receptor Protein, Human, Recombinant (His)
Cat.No: TMPY-00181
Species: Human
Expression System: HEK293 Cells
GPR37 Protein, Human, Recombinant (His)
Cat.No: TMPY-02717
Species: Human
Expression System: HEK293 Cells
EDNRA Protein, Human, Recombinant (His)
Cat.No: TMPH-01294
Species: Human
Expression System: P. pastoris (Yeast)
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。

同位素标记化合物

Macitentan-d4
Cat.No: T11934
Synonym: Macitentan D4,ACT-064992 D4
Target: Endothelin Receptor
TargetMol Loading
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