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Cat. No. | Product Name | Target | Signaling Pathways |
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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。 | |||
T5329 |
Trandolapril
|
Angiotensin-converting Enzyme (ACE) | Metabolism |
Trandolapril 是 Trandolaprilat 的前体药物。Trandolapril 是一种口服血管紧张素转换酶抑制剂,在高血压和充血性心力衰竭及心肌梗死领域有研究价值。 | |||
T3046 |
BMY 7378 dihydrochloride
BMY7378 HCl |
Dopamine Receptor; 5-HT Receptor; Adrenergic Receptor | GPCR/G Protein; Neuroscience |
BMY 7378 dihydrochloride (BMY7378 HCl) 是选择性 α1D 肾上腺素受体拮抗剂,也是5-HT1A 受体部分激动剂。它同表达克隆大鼠 α1D-AR 的膜结合的亲和力 (Ki=2 nM) 是同克隆大鼠 α1A-AR (Ki=800 nM) 或仓鼠 α1B-AR (Ki=600 nM) 结合的亲和力 的100 以上。 | |||
T23044 |
N,N'-Dicyclohexylurea
DCU,1,3-Dicyclohexylurea,NSC 17013,Dicyclohexylurea,Dicyclohexylcarbodiamide,AURORA KA-3582,N,N-二环己脲 |
Epoxide Hydrolase | Metabolism |
N,N'-Dicyclohexylurea (AURORA KA-3582) 是一种可溶性环氧化物水解酶 (sEH) 抑制剂。 | |||
T16329 |
Nitroflurbiprofen
NO-flurbiprofen,Nitroxybutyl flurbiprofen,硝基氟比洛芬,HCT 1206 |
COX | Immunology/Inflammation; Neuroscience |
Nitroflurbiprofen (Nitroxybutyl flurbiprofen) 是一种释放 NO 的环氧合酶抑制剂,可调节门脉高压性肝硬化大鼠肝内血管张力的增加。 | |||
T14942 |
CGP48369
|
RAAS | Endocrinology/Hormones |
CGP48369 是一种有效的血管紧张素 II 受体 (angiotensin II receptor) 拮抗剂,具有降血压作用,可增强自发性高血压大鼠冠状动脉的内皮依赖性松弛。 | |||
T36506 |
Tempone
4-Oxo-tempo |
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Tempone 是一种氨基氧烷,具有自由基清除剂的作用,会与活性氧(ROS)发生反应。静脉注射 Tempone 可降低自发性高血压大鼠的平均动脉。 | |||
T28482 |
Firibastat
QGC 001,QGC-001,RB-150,RB150,QGC001,RB 150 |
Aminopeptidase | Metabolism |
Firibastat (RB150) 是一种具有口服活性的 EC33 前体药物。Firibastat 是一种首创的脑氨基肽酶 A(APA) 抑制剂 (Ki=200 nM),选择性地抑制高血压大鼠脑血管紧张素 II 转化为血管紧张素 III,降低血压。 | |||
T28039 |
Milfasartan
LR-B081,LRB-081,LR-B-081,LRB 081,LR-B 081 |
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Milfasartan is a potent, selective antagonist of AT1 receptor with oral activity. It markedly lowers the blood-pressure in conscious renal and spontaneously hypertensive rats. | |||
T27306 |
Fasidotril
BP 1137,BP1137,BP-1.137,BP1.137,BP-1137,BP 1.137 |
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Fasidotril is a NEP/ACE inhibitor. Fasidotril was an effective oral antihypertensive agent during chronic treatment in high-renin renovascular rats, normal-renin SHR, and low-renin DOCA-salt hypertensive rats and in patients with essential hypertension. | |||
T71396 |
FCE-24379
|
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FCE-24379 is a selective antagonist of vascular serotonin receptors that has been shown to lowers blood pressure in hypertensive rats. | |||
T27743 |
KRH-594 free acid
WK14922K,WK-1492,WK-14922K,WK1492 |
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KRH-594 is a potent, specific and insurmountable AT1 receptor antagonist. KRH-594 ameliorates hyperlipidaemia and nephropathy in diabetic spontaneously hypertensive rats. KRH-594 prevents end-organ damage in stroke-prone spontaneously hypertensive/Izm ra | |||
T38424 |
(R)-Fadrozole
FAD286,(R)-CGS 16949A free base,(R)-Fadrozole |
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(R)-Fadrozole ((R)-CGS 16949A; FAD286) is a potent nonsteroidal inhibitor. (R)-Fadrozole also inhibits human placental aromatase (pIC 50 = 6.17) and aldosterone biosynthesis. (R)-Fadrozole reverses cardiac fibrosis in spontaneously hypertensive heart failure rats.. | |||
T79267 |
Antihypertensive agent 3
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Antihypertensive agent 3 (compound 4a) 是一种针对血管紧张素 II 受体 1(AT1) 的拮抗剂,其在自发性高血压大鼠(SHRs)的模型中表现出显著的降压效果。 | |||
T71065 |
Quinapril-d5
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Quinapril-d5 is intended for use as an internal standard for the quantification of quinapril by GC- or LC-MS. Quinapril is a prodrug form of the angiotensin converting enzyme (ACE) inhibitor quinaprilat. In vivo, quinapril reduces mean arterial pressure in renal hypertensive and spontaneously hypertensive rats. It inhibits angiotensin I-induced pressor responses in normotensive rats and dogs. Quinapril prevents left ventricular heart failure in CHF 14.6 cardiomyopathic hamsters. Formulations con... | |||
TP1892 |
γ1-MSH
|
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Endogenous melanocortin MC3 receptor agonist (pKi = 7.46) that displays ~ 40-fold selectivity over MC4. Increases the release of extracellular dopamine, which induces grooming and vertical activity (rearing) in rats. Exhibits hypertensive, tachycardic and | |||
T12596 |
(4E)-SUN9221
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5-HT Receptor; Adrenergic Receptor | GPCR/G Protein; Neuroscience |
(4E)-SUN9221 是一种有效的 α1-adrenergic 受体和 5-HT2 受体双重拮抗剂,在高血压大鼠中显示出抗高血压和抗血小板聚集活性。 | |||
T63452 |
Benidipine
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Benidipine 是一种有效的、口服具有活力的钙通道拮抗剂。Benidipine 能够提高内皮细胞型一氧化氮合酶的活性,改善高血压大鼠冠状动脉循环。Benidipine 能够抗缺血/再灌注心肌细胞的凋亡。 | |||
T36207 |
Methylspinazarin
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Methylspinazarin is a naphthoquinone bacterial metabolite that has been found in Streptomyces and is an inhibitor of catechol O-methyltransferase (COMT; IC50 = 0.8 μg/ml).1 It is selective for COMT over tyrosine hydroxylase, DOPA decarboxylase, and dopamine-β-hydroxylase at 100 μg/ml. Methylspinazarin decreases blood pressure in spontaneously hypertensive rats when administered at a dose of 50 mg/kg. |1. Chimura, H., Sawa, T., Takita, T., et al. Methylspinazarin and dihydromethylspinazarin, gate... | |||
T36720 |
Deacetylforskolin
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Deacetylforskolin is a diterpene and a derivative of forskolin that has been found inC. forskohliiand has diverse biological activities.1,2,3,4It activates rat adipocyte adenylyl cyclase (IC50= 20 μM) and inhibits glucose transport in rat adipocyte plasma membranes.2Deactylforskolin (30-1,000 μg/kg) reduces blood pressure in spontaneously hypertensive rats.3It also attenuates hypercapnia-induced impairments in the passive avoidance response in mice.4 1.Gabetta, B., Zini, G., and Danieli, B.Minor... | |||
T70883 |
Moexipril-d5
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Moexipril-d5 intended for use as an internal standard for the quantification of moexipril by GC- or LC-MS. Moexipril is a prodrug form of the angiotensin converting enzyme (ACE) inhibitor moexiprilat. It is converted to moexiprilat in vivo by side chain ester hydrolysis. Moexipril inhibits ACE in a cell-free assay (IC50 = 2.7 µM for the rabbit enzyme). It also inhibits phosphodiesterase 4 (IC50s = 38, 160, and 230 µM for PDE4B2, PDE4A5 and PDE4D5, respectively). Moexipril (0.1-30 mg/kg per day) ... | |||
T75137 | BAY-747 | ||
BAY-747 (BAY 1165747) 为一种通过口服生效且具有脑渗透性的sGC刺激剂。它能可逆地逆转L-NAME所诱导的记忆障碍并在大鼠中增强认知功能。BAY-747还可在有意识状态下降低正常血压及自发性高血压大鼠(SHR)的血压。此外,BAY-747在mdx/mTRG2小鼠模型中改善了与Duchenne肌营养不良症(DMD)相关的骨骼肌功能。 | |||
T37496 |
Alamandine
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Alamandine can be formed from angiotensin A by action of ACE-2 or directly from angiotensin-(1-7) by decarboxylation of its aspartate residue. The angiotensin A analog produces effects resembling those of Ang II (1-7). However, it acts independently of the two known vasodilators receptors of the RAS (Mas and angiotensin II type 2). To produce its effects, alamandine binds to the Mas-related receptor, MrgD. A novel orally active formulation of alamandine produced a long-term antihypertensive effe... | |||
T35591 |
Guanfacine-13C,15N3
Guanfacine-13C,15N3 |
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Guanfacine-13C,15N3is intended for us as an internal standard for the quantification of guanfacine by GC- or LC-MS. Guanfacine is an α2-adrenergic receptor (α2-AR) agonist with Kivalues of 93, 1,380, and 3,890 nM for α2A-, α2B-, and α2C-ARs, respectively, in a radioligand binding assay.1It has EC50values of 52, 288, and 602 nM for α2A-, α2B-, and α2C-ARs, respectively, for stimulated [35S]GTPγS binding. It also binds to imidazoline receptor 1 (Ki= 19 nM in a radioligand binding assay).2Guanfacin... | |||
T68616 |
Pentoprilat
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Pentoprilat is a member of a series of l-glutarylindoline-2(S)-carboxylic acid derivatives. Pentopril was evaluated as an inhibitor of a cell-free preparation of angiotensin-converting enzyme (ACE) isolated from rabbit lung. Intravenous administration of incremental doses of pentopril to anesthetized normotensive rats produced a dose-related inhibition of angiotensin I (AI) pressor responses. The onset of inhibition of the A1 pressor response was rapid, and substantial inhibition occurred at 5 m... | |||
T69598 |
Isoproterenol-d7 HCl
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Isoproterenol-d7 is intended for use as an internal standard for the quantification of isoproterenol by GC- or LC-MS. Isoproterenol is an agonist of β1- and β2-adrenergic receptors (β1- and β2-ARs; Kis = 224 and 458 nM, respectively). It is selective for β1- and β2-ARs over β3-ARs (Ki = 1,570 nM). Isoproterenol inhibits contractions in isolated field-stimulated rat vas deferens (EC50 = 45.6 nM). In vivo, isoproterenol (0.33 mg/kg) decreases blood pressure and increases water intake in nephrectom... | |||
T36565 |
Adrenomedullin (13-52) (human) (trifluoroacetate salt)
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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... | |||
T35876 |
Chlorthalidone Impurity G
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Chlorthalidone impurity G is a potential impurity found in commercial preparations of chlorthalidone that has moderate antihypertensive effects. Chlorthalidone is a thiazide-like diuretic that inhibits the Na+/Cl- cotransporter in the distal convoluted tubule of the kidney, which prevents reabsorption of sodium and chloride leading to a reduction in plasma volume and cardiac output. It also inhibits carbonic anhydrase (CA), including the isoforms CAVB, VII, IX, XII, and XIII (Kis = 2.8-23 nM) an... | |||
T36643 |
PKI-166 hydrochloride
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Potent EGFR-kinase inhibitor (IC50 = 0.7 nM). Displays >3000-fold selectivity against a panel of serine/threonine kinases. Reduces metastasis and angiogenesis in a mouse model of pancreatic cancer. Antihypertensive and orally bioavailable. Bruns et al (2000) Blockade of the epidermal growth factor receptor signaling by a novel tyrosine kinase inhibitor leads to apoptosis of endothelial cells and therapy of human pancreatic carcinoma. Cancer Res. 60 2926 PMID:10850439 |Ulu et al (2013) Epidermal ... | |||
T83688 |
R 715 TFA
[Ac-Lys-[D-βNal7,Ile8]des-Arg9]-BK,Ac-Lys-Arg-Pro-Pro-Gly-Phe-Ser-D2Nal-Ile-OH |
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R 715是一种布拉迪肾上腺素B1受体拮抗剂。它抑制在表达布拉迪肾上腺素B1受体的孤立人类脐带中由布拉迪肾上腺素引发的收缩(pA2 = 8.49)。R 715(200、400及600 µg/kg)通过尾部闪烁测试减少了由链脲佐菌素(STZ)诱导的糖尿病神经病变小鼠模型中尾部撤回的潜伏期。它还在以髓磷脂少突胶质细胞糖蛋白(MOG)(35-55)(MOG35-55)抗原肽诱导的实验性自体免疫性脑炎(EAE)小鼠模型中,通过每天1 mg/kg的剂量减少了后肢无力和瘫痪的发病率,改善对称步态,并减少脊髓炎症灶点数、神经元脱髓鞘以及病灶单核细胞侵袭。R 715(0.01 nmol/动物,脑室内)能在自发性高血压大鼠中降低平均动脉血压并增加心率。 |
Cat. No. | Product Name | Target | Signaling Pathways |
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TN2990 |
3alpha-dihydrocadambine
|
Others | Others |
3alpha-Dihydrocadambine exhibits dose-dependent hypotensive and anti-hypertensive effects in anesthetized normotensive rats and in conscious spontaneously hypertensive rats. |