Cat. No. | Product Name | Target | Signaling Pathways |
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T11831 |
LDN-27219
|
Others | Others |
LDN-27219 是一种人组织型转谷氨酰胺酶抑制剂(IC50:600 nM)。 | |||
T34146 |
Propanidid
FBA 1420,Epontol,Sombrevin,Fabontal,Fabantol |
GABA Receptor | Membrane transporter/Ion channel; Neuroscience |
Propanidid (Sombrevin) 是一种 γ-氨基丁酸 A 型受体 (GABAA) 激动剂,也是一种可快速发挥作用的静脉注射麻醉剂,可以降低动脉血压。 | |||
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。 | |||
T0112L |
Diltiazem
Diltiazem free base,Dilticard,地尔硫卓,CRD-401,CRD401,Dilzen,CRD 401 |
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Diltiazem is a non-dihydropyridine (non-DHP) calcium channel blocker that relaxes the smooth muscle in arterial walls, thus opening (dilating) arteries, allowing easier blood flow, and lowering blood pressure, and is used to treat hypertension, angina pec | |||
T9881 |
Benzoquinamide hydrochloride
3-carbamoyl-N,N-diethyl-1,3,4,6,7,11b-hexahydro-9,11-dimethoxy-2H-benzo[a]quinolizin-2-yl acetate hydrochloride |
Others | Others |
Benzoquinamide hydrochloride (3-carbamoyl-N,N-diethyl-1,3,4,6,7,11b-hexahydro-9,11-dimethoxy-2H-benzo[a]quinolizin-2-yl acetate hydrochloride) 是一种止吐剂,其增加动脉内压的作用是由于增加了外周血管阻力。 | |||
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。 | |||
T1462 |
Captopril
SQ 14225,甲巯丙脯酸,卡托普利,SQ-14534,SA333 |
RAAS | Endocrinology/Hormones |
Captopril (SA333) 是一种含巯基的,具有口服活性的血管紧张素转换酶(ACE)抑制剂 ,IC50=0.025 μM,广泛应用于高血压和充血性心力衰竭的研究。Captopril 也是NDM-1抑制剂,IC50=7.9 μM。 | |||
T13604 |
CDDO-dhTFEA
|
Others; NF-κB; Nrf2 | Immunology/Inflammation; NF-κB; Others |
CDDO-dhTFEA 是合成的齐墩果烷三萜化合物,可有效激活Nrf2并抑制促炎转录因子NF-κB。 它可以恢复高血压 (MAP),提高 Nrf2 及其靶基因的表达,抑制 NF-κB 的活化和转化生长因子-β 途径,并减少慢性肾病 (CKD) 大鼠的肾小球硬化,间质纤维化和炎症。 | |||
TP1369L |
[Sar9,Met(O2)11]-Substance P acetate
[Sar9,Met(O2)11]-Substance P acetate(110880-55-2 free base) |
Neurokinin receptor | GPCR/G Protein; Neuroscience |
[Sar9,Met(O2)11]-Substance P acetate(110880-55-2 free base) 是一种速激肽 NK1 受体选择性激动剂。它是一种选择性速激肽 NK1 受体激动剂。它和 septide(每只大鼠 10-100 pmol,i.c.v.)在增加平均动脉血压 (MAP) 和心率 (HR),但它们的时间进程不同。两种激动剂都以剂量依赖性方式增加洗脸和吸鼻,而它是一种产生美容效果的化合物。 | |||
T73216 |
Gepefrine
|
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Gepefrine为具口服活性的升压剂及拟交感神经作用剂,能有效改善动脉压早期直立性失调。 | |||
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... | |||
T25237 |
Chloracyzine
Chloroacizine,Chloroacizin,Chlorazicine,Chloroacyzin |
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Chloracyzine can produce a decrease in myocardial oxygen consumption accompanied by a reduction in coronary blood flow preceded by transient coronary dilatation. It produced an insignificant increase in arterial pressure; heart rate increased slightly in | |||
T81916 |
LPLRF-NH2
|
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YMRF-NH2为一种神经肽,能特异性结合FMRFa-R,其半最大有效浓度(EC50)为31 nM。 | |||
TP1923 |
Elabela(19-32)
ELA-14 (human) |
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Potent apelin (APJ) receptor agonist (Ki = 0.93 nM). Bioactive fragment of ELA-32. Activates Gαi1 pathway and β-arrestin-2 recruitment. Reduces arterial pressure in rat hearts. Active in vivo. | |||
T70654 |
Ciprokiren
|
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Ciprokiren is a renin inhibitor discovered by Roche. Ciprokinen inhibited human renin in a buffer and human plasma with an IC50 of 0.07 and 0.65 nmol/L, respectively. In animal models, acute and chronic administration of ciprokinen lead to a reduction in arterial blood pressure. Development of ciprokinen was discontinued at a preclinical stage. | |||
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 | |||
T76633 |
(Phenylac1,D-Tyr(Et)2,Lys6,Arg8,des-Gly9)-Vasopressin
|
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(Phenylac1,D-Tyr(Et)2,Lys6,Arg8,des-Gly9)-Vasopressin 为一种有效的加压素 V1 受体 (VP V1R) 拮抗剂,能显着降低大鼠的平均动脉压 (MAP)。 | |||
T82933 |
Auriculin A
|
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Auriculin A是一种合成ANF,它对血液动力学具有显著效应。该化合物可阻断犬的肾血管收缩,并在兔子的后肢灌注压、心率及动脉血压的全身调节中发挥作用。 | |||
TP1369 |
[Sar9,Met(O2)11]-Substance P TFA(110880-55-2,free)
[Sar9,Met(O2)11]-Substance P TFA |
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[Sar9,Met(O2)11]-Substance P TFA is a selective tachykinin NK1 receptor agonist.[Sar9,Met(O2)11]-Substance P and septide (10-100 pmol per rat, i.c.v.) are equipotent in increasing mean arterial blood pressure (MAP) and heart rate (HR), yet they have dissi | |||
T35867 |
TRAP-6 Peptide (trifluoroacetate salt)
|
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TRAP-6 peptide is a hexapeptide corresponding to residues 42-47 of protease-activated receptor 1 (PAR1). It acts as an agonist of PAR1, inducing platelet aggregation in human platelet-rich plasma ex vivo (EC50 = 0.8 μM). TRAP-6 (0.3 and 0.6 mg/kg) has a triphasic effect on mean arterial blood pressure (MAP) in anesthetized rats with a short decrease, an increase, and then a longer decrease in MAP following intravenous administration. | |||
T35543 |
Methyl Diethyldithiocarbamate
|
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Methyl diethyldithiocarbamate is an active metabolite of the aldehyde dehydrogenase inhibitor disulfiram .1It is produced by methylation of the disulfiram metabolite diethyldithiocarbamate in mouse liver microsomes.2Methyl diethyldithiocarbamate inhibits liver low Kmaldehyde dehydrogenase (ALDH) in rats (ID50= 15.5 mg/kg).1It decreases mean arterial pressure (MAP) and increases heart rate during ethanol challenge in rats when administered at a dose of 20.6 mg/kg. 1.Hart, B.W., Yourick, J.J., and... | |||
T35797 |
Lithocholic acid 3-sulfate disodium
Sulfolithocholic acid disodium |
Others | Others |
Lithocholic acid 3-sulfate disodium (Sulfolithocholic acid disodium) 可作为 RORgammat 配体,抑制 Th17 细胞分化。Lithocholic acid 3-sulfate disodium 是石胆酸(LCA)的硫酸化产物,可诱导细胞损伤。 | |||
T36767 | Parathyroid Hormone (1-13) (trifluoroacetate salt) | ||
Parathyroid hormone (PTH) (1-13) is an N-terminal fragment of PTH (1-34) . In vivo, PTH (1-13) (0.003-1 μmol/kg) increases mean arterial pressure (MAP) in anesthetized rats. | |||
T76044 |
Elabela(19-32) TFA
|
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Elabela(19-32) TFA 是ELABELA(ELA)与apelin受体(APJ)结合的活性片段,能激活Gαi1和β-arrestin-2信号通路,EC50值分别为8.6 nM和166 nM。该化合物可诱导受体内在化,降低动脉压,并对心脏具有正性肌力作用。 | |||
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... | |||
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... | |||
T36241 |
Arecaidine propargyl ester (hydrobromide)
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Arecaidine propargyl ester is an agonist of M2muscarinic acetylcholine receptors (mAChRs).1It selectively binds to M2over M1, M3, M4, and M5mAChRs in CHO cells expressing the human receptors (Kis = 0.0871, 1.23, 0.851, 0.977, and 0.933 μM, respectively). Arecaidine propargyl ester induces contractions in isolated guinea pig atrium (pD2= 8.67). It induces apoptosis and the production of reactive oxygen species (ROS) in U87 and U251 glioblastoma cells when used at a concentration of 100 μM.2Arecai... | |||
T36777 |
Thrombin Receptor Agonist Peptide (trifluoroacetate salt)
|
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Thrombin receptor agonist peptide (TRAP-14) is a 14-amino acid peptide agonist of the α-thrombin receptor. It induces aggregation of washed platelets as well as platelets in citrated and hirudin plasma. TRAP-14 (100 μM) increases the cytosolic calcium concentration in isolated guinea pig pulmonary smooth muscle cells 5-fold over baseline. It increases pulmonary arterial pressure in isolated guinea pig lung when used at a concentration of 1 μM, which is comparable to the effect induced by 10 nM α... | |||
T35858 |
Adrenomedullin (22-52) (human) (trifluoroacetate salt)
|
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Adrenomedullin (22-52) is a C-terminal fragment of adrenomedullin (1-52) . In vitro, adrenomedullin (22-52) reduces basal corticosterone production in a mixture of rat adrenocortical and adrenomedulllary cells. It also reverses increases in ACTH-stimulated corticosterone production induced by adrenomedullin (1-52). Adrenomedulin (22-52) (0.5 and 5 μg/kg/min) has no effect on basal regional cerebral blood flow but reverses increases in regional cerebral blood flow induced by rat adrenomedullin in... | |||
T83766 |
Moexiprilat
RS 10029 |
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Moexiprilat是一种血管紧张素转换酶(ACE; IC50 = 2.1 nM)的抑制剂,也是前药moexipril的一种活性代谢产物。通过侧链酯水解作用,在体内从moexipril转化而来。Moexiprilat (10 nM)能防止初生大鼠心脏成纤维细胞在雌激素或血管紧张素II刺激下的增殖。在以每天50 mg/kg剂量给药的去卵巢小鼠中,降低平均动脉血压,并增加心房钠尿肽水平,这是高血压的一个标志。 | |||
T83785 |
2-Chloroadenosine-5'-O-diphosphate sodium
2-chloro ADP |
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2-Chloroadenosine-5'-O-diphosphate是一种腺苷5'二磷酸(ADP)的衍生物。它在浓度依赖性的方式下,促进了人类富含血小板的血浆中的聚集,并抑制了由前列腺素E2(PGE2)诱导的环磷酸腺苷(cAMP)的产生。2-Chloroadenosine-5'-O-diphosphate引起预收缩的孤立的豚鼠taenia coli条带放松(pD2 = 6.74),降低大鼠的动脉血压。此外,它还抑制了热休克蛋白70(Hsp70)家族成员mortalin的ATP酶活性(人类酶的表观Ki = 45.05 µM)。 | |||
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。 | |||
T83697 |
PAMP-12 (human, mouse, rat, porcine, bovine) TFA
Proadrenomedullin N-terminal 12 Peptide,PAMP (9-20) |
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Proadrenomedullin N-terminal 12 peptide (PAMP-12) 是一种内源性肽段,源自人体肾上腺髓质,对应人类PAMP-20的9-20氨基酸,涉及降低血压。它是MAS相关G蛋白偶联受体家族成员X2 (MRGPRX2) 的激动剂。在表达人MRGPRX2的CHO细胞中,PAMP-12抑制forskolin诱导的cAMP积累(EC50 = 57.2 nM),特异性诱导表达MRGPRX2的CHO细胞的钙离子动员(EC50 = 41 nM),而在表达MRGPRX1、MRGPRX3或MRGPRX4的细胞中则无此效应(在1 µM浓度下)。PAMP-12还能作为烟碱型乙酰胆碱受体(nAChRs)的拮抗剂,抑制carbachol诱导的儿茶酚胺释放(IC50 = 1.3 µM)及钙和钠的流入(IC50分别为0.39 µM和0.87 µM),但不抑制组胺诱导的儿茶酚胺释放或钙和钠的流入(IC50 >1 µM),在初级牛肾上腺嗜铬细胞中有此表现。当以10至50 nmol/kg剂量给予正常血压大鼠时,PAMP-12能降低平均动脉血压。 |