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48

抑制剂 & 化合物

4

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Cat. No. Product Name Target Signaling Pathways
T12268 NTP42

Prostaglandin Receptor; PPAR DNA Damage/DNA Repair; GPCR/G Protein; Immunology/Inflammation; Metabolism
NTP42 是血栓素 A2 (TXA2) 受体的拮抗剂,IC50为 3.278 nM,可用于肺动脉高压的相关研究。
T11339 Furegrelate sodium

U-63557A

PPAR DNA Damage/DNA Repair; Metabolism
Furegrelate sodium (U-63557A) 是口服有效的、血栓素合酶选择性抑制剂,抑制人血小板微粒体血栓素 A2 (TxA2) 合酶的 IC50为 15 nM。它正在开发作为抗血小板药物。
T8900 Seralutinib

GB002

PDGFR Angiogenesis; Tyrosine Kinase/Adaptors
Seralutinib (GB002) 是可吸入的PDGFRα 和 PDGFRβ激酶抑制剂,可用于研究肺动脉高压。
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。
T14782 Brilaroxazine

RP5063

Dopamine Receptor; 5-HT Receptor GPCR/G Protein; Neuroscience
Brilaroxazine (RP5063) 是一种有效的多模式多巴胺/5-HT 调节剂。 Brilaroxazine 是多巴胺 D2、D3 和 D4 受体、5-HT1A (Ki = 1.5 nM) 和 5-HT2A (Ki = 2.5 nM) 的部分激动剂,具有拮抗活性 5-HT2B 和 5-HT7 受体,Ki 分别为 0.19 nM 和 2.7 nM。 Brilaroxazine 可用于研究神经精神和神经系统疾病的认知障碍。
T3148 MK-571 sodium

L-660711 (sodium salt),L-660711 sodium salt,Verlukast sodium,L-660711,MK571,MK-571 sodium salt,Propanoic acid

Leukotriene Receptor; LTR GPCR/G Protein; Immunology/Inflammation
MK-571 sodium (L-660711 sodium salt) 是一种可口服的选择性白三烯 D4受体拮抗剂,在豚鼠和人肺膜的 Ki 分别为0.22 和 2.1 nM。
T60388 MIF098

Others Others
MIF098 是一种巨噬细胞迁移抑制因子 (MIF) 拮抗剂。MIF098,抑制与 SLE 相关的肺动脉高压,抑制肺平滑肌细胞(PASMC)增殖和迁移。MIF098 可用于研究特发性肺动脉高压。
T3216 Selexipag

NS-304,ACT-293987,赛乐西帕,Uptravi

Others; Prostaglandin Receptor GPCR/G Protein; Immunology/Inflammation; Others
Selexipag (ACT-293987) 是前列环素受体激动剂,可引起肺血管舒张,用于治疗肺动脉高压。
T11339L Furegrelate

PPAR DNA Damage/DNA Repair; Metabolism
FUREGRELATE 是一种血栓素 A2 (TxA2) 合酶抑制剂,可减缓新生仔猪肺动脉高压的发展。
T0467 Sildenafil citrate

UK-92480 citrate,西地那非柠檬酸盐,枸橼酸西地那非

Apoptosis; PDE; Autophagy Apoptosis; Autophagy; Metabolism
Sildenafil citrate (UK-92480 citrate) 是一种磷酸二酯酶 5 抑制剂,IC50为 5.22 nM。
T6968 Riociguat

利奥西呱,BAY 632521

Guanylate cyclase GPCR/G Protein
Riociguat (BAY 632521) 是一种鸟苷酸环化酶的刺激剂,可导致血管平滑肌松弛,用于治疗严重的肺动脉高压。
TP1016L Aviptadil Acetate

醋酸阿肽地尔,阿肽地尔,Vasoactive Intestinal Peptide acetate salt

RAAS; SARS-CoV Endocrinology/Hormones; Microbiology/Virology
Aviptadil Acetate (Vasoactive Intestinal Peptide acetate salt) 是模拟血管活性肠多肽类似物,具有血管舒张效应。它可诱导肺血管舒张并抑制血管 SMC 的增殖和血小板聚集。它可用于研究 SARS-CoV-2 引起的肺纤维化、肺动脉高压和呼吸衰竭。
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。
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)。
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。
T27624 Iptakalim Hydrochloride

Potassium Channel; AChR Membrane transporter/Ion channel; Neuroscience
Iptakalim hydrochloride 是一种亲脂性的对氨基化合物,是 ATP 敏感的钾通道的开放剂,也是含α4β2的烟碱乙酰胆碱受体拮抗剂。它也是一种 K(ir) 6.1/SUR2B 激活剂,可通过保护内皮功能减轻大鼠缺氧引起的肺动脉高压。
T13193 TPN171

PDE Metabolism
TPN171是一种有效的 PDE5抑制剂,对 PDE5具有亚纳摩尔效价,对 PDE5比对 PDE6具有良好的选择性,具有治疗肺动脉高压(PAH)的潜力。在动物模型中,TPN171被证明具有比西地那非更持久的作用,为临床使用每日一次口服提供了基础。
T15238 Epoprostenol sodium

Prostaglandin I2 sodium salt,Prostacyclin sodium salt,Flolan

Others Others
Epoprostenol sodium is a potent inhibitor of platelet aggregation used in pulmonary hypertension and transplantation.
T19660 QCC-374

QCC374

QCC-374 is a prostanoid agonist. It potentially for the treatment of pulmonary arterial hypertension.
T24389 LASSBio-1366

LASSBio 1366

LASSBio-1366 is an agonist of adenosine A2a receptor that acts by attenuating the progression of monocrotaline-induced pulmonary hypertension.
T30501 BMS-193884

BMS193884,BMS 193884

BMS-193884 is an oral endothelin antagonist for the treatment of congestive heart failure (CHF) and pulmonary arterial hypertension.
T20024 Tadalafil, (6R ,12aS)-

Tadalafil (6R ,12aS)- Lilly,Tadalafil specified impurity A,(-)-Tadalafil (6R ,12aS) diastereomer

Tadalafil is a carboline derivative and Phosphodiesterase 5 Inhibitor. It is used primarily to treat Erectile dysfunction, Benign Prostatic Hyperplasia, and Primary Pulmonary Hypertension.
T25568 Ketanserinol

Reduced ketanserin

Ketanserinol is the metabolite of ketanserin. Ketanserin is a hypotensive drug with 5-HT2 receptor antagonism, used to reverse pulmonary hypertension caused by protamine.
T11935 Macitentan (n-butyl analogue)

Others Others
Macitentan n-butyl analogue, a derivative of Macitentan, functions as an orally active dual antagonist targeting both endothelin ETA and ETB receptors. This compound shows promise for treating idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH), leveraging its non-peptide structure for potential therapeutic applications.
T36210 15-keto Treprostinil (sodium salt)

15-keto Treprostinil is an impurity found in treprostinil , which is a stable analog of prostaglandin I2 with a longer plasma half-life. Formulations containing treprostinil are used for the treatment of primary pulmonary hypertension.
T6959 PRX-08066 Maleic acid

5-HT Receptor GPCR/G Protein; Neuroscience
PRX-08066 Maleic acid 是一种选择性 5-HT2B 受体拮抗剂,IC50 为 3.4 nM,可防止 MCT 大鼠模型中肺动脉高压的严重程度。
T70704 RB-005

RB-005 is a potent sphingosine kinase isoform 1 (SK1) inhibitor, which may serve as therapeutic agent for proliferative diseases, including hypertension. RB-005, (IC(50) = 3.6 μM), which also induced proteasomal degradation of SK1 in human pulmonary arterial smooth muscle cells.
T74406 BRD2889

BRD2889 是生物碱胡椒胺的类似物。BRD2889 是肺动脉高压 (PH) 中GSTP1-ISCU 轴的强大调节剂。
T80075 Cyclo(Ala-Arg-Gly-Asp-Mamb)

XJ735

Integrin Cytoskeletal Signaling
Cyclo(Ala-Arg-Gly-Asp-Mamb) 是选择性的RGD肽拮抗剂,用于肺动脉高压治疗研究。
TMIH-0520 Selexipag-d7

Selexipag-d7 是 Selexipag 的氘代化合物。Selexipag 的 CAS 号为 475086-01-2。Selexipag 是前列环素受体激动剂,可引起肺血管舒张,用于治疗肺动脉高压。
T16779 Rodatristat ethyl

RVT-014,KAR5585,RVT-1201

5-HT Receptor; Hydroxylase GPCR/G Protein; Metabolism; Neuroscience
Rodatristat ethyl (KAR5585) 是一种首新型具有口服活性和有效性的 tryptophan hydroxylase 1 (TPH1) 抑制剂,低浓度下可显著降低 5-hydroxytryptamine (5-HT) 的水平并降低肺动脉高压 (PAH),
TP2000 MM 07

Apelin biased agonist; exhibits bias for the G protein pathway. Stimulates endothelial NOS phosphorylation and expression, promotes proliferation, and attenuates apoptosis of human pulmonary arterial endothelial cells in vitro. Shows positive inotropic an
T60429 SY-LB-57

SY-LB-57 是骨形态发生蛋白 (BMP) 受体信号传导的高效激动剂。SY-LB-57可用于骨折和肺动脉高压等病症的研究。
T79223 BMPR2-IN-1

MPR2-IN-1(Compound 8a)为BMPR2抑制剂,IC50为506 nM,KD值83.5 nM,适用于肺动脉高压、阿尔茨海默病及癌症研究。
T78721 Smurf1-IN-1

E1/E2/E3 Enzyme Ubiquitination
SMURF1-IN-1是一种口服活性的特异性E3泛素蛋白连接酶1(SMURF1)选择性抑制剂,IC50值为92 nM。在大鼠肺部高压模型中显示出显著疗效,适用于肺动脉高压疾病的研究。
T79574 ET receptor antagonist 2

Estrogen Receptor/ERR Endocrinology/Hormones
ET receptor antagonist 2 (compound 16j) 作为一种ET受体拮抗剂,具有0.22 nM的IC50,主要应用于肺动脉高压(PAH)的研究。在大鼠模型中,它能够有效减缓野百合碱诱导的PAH症状。
T79575 ET receptor antagonist 3

Estrogen Receptor/ERR Endocrinology/Hormones
ET receptor antagonist 3 (compound 17d)为ET受体拮抗剂,其IC50值为0.26 nM,主要用于肺动脉高压(PAH)的研究应用。在大鼠模型中,该化合物能有效减轻由野百合碱诱导的PAH症状。
T79573 ET receptor antagonist 1

Estrogen Receptor/ERR Endocrinology/Hormones
ET receptor antagonist 1 (compound 16h),作为ET受体拮抗剂(IC50=0.18 nM),主要用于肺动脉高压(PAH)的研究。该化合物能缓解大鼠模型中由野百合碱引发的PAH症状。
TMIH-0497 Riociguat-13C-d6

Riociguat-13C-d6 是 Riociguat 的 13C 和氘代化合物。Riociguat 的 CAS 号为 625115-55-1。Riociguat 是一种鸟苷酸环化酶的刺激剂,可导致血管平滑肌松弛,用于治疗严重的肺动脉高压。
T78076 PBR28

Others Others
PBR28是一种TSPO调节剂,适用于肺动脉高压(PAH)预防研究。通过增加放射性标记的PBR28能够示踪18KDa转运蛋白(TSPO),在脑正电子发射断层扫描(PET)成像中具有关键作用。
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。
T62909 SGC agonist 2

SGC agonist 2 是一种有效的可溶性鸟苷酸环化酶 (SGC) 激动剂。其中可溶性鸟苷酸环化酶是 NO-sGC-cGMP 信号通路中的关键信号转导酶。SGC agonist 2 具有潜力进行心血管疾病 (心力衰竭、心绞痛、肺动脉高压、心肌梗塞) 和纤维化疾病 (肾纤维化、系统性硬化症) 的研究。
TMIH-0519 Selexipag Active Metabolite-d7

Selexipag Active Metabolite-d7 是 Selexipag Active Metabolite 的氘代化合物。Selexipag Active Metabolite 的 CAS 号为 475085-57-5。MRE269 是一种口服的长效前列环素受体激动剂前药,是 Selexipag 的活性代谢物,用于治疗肺动脉高压。
T76995 Sotatercept

Sotatercept (ACE-011) 是一种可溶性激活素受体 2A (ACVR2A) 型 IgGFc 融合蛋白。Sotatercept 结合了激活素和生长分化因子,试图恢复生长促进和生长抑制信号通路之间的平衡。Sotatercept 在肺动脉高压、贫血、骨质流失、红细胞生成、多发性骨髓瘤 (MM) 溶骨性病变中有潜在的应用。
TP2214 Adrenomedullin (1-12), human

Others Others
Adrenomedullin (AM) (1-12), human, is a peptide with the sequence Tyr-Arg-Gln-Ser-Met-Asn-Asn-Phe-Gln-Gly-Leu-Arg. Adrenomedullin (AM) (1-12), human, was initially identified as a vasodilator, and as such, it has the ability to relax vascular tone. Other
T36405 Pro-Adrenomedullin (153-185), human

Pro-Adrenomedullin (153-185), human,H2N-Ser-Leu-Pro-Glu-Ala-Gly-Pro-Gly-Arg-Thr-Leu-Val-Ser-Ser-Lys-Pro-Gln-Ala-His-Gly-Ala-Pro-Ala-Pro-Pro-Ser-Gly-Ser-Ala-Pro-His-Phe-Leu-OH

Pro-Adrenomedullin(153-185),human, (C143H224N42O43), a peptide with the sequence H2N-SLPEAGPGRTLVSSKPQAHGAPAPPSGSAPHFL-OH, MW= 3219.6. Adrenomedullin (AM) is a ubiquitously expressed peptide initially isolated from phaechromyctoma in 19931. AM was initially identified as a vasodilator, some have cited this as the most potent endogenous vasodilatory peptide found in the body2. Differences in opinion regarding the ability of AM to relax vascular tone arises from the differences in the model system...
T65598 Cefminox sodium

Cefminox (Sodium) is a new cephamycin antibiotic possessing a D-amino acid moiety derived from D-cysteine at the C-7B side chain. Cefminox is active against a wide range of bacteria, especially Gram-negative and anaerobic bacteria. Cefminox shows excellent in vivo efficacy (ED50) which is higher than would be expected from its in vitro activity (MIC). Moreover, cefminox possesses more potent activity in suppression of bacterial regrowth than other cephems[1]. Cefminox (Sodium) was the most activ...
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...

化合物

NTP42
Cat.No: T12268
Synonym:
Target: Prostaglandin Receptor, PPAR
Furegrelate sodium
Cat.No: T11339
Synonym: U-63557A
Target: PPAR
Seralutinib
Cat.No: T8900
Synonym: GB002
Target: PDGFR
Macitentan
Cat.No: T2561
Synonym: 马西替坦,ACT-064992
Target: Apoptosis, Endothelin Receptor
Brilaroxazine
Cat.No: T14782
Synonym: RP5063
Target: Dopamine Receptor, 5-HT Receptor
MK-571 sodium
Cat.No: T3148
Synonym: L-660711 (sodium salt),L-660711 sodium salt,Verlukast sodium,L-660711,MK571,MK-571 sodium salt,Propanoic acid
Target: Leukotriene Receptor, LTR
MIF098
Cat.No: T60388
Synonym:
Target: Others
Selexipag
Cat.No: T3216
Synonym: NS-304,ACT-293987,赛乐西帕,Uptravi
Target: Others, Prostaglandin Receptor
Furegrelate
Cat.No: T11339L
Synonym:
Target: PPAR
Sildenafil citrate
Cat.No: T0467
Synonym: UK-92480 citrate,西地那非柠檬酸盐,枸橼酸西地那非
Target: Apoptosis, PDE, Autophagy
Riociguat
Cat.No: T6968
Synonym: 利奥西呱,BAY 632521
Target: Guanylate cyclase
Aviptadil Acetate
Cat.No: TP1016L
Synonym: 醋酸阿肽地尔,阿肽地尔,Vasoactive Intestinal Peptide acetate salt
Target: RAAS, SARS-CoV
Ambrisentan
Cat.No: T1655
Synonym: BSF-208075,BSF 208075,安倍生坦,LU 208075
Target: Endothelin Receptor
Bosentan
Cat.No: T6264
Synonym: Actelion,波生坦,Ro 47-0203,Benzenesulfonamide
Target: Endothelin Receptor
Nebentan potassium
Cat.No: T36008
Synonym: YM598
Target: Endothelin Receptor
Iptakalim Hydrochloride
Cat.No: T27624
Synonym:
Target: Potassium Channel, AChR
TPN171
Cat.No: T13193
Synonym:
Target: PDE
Epoprostenol sodium
Cat.No: T15238
Synonym: Prostaglandin I2 sodium salt,Prostacyclin sodium salt,Flolan
Target: Others
QCC-374
Cat.No: T19660
Synonym: QCC374
Target:
LASSBio-1366
Cat.No: T24389
Synonym: LASSBio 1366
Target:
BMS-193884
Cat.No: T30501
Synonym: BMS193884,BMS 193884
Target:
Tadalafil, (6R ,12aS)-
Cat.No: T20024
Synonym: Tadalafil (6R ,12aS)- Lilly,Tadalafil specified impurity A,(-)-Tadalafil (6R ,12aS) diastereomer
Target:
Ketanserinol
Cat.No: T25568
Synonym: Reduced ketanserin
Target:
Macitentan (n-butyl analogue)
Cat.No: T11935
Synonym:
Target: Others
15-keto Treprostinil (sodium salt)
Cat.No: T36210
Synonym:
Target:
PRX-08066 Maleic acid
Cat.No: T6959
Synonym:
Target: 5-HT Receptor
RB-005
Cat.No: T70704
Synonym:
Target:
BRD2889
Cat.No: T74406
Synonym:
Target:
Cyclo(Ala-Arg-Gly-Asp-Mamb)
Cat.No: T80075
Synonym: XJ735
Target: Integrin
Selexipag-d7
Cat.No: TMIH-0520
Synonym:
Target:
Rodatristat ethyl
Cat.No: T16779
Synonym: RVT-014,KAR5585,RVT-1201
Target: 5-HT Receptor, Hydroxylase
MM 07
Cat.No: TP2000
Synonym:
Target:
SY-LB-57
Cat.No: T60429
Synonym:
Target:
BMPR2-IN-1
Cat.No: T79223
Synonym:
Target:
Smurf1-IN-1
Cat.No: T78721
Synonym:
Target: E1/E2/E3 Enzyme
ET receptor antagonist 2
Cat.No: T79574
Synonym:
Target: Estrogen Receptor/ERR
ET receptor antagonist 3
Cat.No: T79575
Synonym:
Target: Estrogen Receptor/ERR
ET receptor antagonist 1
Cat.No: T79573
Synonym:
Target: Estrogen Receptor/ERR
Riociguat-13C-d6
Cat.No: TMIH-0497
Synonym:
Target:
PBR28
Cat.No: T78076
Synonym:
Target: Others
BQ-123 TFA
Cat.No: T73877
Synonym:
Target:
SGC agonist 2
Cat.No: T62909
Synonym:
Target:
Selexipag Active Metabolite-d7
Cat.No: TMIH-0519
Synonym:
Target:
Sotatercept
Cat.No: T76995
Synonym:
Target:
Adrenomedullin (1-12), human
Cat.No: TP2214
Synonym:
Target: Others
Pro-Adrenomedullin (153-185), human
Cat.No: T36405
Synonym: Pro-Adrenomedullin (153-185), human,H2N-Ser-Leu-Pro-Glu-Ala-Gly-Pro-Gly-Arg-Thr-Leu-Val-Ser-Ser-Lys-Pro-Gln-Ala-His-Gly-Ala-Pro-Ala-Pro-Pro-Ser-Gly-Ser-Ala-Pro-His-Phe-Leu-OH
Target:
Cefminox sodium
Cat.No: T65598
Synonym:
Target:
Nebentan
Cat.No: T36007
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
T1680 Tolazoline hydrochloride

Imidaline hydrochloride,苯甲唑啉盐酸盐,Imidaline (hydrochloride),Benzidazol hydrochloride,Tolazoline HCl,NSC35110 (hydrochloride)

Adrenergic Receptor GPCR/G Protein; Neuroscience
Tolazoline hydrochloride (NSC35110(hydrochloride)) 是一种 α 肾上腺素受体抑制剂。
T2803 Monocrotaline

野百合碱,Crotaline

TGF-beta/Smad Stem Cells
Monocrotaline (Crotaline) 是一种吡咯里西啶生物碱,从猪屎豆植物的种子中提取得到,可诱导啮齿动物产生肺动脉高血压。
T3S2007 MRE-269

3-氧代-12-烯-28-乌苏酸,MRE 269,ACT-333679,MRE269

Prostaglandin Receptor GPCR/G Protein; Immunology/Inflammation
MRE-269 (ACT-333679) 是一种口服的长效前列环素受体激动剂前药,是 Selexipag 的活性代谢物,用于治疗肺动脉高压。
TN4654 Niazirin

Others Others
The Moringa oleifera extract(including niaziridin and Niazirin) can successfully attenuate the development of pulmonary hypertension via direct vasodilatation and a potential increase in antioxidant activity.

天然产物

Tolazoline hydrochloride
Cat.No: T1680
Synonym: Imidaline hydrochloride,苯甲唑啉盐酸盐,Imidaline (hydrochloride),Benzidazol hydrochloride,Tolazoline HCl,NSC35110 (hydrochloride)
Target: Adrenergic Receptor
Monocrotaline
Cat.No: T2803
Synonym: 野百合碱,Crotaline
Target: TGF-beta/Smad
MRE-269
Cat.No: T3S2007
Synonym: 3-氧代-12-烯-28-乌苏酸,MRE 269,ACT-333679,MRE269
Target: Prostaglandin Receptor
Niazirin
Cat.No: TN4654
Synonym:
Target: Others
TargetMol Loading
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