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Cat. No. | Product Name | Target | Signaling Pathways |
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T3474 |
RO 46-8443
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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。 | |||
T10357 |
AR-13324 analog mesylate
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Others | Others |
AR-13324 analog mesylate is an inhibitor of Rho-kinase and a norepinephrine transporter and reduces intraocular pressure in normotensive monkey eyes. | |||
T61180 | GAT564 | ||
GAT564 (Compound 15d) is a highly effective allosteric modulator of cannabinoid 1 receptor (CB1R), having EC50 values of 87 nM and 320 nM for cAMP and β-arrestin2, respectively. It significantly enhances the binding of orthosteric ligands to hCB1R. Moreover, GAT564 exhibits remarkable efficacy as a topical agent, resulting in a significant reduction of intraocular pressure (IOP) in an ocular normotensive murine model of glaucoma [1]. | |||
T37931 |
15(S)-Latanoprost
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15(S)-Latanoprost is an analog of latanoprost in which the hydroxyl at carbon 15 is inverted relative to latanoprost. The IC50 values for the free acid forms of latanoprost and 15(S)-latanoprost were determined to be 3.6 nM and 24 nM, respectively, in a FP receptor binding assay using the cat iris sphincter muscle. A 3 μg dose of 15(S)-latanoprost caused a 1 mmHg reduction of IOP in normotensive cynomolgus monkeys. 15(S)-Latanoprost is a potential impurity in most commercial preparations of the ... | |||
T71205 |
Fosinopril-d7 sodium salt
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Fosinopril-d7 is intended for use as an internal standard for the quantification of fosinopril by GC- or LC-MS. Fosinopril is a prodrug form of the angiotensin-converting enzyme inhibitor fosinoprilat. Oral administration of fosinopril inhibits angiotensin I-induced pressor responses in normotensive rats, dogs, and monkeys when administered at doses of 15, 15, and 10 µmol/kg, respectively. Fosinopril reduces fractional shortening and decreases left ventricular size in a porcine model of congesti... | |||
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... | |||
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... | |||
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... | |||
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。 | |||
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。 |
Cat. No. | Product Name | Target | Signaling Pathways |
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TN2990 |
3alpha-dihydrocadambine
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Others | Others |
3alpha-Dihydrocadambine exhibits dose-dependent hypotensive and anti-hypertensive effects in anesthetized normotensive rats and in conscious spontaneously hypertensive rats. |