ca1

Bucladesine sodium (DC2797) is a cAMP analog with cell-permeable properties. Bucladesine sodium is also a cAMP-dependent protein kinase (PKA) activator and a phosphodiester (PDE) inhibitor. Bucladesine sodium has anti-inflammatory activity.

Methocarbamol (AHR 85) is a centrally acting muscle relaxant whose mode of action has not been established. It is used as an adjunct in the symptomatic treatment of musculoskeletal conditions associated with painful muscle spasm.

MEDICA16 is a selective agonist for GPR40 as well as a partial agonist for GPR120. MEDICA16, an ATP-citrate lyase inhibitor, significantly reduces intracellular TG content in gastrocnemius muscle with an increase in insulin sensitivity.

BRCA1-IN-1 is a novel small-molecule-like inhibitor of BRCA1 with an IC50 of 0.53 μM and a Ki of 0.71 μM.

BRCA1-IN-2 is a cell membrane-crossing BRCA1 protein-protein interaction (PPI) inhibitor with antitumor activity that acts by disrupting the interaction of BRCA1 (BRCT)2 with proteins.

ABCA1 inducer 1, a non-lipid inducer of ABCA1, enhances ABCA1 expression in E3 4FAD mice expressing human APOE 3 4, augments the lipidation of apolipoprotein (APOE), and reverses various Alzheimer's disease (AD) phenotypes without increasing triglycerides.

ABCA1 inducer 2 is a non-lipogenic inducer of ABCA1. It increases the expression of ABCA1 by targeting the LXR pathway, thereby reducing lipid accumulation induced by ox-LDL and inhibiting foam cell formation. ABCA1 inducer 2 holds potential as an anti-atherosclerotic agent.

MCA17-1 exhibits superior bioactivity compared to the positive control, obeticholic acid (OCA), in the treatment of liver fibrosis.

TCA1 (TCA 1) is a small molecule with activity against drug-resistant and persistent tuberculosis.

KCa1.1 Channel Activator-1, a hybrid derivative of Quercetin, selectively stimulates the vascular KCa1.1 channels while also blocking CaV1.2 channels. Additionally, it demonstrates weak myorelaxant activity.

KCa1.1 channel activator-2, a hybrid derivative of Quercetin, selectively stimulates the vascular KCa1.1 channels. This compound demonstrates significant myorelaxant activity.

The Anti-BRCA1 Antibody (BR64) is a mouse IgG1, κ chimeric antibody that specifically targets human BRCA1. The recommended isotype control for the Anti-BRCA1 Antibody (BR64) is the Mouse IgG1 kappa, Isotype Control.

Anti-CA19-9 Antibody (1116-NS-19-9) is a mouse IgG1, κ chimeric antibody designed to target human CA19-9. The recommended isotype control for this antibody is Mouse IgG1 kappa, Isotype Control.

Benzthiazide (Lemazide) is used in the therapy of edema and hypertension. Like other thiazides, benzthiazide accelerates water loss from the body (diuretics). They inhibit Na+/Cl- reabsorption from the distal convoluted tubules in the kidneys. Thiazides also cause loss of potassium and an increase in serum uric acid. Thiazides are often used to treat hypertension, but their hypotensive effects are not necessarily due to their diuretic activity. Thiazides have been shown to prevent hypertension-related morbidity and mortality although the mechanism is not fully understood. Thiazides cause vasodilation by activating calcium-activated potassium channels (large conductance) in vascular smooth muscles and inhibiting various carbonic anhydrases in vascular tissue.

Tetrasodium pyrophosphate has inhibitory activity against CA1 and CA2 and is commonly used as a chelating agent, emulsifier and buffer. It is widely used in biochemical experiments and drug synthesis research.

Unifiram is a nootropic agent.1It increases acetylcholine (ACh) release in the rat cerebral cortexin vivoand induces a long-lasting increase in the amplitude of field excitatory postsynaptic potentials (fEPSPs) in the rat hippocampal CA1 region (EC50= 27 nM). It does not bind to serotonin (5-HT), dopamine, muscarinic, nicotinic, adrenergic, glutamate, histamine, opioid, or GABA receptors at 1 μM. Unifiram (0.1 mg kg) improves memory in non-memory-impaired rats in a social learning test.2It also prevents memory deficits induced by the anticholinergic agent scopolamine, nicotinic receptor antagonist mecamylamine, GABABreceptor agonist baclofen, or α2-adrenergic receptor agonist clonidine in the passive avoidance test in mice when administered at a dose of 0.01 mg kg and prevents memory deficits induced by the AMPA kainate glutamate receptor antagonist NBQX at 0.1 mg kg.1 1.Romanelli, M.N., Galeotti, N., Ghelardini, C., et al.Pharmacological characterization of DM232 (unifiram) and DM235 (sunifiram), new potent cognition enhancersCNS Drug Rev.12(1)39-52(2006) 2.Ghelardini, C., Galeotti, N., Gualtieri, F., et al.The novel nootropic compound DM232 (unifiram) ameliorates memory impairment in mice and ratsDrug Develop. Res.56(1)23-32(2002)

In the central nervous system, 2-Arachidonoylglycerol is a second endogenous cannabinoid ligand

N-Stearoyltyrosine (N-(1-Oxooctadecyl)-L-tyrosine) is an analog of Anandamide. It exhibits neuroprotective effects by safeguarding the CA1 region of the hippocampus in a gerbil ischemia-reperfusion model. Additionally, N-Stearoyltyrosine inhibits free radical generation, enhances antioxidant capacity, and reduces IR-induced apoptosis (cell apoptosis).

Nonacosanoic Acid exhibits micromolar-level inhibitory activity against AChE, ChE, CA1, and CA2.

WAY-100635 is a potent 5-HT 1A receptor antagonist with an IC50 = 0.91 nM that abrogates the reduction in hippocampal CA1 pyramidal neuron firing frequency during conditioned reflexes; it also acts as a dopamine D4 receptor agonist with an affinity of 3.3 nM.

UBP714 is a derivative of the NMDA receptor negative allosteric modulator UBP608. It also enhanced NMDAR mediated field EPSPs in the CA1 region of the hippocampus. UBP714 is a novel template for the development of potent and subunit selective NMDAR potent

S-8510 is a GABA-A receptor inverse agonist. S-8510 selectively potentiated pentylenetetrazol-induced convulsion without affecting minimal electroconvulsive shock- or strychnine-induced convulsion in ddY mice. S-8510 ameliorated memory impairment induced

(E)-Ajoene is a disulfide that has been found inA. sativumand has diverse biological activities.1,2,3,4It is active against Gram-positive and Gram-negative bacteria (MICs = 10-250 and 150->500 μg/ml, respectively) and fungi (MICs = 15-50 μg/ml).1(E)-Ajoene inhibits proliferation of a variety of cancer cells, including MDA-MB-231 breast, HeLa cervical, and WHCO1 esophageal cancer cells (IC50s = 18.6, 61, and 39.2 μM, respectively).2It also inhibits human glutathione reductase andT. cruzitrypanothione reductase when used at a concentration of 200 μM.3(E)-Ajoene (25 mg/kg) is neuroprotective in a gerbil model of ischemia-reperfusion injury, reducing reactive astrocytosis and microgliosis in the hippocampal CA1 region.4 1.Yoshida, H., Iwata, N., Katsuzaki, H., et al.Antimicrobial activity of a compound isolated from an oil-macerated garlic extractBiosci. Biotechnol. Biochem.62(5)1014-1017(1998) 2.Kaschula, C.H., Hunter, R., Hassan, H.T., et al.Anti-proliferation activity of synthetic ajoene analogues on cancer cell-linesAnticancer Agents Med. Chem.11(3)260-266(2011) 3.Gallwitz, H., Bonse, S., Martinez-Cruz, A., et al.Ajoene is an inhibitor and subversive substrate of human glutathione reductase and Trypanosoma cruzi trypanothione reductase: Crystallographic, kinetic, and spectroscopic studiesJ. Med. Chem.42(3)364-372(1999) 4.Yoo, D.Y., Kim, W., Nam, S.M., et al.Neuroprotective effects of Z-ajoene, an organosulfur compound derived from oil-macerated garlic, in the gerbil hippocampal CA1 region after transient forebrain ischemiaFood Chem. Toxicol.721-7(2014)

NAP-1 is a compound with anesthetic activity.1 It increases paired-pulse inhibition in the CA1 region of rat hippocampal brain slices when used at a concentration of 100 μM. NAP-1 also induces loss of righting reflex in tadpoles (EC50 = 0.53 μM).References NAP-1 is a compound with anesthetic activity.1 It increases paired-pulse inhibition in the CA1 region of rat hippocampal brain slices when used at a concentration of 100 μM. NAP-1 also induces loss of righting reflex in tadpoles (EC50 = 0.53 μM). References