pressor

Losartan Carboxylic Acid (E-3174), a potent AT1 antagonist (Kis: 0.57 nM, rat; 0.67 nM, human), produces a depressor response and vasodilatation. As a metabolite of losartan, it is more potent than losartan in blocking angiotensin II-induced responses in vascular smooth muscle cells.

Lac repressor fragment 33-38 Lys-Arg-Glu-Lys-Val fragment from lac repressor.

p53 tumor suppressor fragment (232-240) is a peptide with the sequence H2N-Lys-Tyr-Met-Cys-Asn-Ser-Ser-Cys-Met-OH, MW= 1066.3. p53 is a tumor suppressor protein that in humans is encoded by the TP53 gene. p53 is crucial in multicellular organisms, where i

Glycyl-L-histidyl-L-lysine is a synthetic hepatotrophic agent and liver cell growth factor that stimulates the production of hepatic erythropoietic factor.

Metaraminol tartrate (Metaradrine tartrate) is a sympathomimetic agent that acts predominantly at alpha-1 adrenergic receptors. It has been used primarily as a vasoconstrictor in the treatment of HYPOTENSION.

Ubiquitination-IN-1 is an inhibitor of ubiquitination and Cksl-Skp2 protein-protein interaction (IC50: 0.17 μM).

BCL6-IN-8c is an orally active and potent inhibitor of B-cell lymphoma 6 (BCL6)-corepressor interaction(IC50 of 0.10 μM in cell-free enzyme-linked immunosorbent assay).

Nanaomycin A, a quinone antibiotics, reactivates silenced tumor suppressor genes in human cancer cells. Nanaomycin A is a selective inhibitor of DNMT3B (IC50 = 500 nM).

NSC622608 is a small-molecule ligand for V-domain Ig suppressor of T-cell activation (VISTA) which is an immune checkpoint that affects the ability of T-cells to attack tumors.

Metoprolol fumarate (CGP 2175C) is a selectively active β1-adrenoceptor antagonist administered orally, exhibiting anti-inflammatory, antitumor, and anti-angiogenic properties.

Onvatilimab (JNJ-61610588) is a human IgG1 κ-anti-Vista (T-cell-activated V-domain Ig inhibitor) monoclonal antibody with antitumor activity, potentially used for treating advanced head and neck cancers.

viFSP1, a species-independent FSP1 inhibitor, effectively induces ferroptosis in FSP1-dependent cells by targeting the highly conserved NAD(P)H binding pocket of FSP1, directly inhibiting its activity. This action results in lipid peroxidation and exhibits anticancer activity [1].

SX-682 is an orally available allosteric inhibitor of CXCR1 and CXCR2 that blocks tumor myeloid suppressor cell recruitment and enhances T cell activation and anti-tumor immunity, with the potential to treat castration-resistant prostate cancer.

Hamamelitannin has cytotoxic, and antibiofilm activities. It increases the susceptibility of S. aureus to antibiotic treatment in in vivo Caenorhabditis elegans and mouse mammary gland infection models. It also has a high protective activity on cell damag

N6-Cyclohexyladenosine (CHA) is a selective agonist of A1 receptor with EC50 of 8.2 Nm. N6-Cyclohexyladenosine exerts anticonvulsant effects and protects against neuronal death. CHA was also found to inhibit the pressor effects of lumbar sympathetic nerve stimulation in rats.

Human Big ET-1 comprises residues 53-90 of the endothelin precursor (preproendothelin). Compared to the mature endothelin-1 (hET-1), the peptide show less vasoconstrictor activity in vitro, but similar pressor effects in vivo. Former CAS-number 121014-53-7.

The big endothelins comprise residues 53-90 (human big ET-1) and 53-91 (porcine big ET-1) of the endothelin precursor (preproendothelin). Compared to the mature endothelin-1 (ET-1), both peptides show less vasoconstrictor activity in vitro, but similar pressor effects in vivo. Former CAS-number 121014-54-8.

Urotensin II is a peptide vasoconstrictor and agonist of the urotensin (UT) receptor (Ki= 2.06 nM for the human recombinant receptor expressed in HEK293 cells).1It stimulates intracellular calcium mobilization in HEK293 cells expressing human and rat UT (EC50s = 0.47 and 0.78 nM, respectively) but decreases intracellular calcium concentration in goby (G. mirabilis) enterocytes when used at a concentration of 500 nM.2Urotensin II (20 mU/ml) stimulates active sodium and chloride absorption across isolated goby posterior intestine in 5% seawater-adapted solution.3In vivo, urotensin II (1.5-150 nmol/kg) decreases diastolic blood pressure and increases heart rate in anesthetized rats.4It also reduces the pressor responses to sympathetic nerve stimulation, norepinephrine , and vasopressin in pithed rats when administered at a dose of 150 nmol/kg. 1.Ames, R.S., Sarau, H.M., Chambers, J.K., et al.Human urotensin-II is a potent vasoconstrictor and agonist for the orphan receptor GPR14Nature401(6750)282-286(1999) 2.Loretz, C.A., and Assad, J.A.Urotensin II lowers cytoplasmic free calcium concentration in goby enterocytes: Measurements using quin2Gen. Comp. Endocrinol.64(3)355-361(1986) 3.Loretz, C.A., Freel, R.W., and Bern, H.A.Specificity of response of intestinal ion transport systems to a pair of natural peptide hormone analogs: Somatostatin and urotensin IIGen. Comp. Endocrinol.52(2)198-206(1983) 4.Gibson, A., Wallace, P., and Bern, H.A.Cardiovascular effects of urotensin II in anesthetized and pithed ratsGen. Comp. Endocrinol.64(3)435-439(1986)

The alpha-adrenoceptors blocking effect of (N-piperidinomethyl)-2-chromanne was studied in vivo and in vitro in the rat. In the pithed rat, (N-piperidinomethyl)-2-chromanne (1 mg/kg i.v.) antagonized the pressor effects induced by alpha agonists. (N-piperidinomethyl)-2-chromanne competitively antagonized the pressor effects of M7 (alpha 2-agonist) and cirazoline (alpha 1-agonist). (N-piperidinomethyl)-2-chromanne antagonized the inhibitory effects of clonidine on presynaptic alpha 2-receptors in stimulated pithed rats.

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 min after administration of the ACE inhibitors. Pentopril hydrolyzed in vivo to the biologically active free-acid form of CGS 13934. It was well tolerated in normal volunteers and hypertensive patients. Pentopril was developed for the treatment of both hypertension and congestive heart failure. Pentopril produced little clinical improvement and no biochemical improvement in a patients with rheumatoid arthritis.

FRAN-12 is a histamine and 5-hydroxytryptamine antagonist with pressor properties.

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 containing quinapril have been used in the treatment of hypertension, heart failure, and diabetic nephropathy.

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 congestive heart failure. Formulations containing fosinopril have been used in the treatment of hypertension and congestive heart failure.

Gepefrine, an orally active pressor and sympathomimetic agent, enhances the initial orthostatic regulation of arterial pressure.