Others

Sovesudil (PHP-201) 是有效的、ATP 竞争性局部作用 Rho 激酶(ROCK)抑制剂。Sovesudil 抑制 ROCK I 和 ROCK II 的IC50分别为 3.7 和 2.3 nM。Sovesudil 可以降低眼压而不引起充血。

SB-682330A 是一种 Raf 激酶抑制剂。

16,17-Dihydroheronamide C 是一种用做 heronamide C 作用模式分析的探针，具有抗真菌作用。

PAR 4 (1-6) 可用于生命科学领域的相关研究。其产品编号为 T36293，CAS号为 225779-44-2。

1-Myristoyl-2-hydroxy-sn-glycero-3-PE is a naturally occurring lysophospholipid. It induces transient increases in intracellular calcium in PC12 cells. Serum levels of 1-myristoyl-2-hydroxy-sn-glycero-3-PE are elevated in patients with malignant breast cancer compared to healthy controls.

Setosusin is a meroterpenoid fungal metabolite originally isolated from C. setosus. It reduces neurotoxicity induced by amyloid-β (Aβ) aggregates in PC12 cells (EC50 = 112.6 μM). In vivo, setosusin (30 mg/kg) induces tremors in mice.

9(R)-HODE is one of several monohydroxylated products of linoleic acid. All known mammalian lipoxygenases appear to catalyze the oxygenation of arachidonic and linoleic acid to give products having strictly the (S) configuration at the site of oxygen insertion. However, both human umbilical vein endothelial cells and bovine aorta endothelial cells have been shown to produce 9(R)-HODE when incubated with linoleic acid. The physiological function of 9(R)-HODE and the enzyme that catalyzes its formation have not been determined.

CAY10726 is an arylurea fatty acid. It decreases ATP production by 28% in MDA-MB-231 breast cancer cells when used at a concentration of 10 μM. CAY10726 decreases proliferation and initiates apoptosis in MDA-MB-231 cells via depletion of the phospholipid cardiolipin and its precursor phosphatidylglycerol from the mitochondrial membrane. In vivo, CAY10726 (2.5-40 mg/kg) reduces tumor volume and increases tumor cell apoptosis in a mouse MDA-MB-231 breast cancer xenograft model in a dose-dependent manner.

CAY10767 is an agonist of peroxisome proliferator-activated receptor α (PPARα; EC50= 37 nM in a reporter assay).1It is greater than 2,700-fold selective for PPARα over PPARγ or PPARδ.

Reveromycin B is a spiroketal bacterial metabolite originally isolated from Streptomyces. It inhibits EGF-induced mitogenic activity in Balb/MK cells (IC50 = 6 μg/ml) and exhibits pH-dependent antifungal activity against C. albicans (MICs = 15.6 and >500 μg/ml at pH 3.0 and 7.4, respectively). Unlike reveromycin A and reveromycin C , reveromycin B does not inhibit proliferation of KB and K562 cells.

5(S)-HETrE is produced by the action of 5-LO when mead acid is the substrate. There are no literature reports of the biological activity or further metabolic fate of 5(S)-HETrE.

Avenaciolide is a water-insoluble fungal metabolite originally isolated from A. avenaceus. It inhibits glutamate transport in isolated rat liver mitochondria (Ki = 8 μM).

(±)8-HDHA is an autoxidation product of docosahexaenoic acid (DHA) in vitro. It is also produced from incubations of DHA in rat liver, brain, and intestinal microsomes. (±)8-HDHA is a potential marker of oxidative stress in brain and retina where DHA is an abundant polyunsaturated fatty acid.

1-Stearoyl-2-adrenoyl-sn-glycero-3-PE is a phospholipid that contains stearic acid and adrenic acid at thesn-1 andsn-2 positions, respectively. 1-Stearoyl-2-adrenoyl-sn-glycero-3-PE levels are inversely correlated with subject age in mitochondria isolated from human post-mortem hippocampus.1 1.Hancock, S.E., Friedrich, M.G., Mitchell, T.W., et al.Decreases in phospholipids containing adrenic and arachidonic acids occur in the human hippocampus over the adult lifespanLipids50(9)861-872(2015)

A number of 17-phenyl trinor prostaglandin F2α (17-phenyl trinor PGF2α) derivatives have been approved for the treatment of glaucoma. Of these, the unsubstituted or meta-substituted aromatic derivatives are the most potent FP receptor agonists. 17-trifluoromethylphenyl trinor PGF2α bears an aromatic ring which is reminiscent of the trifluoromethyl-phenoxy ring of travoprost ((+)-fluprostenol isopropyl ester). As an ocular hypotensive agent, it would be expected that 17-trifluoromethylphenyl trinor PGF2α would act very much like the free acid of travoprost. 17-phenyl trinor PGF2α is a potent luteolytic and abortifacient, with a potency equal to or greater than fluprostenol and cloprostenol.

Cellobiosan is an anhydro sugar formed during biofuel production from the fast pyrolysis of wood.

2,3-Dehydro-3,4-dihydro ivermectin is an analog of ivermectin and an anthelmintic. 2,3-Dehydro-3,4-dihydro ivermectin has activity against L. amazonensis promastigotes and amastigotes ( IC 50 s=13.8 and 3.6 μM, respectively) without inducing cytotoxicity to macrophages ( IC 50 = 65.5 μM).

1-Undecanoyl-rac-glycerol is a monoacylglycerol that contains undecanoic acid at the sn-1 position. It completely inhibits the growth of the bacteria B. cereus, B. subtilis, M. luteus, E. faecalis, and S. aureus when used at concentrations ranging from 250 to 1,500 mg/L.1 1-Undecanoyl-rac-glycerol (0.1 and 0.3 mg/ml) also has antifungal activity against K. marxianus, S. cerevisiae, and C. maltosa.2

Dichloroiodomethane is a natural compound in human beings[1]. [1]. Lalith K. Silva, et al. Quantification of Dichloroiodomethane and Bromochloroiodomethane in Human Blood by Solid-Phase Microextraction Coupled with Gas Chromatography-High-Resolution Mass Spectrometry. Journal of Analytical Toxicology, Volume 30, Issue 9, November-December 2006, Pages 670-678.

9-deoxy-9-methylene Prostaglandin E2 (9-deoxy-9-methylene PGE2) is a stable, isosteric analog of PGE2 . 9-deoxy-9-methylene PGE2 retains the biological profile of PGE2 with fewer side effects. In the rat 9-deoxy-9-methylene PGE2 is equipotent to PGE2 in decreasing blood pressure. It also stimulates the gerbil colon and primate uterus at the same potency as PGE2.

AcylCoA:cholesterol acyltransferase (ACAT) is an intracellular cholesteryl ester synthase tied closely to the absorption of dietary cholesterol. Oleyl analide (OA) is a weak inhibitor of acylCoA:cholesterol acyltransferase (ACAT) with an IC50 of 26 μM. OA and the related glyceride dioleoyl phenylamino propane 1,2-diol have been linked to a syndrome of eosinophilia, excessive T-cell activation, and elevated interleukin-4 (IL-4), soluble IL-2R, and IL-5. The clinical consequences are an acute pulmonary inflammatory reaction followed by chronic neuropathy, myalgia, and autoimmune connective tissue disease, generally referred to as toxic oil syndrome (TOS). Aniline-denatured cooking oil is a source of OA associated with TOS.

7-hydroxy Coumarin sulfate is a phase II metabolite of coumarin that can be used as an internal standard for the analysis of 7-hydroxy coumarin metabolism using GC- or LC-MS.

Pheleuin is a pyrazinone derivative synthesized from a dipeptide aldehyde. Although the biological activity of this compound has not been reported, similar diketopiperazines are known to inhibit calpain and/or regulate S. aureus virulence factor expression.

Seco Rapamycin, also known as Secorapamycin A, is a ring-opened derivative derived from Rapamycin. It has been observed that Seco-rapamycin does not impact the function of mTOR.

7-Deaza-2'-deoxy-7-iodoadenosine is a modified oligonucleotide containing 7-Deazaadenine.

4-Hydroxyphenylbutazone, a metabolite of Phenylbutazone, functions as an effective reducing cofactor for the peroxidase activity of prostaglandin H synthase (PHS). Phenylbutazone is a nonsteroidal anti-inflammatory drug (NSAID) known for its efficiency in this role.

(Rac)-Zevaquenabant ((Rac)-MRI-1867, compound 6b) is a potent and selective antagonist of the cannabinoid receptor type 1 (CB1R) and inducible nitric oxide synthase (iNOS), exhibiting a binding affinity (Ki) of 5.7 nM specifically for CB1R. Due to its characteristics, (Rac)-Zevaquenabant holds promise as an investigative tool in liver fibrosis research.

CU-32 is an inhibitor of cyclic GMP-AMP (cGAMP) synthase (cGAS; IC50= 0.45 μM).1It reduces DNA-, but not Sendai virus-, induced dimerization of IFN regulatory factor 3 in THP-1 cells, indicating selectivity for the cGAS DNA sensing pathway over the RIG-I-MAVS RNA sensing pathway. It is also selective for cGAS over toll-like receptors (TLRs) at 50 μM. CU-32 decreases IFN-stimulatory DNA-induced production of IFN-β in THP-1 cells when used at concentrations of 10, 30, and 100 μM. 1.Padilla-Salinas, R., Sun, L., Anderson, R., et al.Discovery of small-molecule cyclic GMP-AMP synthase inhibitorsJ. Org. Chem.85(3)1579-1600(2020)

93-O17O is a chalcogen-containing cationic lipidoid.1,2It has been used in the generation of lipid nanoparticles (LPNs). LPNs containing 93-O17O localize to the spleen after intravenous injection into mice.1LPNs containing 93-O17O have been used for the delivery of Cre recombinase and ribonucleoproteins for genome editing in mice and for the intratumoral delivery of cGAMP to enhance cross-presentation of tumor antigens.3,2 1.Zhao, X., Chen, J., Qiu, M., et al.Imidazole-based synthetic lipidoids for in vivo mrna delivery into primary T lymphocytesAngew Chem. Int. Ed. Engl.59(45)20083-20089(2020) 2.Chen, J., Qiu, M., Ye, Z., et al.In situ cancer vaccination using lipidoid nanoparticlesSci. Adv.7(19)eabf1244(2021) 3.Li, Y., Yang, T., Yu, Y., et al.Combinatorial library of chalcogen-containing lipidoids for intracellular delivery of genome-editing proteinsBiomaterials178652-662(2018)

2'-F-Bz-dC Phosphoramidite can be used in the synthesis of oligoribonucleotides.

ATX-002 is a property-tunable lipid for RNA drug delivery.

Adenosine 5′-monophosphoramidate sodium is a derivative of adenosine used as an intermediate for nucleotide synthesis. It significantly influences the accumulation of cyclic AMP.

Drimentine C is a terpenylated diketopiperazine antibiotic originally isolated from Actinomycete bacteria. It inhibits proliferation of NS-1 murine β lymphocyte myeloma cells by 63 and 98% in vitro when used at concentrations of 12.5 and 100 μg/ml, respectively.

TAS 205 is an inhibitor of hematopoietic prostaglandin D synthase (H-PGDS; IC50= 55.8 nM).1It is selective for H-PGDS over lipocalin-type PGDS (L-PGDS) at 100 μM, as well as over enzyme and receptor panels at 10 μM. TAS 205 inhibits production of prostaglandin D2induced by A23187 in KU812 human and RBL-2H3 rat basophils with IC50values of 78.3 and 181.3 nM, respectively. It inhibits ovalbumin-induced nasal lavage fluid eosinophil infiltration and late-phase nasal obstruction in an ovalbumin-sensitized guinea pig model of allergic rhinitis when administered at a dose of 30 mg/kg. 1.Aoyagi, H., Kajiwara, D., Tsunekuni, K., et al.Potential synergistic effects of novel hematopoietic prostaglandin D synthase inhibitor TAS-205 and different types of anti-allergic medicine on nasal obstruction in a Guinea pig model of experimental allergic rhinitisEur. J. Pharmacol.875173030(2020)

CAY10657 在生命科学相关研究中具有广泛的应用。

Isomazole hydrochloride is a cardiotonic.