change

Giredestrant (GDC-9545) potently competes with estradiol for binding and induces a conformational change within the ER ligand binding domain. Giredestrant has anti-tumor activity. Giredestrant, a non-steroidal ER ligand, is an orally active and selective estrogen receptor (ER) antagonist.

Archangelicin is a useful organic compound for research related to life sciences. The catalog number is T125179 and the CAS number is 2607-56-9.

Na+-Ca2+Exchanger inhibitory peptide (XIP) is an inhibitor of the Na+-Ca2+ exchanger with a Ki of 200 nM. It acts non-competitively to inhibit Na+-dependent Ca2+ uptake and Na+-dependent Ca2+ efflux in sarcolemmal vesicles.

Elubrixin (SB-656933) inhibits neutrophil CD11b upregulation (IC50 of 260.7 nM) and shape change (IC50 of 310.5 nM). Elubrixin can be used for inflammatory diseases such as inflammatory bowel disease and airway inflammation. Elubrixin is a potent, selective, competitive, reversible and orally active CXCR2 antagonist and an IL-8 receptor antagonist.

EMD57439 is a selective PDE-III inhibitor, showing no significant increase in c-AMP concentration and producing little change in Ca(50).

Enflurane (Efrane), a volatile anaesthetic, is a potent inhibitor of high conductance Ca2+-activated K+ channels of Chara australis. Enflurane is an internal standard in monitoring halogenated volatile anaesthetics by headspace gas chromatography-mass spectrometry. It allows rapid adjustments of anesthesia depth with little change in pulse or respiratory rate.

Lecithin (L-alpha-phosphatidylcholine) is considered a safe source of conventional phospholipids. Phospholipids can change the fatty acid composition and microstructure of animal cell membrane.

Elubiol (dichlorophenyl imidazoldioxolan) is a new broad-spectrum antifungal product of imidazole, which can inhibit the biosynthesis of fungal ergosterol and change the composition of other lipid compounds in the cell membrane. Elubiol is used for skin and hair care in subjects with oily skin or dandruff.

Phosphorylcholine chloride calcium salt tetrahydrate (Phosphocholine chloride calcium salt tet) is a small haptenic molecule, is found in a wide variety of organisms. Human hepatic tumors undergo an elevation in the concentration of phosphorylcholine as the principal metabolic change is observed (PMID: 11076016 ). Phosphorylcholine chloride calcium salt tetrahydrate is the precursor metabolite of choline in the glycine, serine and threonine metabolism pathways (KEGG, map00260) and in intermediate between choline and cytidine-diphosphate choline in the glycerophospholipid metabolism pathway (KEGG, map00564).

2-Amino-2-methyl-1,3-propanediol is an activator of 2-oxoaldehyde dehydrogenase and can also be used as a solid-solid phase change material (PCM) and biological buffer.

Sodium acetate trihydrate is a phase-change energy storage material that releases heat when forming crystals. It can also be used to prepare buffer solutions with a pH of 3.6-5.6 to maintain a stable pH environment, and is widely applied in biochemical and cell biology experiments.

Bavisant dihydrochloride hydrate (JNJ31001074AAC) is a highly selective, orally active antagonist of the human H3 receptor with a novel mechanism of action related to wakefulness and cognition, and it has potential as a treatment for ADHD. In a clinical trial, the mean change from baseline in the total ADHD-RS-IV score at day 42 was -8.8 in the placebo group versus -9.3, -11.2, and -12.2 in the bavisant 1 mg day, 3 mg day, and 10 mg day groups, respectively; however, the change in the 10 mg day group was not statistically superior to placebo (p=0.161). Statistical comparisons of the 1 mg day and 3 mg day groups with placebo based on a step-down closed testing procedure were not performed. Bavisant has completed a phase II ADHD trial, but no results have been reported [1]. Clinical trial: A Study to Characterize the Pharmacokinetics and Effect of Food on JNJ-31001074 in Healthy Volunteers. Phase 2. IC50 Value: Target: H3 receptor in vitro.

Imetit dihydrobromide is a high affinity and effective agonist of histamine H3 and H4 receptors (Ki: 0.3 and 2.7 nM). Imetit mimics the histamine effect in triggering a shape change in eosinophils (EC50: 25 nM).

SBI-425 is an effective and orally bioavailable inhibitor of tissue-nonspecific alkaline phosphatase (TNAP). SBI-425 effectively inhibits TNAP in the vasculature and improves cardiovascular parameters and survival without a detectable change in the bone.

CIM-834 is an orally active, selective inhibitor that targets the coronavirus membrane protein (M protein), exhibiting potent inhibition of viral assembly in both SARS-CoV-2 and SARS-CoV. It binds non-covalently to the short form of the M protein (Mshort), stabilizing it and preventing its conformational change to the long form (Mlong) necessary for virion assembly, thus blocking virus particle formation. CIM-834 holds potential for research in COVID-19 and other coronavirus infections.

CS-VIP 8 TFA is a selective allosteric inhibitor of the WDR5 protein (Ki= 0.008 μM). It induces a conformational change in the MLL1 complex, leading to the dissociation of MLL1 from the complex, thereby inhibiting the MLL1 histone methyltransferase activity and modulating HOX gene expression. CS-VIP 8 TFA shows potential for research in hematological disorders such as leukemia.

U-46619 serinol amide is a derivative of U-46619, acting as a stable analog of Thromboxane A2 (TXA2). It effectively functions as a TXA2 agonist, capable of inducing platelet shape change and aggregation.

RS-104966 is an inhibitor of collagenase that acts by inducing the conformational change in the side-chains of the S1 pocket of MMP-1.

MRS2179 is a competitive P2Y1 receptor antagonist (Kb = 100 nM) with no appreciable activity at P2Y2, P2Y4, or P2Y6 at concentrations up to 30 µM, or at P2Y12 and P2Y13. It inhibits ADP-induced platelet shape change and aggregation (pA2 = 6.55) in vitro a

Dimethylmyleran can promote Haematological change and affect spermatogenesis.

I-SAP is a high affinity TP receptor antagonist. At physiologic pH, I-SAP produces platelet shape change, but not aggregation, with an EC50 value of 9.7 nM. I-SAP binds to human platelets with the maximum binding obtained between pH 6.5 and pH 7.4. In washed human platelets, the Kd for I-SAP is 468 pM at pH 7.4 and 490 pM at pH 6.5.

8-iso PGF3α is an isoprostane produced from the free-radical peroxidation of EPA. While little is known about its biological activity, one report indicates it is inactive in a TP receptor-mediated assay of human platelet shape change, a test in which 8-iso PGF2α has an ED50 value of 1 uM. [1]

CD532 hydrochloride is a potent inhibitor of Aurora A kinase, having an IC50 of 45 nM. It not only blocks the activity of Aurora A kinase but also facilitates the degradation of the protein MYCN. Furthermore, CD532 hydrochloride interacts directly with AURKA, inducing a significant conformational change. Its utility in cancer research has been demonstrated [1][2].

N-(3-hydroxy-7-cis tetradecenoyl)-L-Homoserine lactone is a long-chain N-acyl-homoserine lactone (AHL) produced by some Gram-negative bacteria and is involved in quorum sensing. Quorum sensing enables bacteria to change gene expression based on cues from nearby bacteria and from eukaryotic hosts about nutrients, environmental conditions, or threats. Due to the benefit of quorum sensing for bacterial survival, quorum sensing molecules are potential targets for controlling bacterial infections. In mouse and human leukocyte immunoassays using LPS-stimulated macrophages, N-(3-hydroxy-7-cis tetradecenoyl)-L-homoserine lactone did not have an effect on cytokine or antibody production.