Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
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。 | |||
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。 | |||
T36480 |
Big Endothelin-1 (1-39), porcine
|
||
The big endothelins comprise residues 53-90 (human big ET-1) and 53-91 (porcine big ET-1) of the endothelin precursor (preproendothelin). Compared to the mature endothelin-1 (ET-1), both peptides show less vasoconstrictor activity in vitro, but similar pressor effects in vivo. Former CAS-number 121014-54-8. | |||
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. | |||
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. | |||
T36479 |
Big Endothelin-1 (1-38), human
|
||
Human Big ET-1 comprises residues 53-90 of the endothelin precursor (preproendothelin). Compared to the mature endothelin-1 (hET-1), the peptide show less vasoconstrictor activity in vitro, but similar pressor effects in vivo. Former CAS-number 121014-53-7. | |||
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 | |||
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。 | |||
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 | |||
T15232 |
TBC3711
Endothelin Mordulator 1 |
Others | Others |
TBC3711 is an endothelin receptor modulator. It is used for the research of endothelin-mediated disorders. | |||
T76564 |
Endothelin-1 (1-31) (Human)
|
||
Endothelin-1 (1-31) (Human) 是源于chymase对大ET-1选择性水解而来的有效血管收缩剂和血压升高剂。 | |||
T76329 |
[Asn18] Endothelin-1, human
|
||
[Asn18] Endothelin-1, human 为一种多肽,属于内皮素家族中的主要亚型,关键于血管功能调节。 | |||
T76564L |
Endothelin-1 (1-31) (Human) acetate
|
||
Endothelin-1 (1-31) (Human) acetate,源自于chymase对大ET-1的选择性水解,是一种有效的血管收缩剂和血压升高剂。 | |||
T78063 |
Endothelin-1 (1-31) (Human) TFA
|
ERK | MAPK |
Endothelin-1 (1-31) (Human) TFA 是源自chymase对大ET-1选择性水解的一种有效血管收缩剂和血压升高剂。 | |||
T82886 |
Big endothelin-1 (rat 1-39)
|
||
Big endothelin-1 (rat 1-39) 是一个由39个氨基酸残基组成的多肽。它能在清醒状态的Sprague-Dawley大鼠中诱导利尿和利钠的反应,并可导致小鼠血压上升。 | |||
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。 | |||
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。 | |||
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)。 | |||
T14219 |
Aminaftone
Aminaphthone |
Endothelin Receptor | GPCR/G Protein |
Aminaftone 是 4-氨基苯甲酸的衍生物,可抑制内皮素-1 (ET-1) 的产生,可用于研究高血压和系统硬化症。 | |||
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。 | |||
TP1220L |
Carperitide acetate
醋酸卡培立肽,Carperitide acetate (89213-87-6 Free base),Atrial Natriuretic Peptide (ANP) (1-28), human, porcine Acetate |
Endothelin Receptor | GPCR/G Protein |
Carperitide acetate (Atrial Natriuretic Peptide (ANP) (1-28), human, porcine Acetate) 是一种由 28 个氨基酸组成的激素,由心脏产生并分泌,以响应心脏损伤和机械拉伸。Carperitide acetate 抑制内皮素-1 (endothelin-1) 分泌。 | |||
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)。 | |||
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。 | |||
T77374 |
Ontuxizumab
MORAb-004 |
Others | Others |
Ontuxizumab (MORAb-004) 是一种靶向内髓酸的单克隆抗体,具有抗肿瘤作用。Ontuxizumab 是一种有效的 IgG1/κ 抗内皮素 (TEM-1 或 CD248) 的单克隆抗体,可用于治疗转移性黑色素瘤。 | |||
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。 | |||
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. | |||
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... | |||
T35623 |
ACT-373898
|
||
ACT-373898 is a metabolite of the endothelin (ET) receptor type A (ETA) and ETBdual antagonist macitentan .1 1.Dingemanse, J., Sidharta, P.N., Maddrey, W.C., et al.Efficacy, safety and clinical pharmacology of macitentan in comparison to other endothelin receptor antagonists in the treatment of pulmonary arterial hypertensionExpert Opin. Drug Saf.13(3)391-405(2013) | |||
T27119 |
Daglutril
SLV306,SLV 306,SLV-306 |
||
Daglutril, a NEP/ECE inhibitor, is potentially used for the treatment of hypertension, heart failure andpulmonary. Daglutril inhibits systemic conversion of big endothelin-1 in humans. | |||
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]. | |||
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。 | |||
T37351 |
Desmethyl Bosentan
|
||
Desmethyl bosentan is an active metabolite of the endothelin receptor antagonist bosentan .1Desmethyl bosentan (25 μM) activates the pregnane X receptor (PXR) in CV-1 monkey kidney cells expressing the human receptor in a reporter assay. 1.van Giersbergen, P.L.M., Gnerre, C., Treiber, A., et al.Bosentan, a dual endothelin receptor antagonist, activates the pregnane X nuclear receptorBr. J. Clin. Pharmacol.54(5)561-562(2002) | |||
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。 | |||
TP1220 |
Carperitide
Atrial Natriuretic Peptide (ANP) (1-28), human, porcine |
||
Carperitide, a 28-amino acid hormone known as Atrial Natriuretic Peptide (ANP) (1-28), is naturally synthesized and released by the human heart in reaction to cardiac injury and mechanical stretch. This compound effectively suppresses endothelin-1 secretion in a dose-dependent manner. | |||
TP1218 |
Atrial natriuretic factor (1-28) (rat) TFA
Atrial Natriuretic Peptide (ANP) (1-28), rat TFA |
||
Atrial Natriuretic Peptide (ANP) (1-28),rat (TFA) is the main circulating forms of Atrial Natriuretic Peptide (ANP) in rats, which strongly inhibit the secretion of Ang II - stimulated endothelin-1. | |||
T14672 | BMS-248360 | Others | Others |
BMS-248360 is a potent and orally active dual antagonist of both angiotensin II receptor (AT1) and endothelin A (ETA) receptor. With Kis of 10 nM and 1.9 nM for hAT1 and hETA receptor, respectively. BMS-248360 shows hypertensive effects[1]. | |||
T76302 |
[Lys4] Sarafotoxin S6c
|
||
[Lys4] Sarafotoxin S6c 是一种 sarafotoxin 类似物,是一种有效的内皮素受体 (endothelin receptor) 的部分激动剂。[Lys4] Sarafotoxin S6c 可诱导猪冠状动脉收缩,其 EC50为 1.5 nM。 | |||
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). | |||
T83687 |
Mca-RPPGFSAFK(Dnp)-OH TFA
(7-methoxycoumarin-4-yl)acetyl-Arg-Pro-Pro-Gly-Phe-Ser-Ala-Phe-Lys(2,4-dinitrophenyl)-OH |
||
Mca-RPPGFSAFK(Dnp)-OH 是 endothelin-converting enzyme-1 (ECE-1) 的一种荧光底物。当 ECE-1 切割该底物时,会释放 7-methoxycoumarin-4-acetyl (Mca),其荧光可以用来量化 ECE-1 的活性。Mca 的激发/发射峰值分别为 328/420 nm。 | |||
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 | |||
T41232 |
GSK 2833503A
|
||
GSK 2833503A is a potent and selective TRPC6 and TRPC3 antagonist (IC50 = 3-16 nM and 21-100 nM, respectively). GSK 2833503A exhibits >63-fold selectivity over other ion channels, including other TRP channels, CaV1.2, hERG and NaV1.5. GSK 2833503A suppresses angiotensin II or endothelin-1-induced cardiac hypertrophy signaling in HEK293 cellsin vitroand in cardiomyocytes. | |||
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。 | |||
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 | |||
T36565 |
Adrenomedullin (13-52) (human) (trifluoroacetate salt)
|
||
Adrenomedullin (13-52) is a truncated form of adrenomedullin (1-52) . It induces nitric oxide-dependent relaxation of and inhibits release of angiotensin II and endothelin-1 from isolated rat aorta. In vivo, adrenomedullin (13-52) decreases mean arterial pressure (MAP) in spontaneously and renal hypertensive rats in a dose-dependent manner. Adrenomedullin (13-52) (10-3,000 ng per animal) reverses increases in lobar arterial pressure induced by U-46619 in a dose-dependent manner in cats but has n... | |||
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。 | |||
T38167 |
BE-24566B
|
||
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... | |||
TP2106 |
Urantide
|
||
Selective and competitive urotensin-II (UT) receptor antagonist (pKB = 8.3). Blocks hU-II induced contractions in thoracic aorta ex vivo. Exhibits no effect on noradrenaline or endothelin 1-induced contraction or on acetylcholine-induced relaxation. Behav |