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抑制剂 & 化合物

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Cat. No. Product Name Target Signaling Pathways
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。
T10357 AR-13324 analog mesylate

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

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

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

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)

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

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)

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。

化合物

RO 46-8443
Cat.No: T3474
Synonym:
Target: Endothelin Receptor
AR-13324 analog mesylate
Cat.No: T10357
Synonym:
Target: Others
GAT564
Cat.No: T61180
Synonym:
Target:
15(S)-Latanoprost
Cat.No: T37931
Synonym:
Target:
Fosinopril-d7 sodium salt
Cat.No: T71205
Synonym:
Target:
Quinapril-d5
Cat.No: T71065
Synonym:
Target:
Arecaidine propargyl ester (hydrobromide)
Cat.No: T36241
Synonym:
Target:
Pentoprilat
Cat.No: T68616
Synonym:
Target:
BAY-747
Cat.No: T75137
Synonym:
Target:
PAMP-12 (human, mouse, rat, porcine, bovine) TFA
Cat.No: T83697
Synonym: Proadrenomedullin N-terminal 12 Peptide,PAMP (9-20)
Target:
Cat. No. Product Name Target Signaling Pathways
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.

天然产物

3alpha-dihydrocadambine
Cat.No: TN2990
Synonym:
Target: Others
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