5-ht2c agonist 58

ANN33840 is a novel selective 5-HT2C agonist with >300-fold functional selectivity over 5-HT2B and >70-fold functional selectivity over 5-HT2A, reducing food intake in an acute rat feeding model.

Undecanoic acid (Hendecanoic acid) is a monocarboxylic acid with antimycotic property. Undecanoic acid inhibits the production of exocellular keratinase, lipase and the biosynthesis of several phospholipids in T. rubrum.

ALPHA-PINENE ((-)-Alpha-Pinene) is a bicyclic monoterpene found in pine trees and other plants, including Cannabis with diverse biological activities [1]. It reduces the growth of a panel of seven Gram-positive bacteria, seven Gram-negative bacteria, and eight yeast strains with MIC values of 0.75-1.29, 1.05-1.59, and 0.7-1.17%, respectively [2]. It has insecticidal activity against C. molestus larvae with LC50 values ranging from 47 to 49 mg L.3 ALPHA-PINENE (100 μg ml) induces apoptosis, increases anion superoxide production and DNA fragmentation, and activates caspase-3 in B16 F10 melanoma cells [4]. In a B16 F10 mouse xenograft model, ALPHA-PINENE(100 ml of a 10 mg ml solution) reduces the number of metastatic lung nodules by approximately 7-fold. ALPHA-PINENE(8.6 mg L, aerosol) also increases the time spent in the open arms of the elevated plus maze by approximately 2-fold in mice, indicating anxiolytic-like activity [5].

Indomethacin sodium hydrate (Indometacin sodium hydrate) is an orally active, competitive and reversible COX1 2 inhibitor with potential anti-inflammatory activity in induced migraines, induced gastrointestinal injuries, and may be used in studies of increased intracranial pressure secondary to severe traumatic brain injury and rheumatoid arthritis in adults.

Beauvericin A is a cyclodepsipeptide and derivative of beauvericin originally isolated fromB. bassianathat has diverse biological activities.1,2,3It is active againstM. tuberculosis(MIC = 25 μg/ml) andP. falciparum(IC50= 12 μg/ml).2Beauvericin A is toxic to brine shrimp (LD100= 32 μg/ml).3 1.Gupta, S., Montillor, C., and Hwang, Y.-S.Isolation of Novel Beauvericin Analogues from the Fungus Beauveria bassianaJ. Nat. Prod.58(5)733-738(1995) 2.Nilanonta, C., Isaka, M., Kittakoop, P., et al.Antimycobacterial and antiplasmodial cyclodepsipeptides from the insect pathogenic fungus Paecilomyces tenuipes BCC 1614Planta Med.66(8)756-758(2000) 3.Shi, S., Li, Y., Ming, Y., et al.Biological activity and chemical composition of the endophytic fungus Fusarium sp. TP-G1 obtained from the root of Dendrobium officinale Kimura et MigoRec. Nat. Prod.12(6)549-556(2018)

Emestrin, a mycotoxin originally isolated from *E. striata*, exhibits antimicrobial, immunomodulatory, and cytotoxic activities. It is effective against fungi *C. albicans* and *C. neoformans*, and bacteria *E. coli*, *S. aureus*, and methicillin-resistant *S. aureus* (MRSA; IC50s = 3.94, 0.6, 2.21, 4.55, and 2.21 μg ml, respectively). Emestrin acts as a chemokine (C-C motif) receptor 2 (CCR2) antagonist (IC50 = 5.4 μM in a radioligand binding assay using isolated human monocytes). At 0.1 μg ml, it induces apoptosis in HL-60 cells and causes necrosis in heart, thymus, and liver tissues in mice at doses of 18-30 mg kg.

Potent cholesteryl ester transfer protein (CETP) inhibitor (IC50 = 4 nM in an enzyme-based scintillation proximity assay). Inhibits cholesteryl ester transfer and increases HDL-C levels in vivo. Orally bioavailable. Qiao et al (2015) Triphenylethanamine derivatives as cholesteryl ester transfer protein inhibitors: discovery of N-[(1R)-1-(3-cyclopropoxy-4-fluorophenyl)-1-[3-fluoro-5-(1,1,2,2-tetrafluoroethoxy)phenyl]-2-phenylethyl]-4-fluoro-3-(trifluoromethyl)benzamid J.Med.Chem. 58 9010 PMID:26524347

Geranylgeranoic acid (GGA) is an isoprenoid that has been found inS. chinensisand has anticancer activity.1It induces apoptosis in Huh7 and PLC/PRF/5 human hepatoma cells and MLE-10 transformed mouse hepatocytes, but not primary mouse hepatocytes, when used at concentrations ranging from 1 to 20 μM. GGA (10 μM) induces apoptosis in Huh7 cellsvialoss of the mitochondrial membrane potential and activation of interleukin-1β-converting enzyme (ICE) and cysteine protease precursor 32 (CPP32).2It also inhibits lysine-specific demethylase 1 (LSD1; IC50= 46.97 μM).3 1.Shidoji, Y., and Ogawa, H.Natural occurrence of cancer-preventive geranylgeranoic acid in medicinal herbsJ. Lipid Res.45(6)1092-1103(2004) 2.Shidoji, Y., Nakamura, N., Moriwaki, H., et al.Rapid loss in the mitochondrial membrane potential during geranylgeranoic acid-induced apoptosisBiochem. Biophys. Res. Commun.230(1)58-63(1997) 3.Sakane, C., Okitsu, T., Wada, A., et al.Inhibition of lysine-specific demethylase 1 by the acyclic diterpenoid geranylgeranoic acid and its derivativesBiochem. Biophys. Res. Commun.444(1)24-29(2014)

Resolvin conjugate in tissue regeneration 1 (RCTR1) is a specialized pro-resolving mediator (SPM) biosynthesized from docosahexaenoic acid by isolated human macrophages and apoptotic polymorphonuclear (PMN) neutrophils.1It has been found in human spleen and bone marrow.2RCTR1 is produced via lipoxygenase-mediated oxidation of DHA to 7(S)-8-epoxy-17(S)-HDHA, which is conjugated to glutathione.1,2,3RCTR1 (10 nM) increases phagocytosis ofE. colior apoptotic neutrophils in isolated human monocyte-derived macrophages.2It decreases chemotaxis induced by leukotriene B4in isolated human neutrophils when used at a concentration of 10 nM. RCTR1 (1 and 10 nM) accelerates tissue regeneration in planaria. Intraperitoneal administration of RCTR1 (100 ng/animal) shortens the inflammatory resolution period and decreases inflammatory exudate neutrophil infiltration in a mouse model ofE. coli-induced peritonitis. 1.Dalli, J., Ramon, S., Norris, P.C., et al.Novel proresolving and tissue-regenerative resolvin and protectin sulfido-conjugated pathwaysFASEB J.29(5)2120-2136(2015) 2.de la Rosa, X., Norris, P.C., Chiang, N., et al.Identification and complete stereochemical assignments of the new resolvin conjugates in tissue regeneration in human tissues that stimulate proresolving phagocyte functions and tissue regenerationAm. J. Pathol.188(4)950-966(2018) 3.Rodriguez, A.R., and Spur, B.W.First total synthesis of pro-resolving and tissue-regenerative resolvin sulfido-conjugatesTetrahedron Lett.58(16)1662-1668(2017)

Pantothenate Kinase Inhibitor (PANKi) is a reversible inhibitor of pantothenate kinase (PanK; IC50s = 70, 92, and 25 nM for PanK1β, PanK2, and PanK3, respectively), the rate-limiting enzyme in the synthesis of coenzyme A .1It binds to the ATP-PanK3 complex with an apparent binding constant of 300 nM and exhibits mixed-type inhibition with respect to ATP and pantothenate. PANKi inhibits CoA biosynthesis in C3A cells (IC50= 0.9 μM) with no effect on cell viability when used at concentrations up to 8 μM. PANKi (5 μM) synergizes with BSO to induce ferroptosis in PANC-1 cells and sensitizes the cells to imidazole ketone erastin-induced ferroptosis.2 1.Sharma, L.K., Leonardi, R., Lin, W., et al.A high-throughput screen reveals new small-molecule activators and inhibitors of pantothenate kinasesJ. Med. Chem.58(3)1563-1568(2015) 2.Badgley, M.A., Kremer, D.M., Maurer, H.C., et al.Cysteine depletion induces pancreatic tumor ferroptosis in miceScience368(6486)85-89(2020)

A-971432 is a sphingosine-1-phosphate receptor 5 (S1P5) agonist that is selective for S1P5 over S1P1 and S1P3 (IC50s = 0.006, 0.362, and >10 µM, respectively). It inhibits forskolin-induced cAMP production in CHO cells expressing S1P5 (EC50 = 4.1 nM). A-971432 (1 µM) increases electrical resistance of hCMEC D3 cells in an in vitro blood-brain barrier model, indicating enhanced barrier integrity, and attenuates blood-brain barrier leakage in an R6 2 transgenic mouse model of Huntington's disease when administered at a dose of 0.1 mg kg.[1] [2] A-971432 (0.1 mg kg per day, i.p.) decreases the number of errors made in a horizontal ladder task and increases latency to fall in the rotarod test in R6 2 mice. It also increases spontaneous alternation in the t-maze in aged mice when administered at a dose of 0.1 mg kg.[1] References [1].Hobson, A.D., Harris, C.M., van der Kam, E.L., et al. Discovery of A-971432, an orally bioavailable selective sphingosine-1-phosphate receptor 5 (S1P5) agonist for the potential treatment of neurodegenerative disorders. J. Med. Chem. 58(23), 9154-9170 (2015).[2]. Di Pardo, A., Castaldo, S., Amico, E., et al. Stimulation of S1PR5 with A-971432, a selective agonist, preserves blood-brain barrier integrity and exerts therapeutic effect in an animal model of Huntington's disease. Hum. Mol. Genet. 27(14), 2490-2501 (2018).

Purfalcamine is an orally active, selective Plasmodium falciparum calcium-dependent protein kinase 1 (PfCDPK1) inhibitor with an IC50 of 17 nM and an EC50 of 230 nM, exhibiting antimalarial activity by inducing developmental arrest of malaria parasites at the schizont stage[1][2].

11(Z),14(Z)-Eicosadienoic acid methyl ester is a more lipid soluble form of the ω-6 C20-2 fatty acid 11(Z),14(Z)-eicosadienoic acid , a naturally occurring PUFA. 11(Z),14(Z)-Eicosadienoic acid competitively inhibits inosine 5'-monophosphate dehydrogenase (Ki = 3.1 μM) and inhibits the binding of LTB4 to its receptor on neutrophils (Ki = 3.0 μM). Also, serum levels of eicosadienoic acids negatively correlate with degree of sleep disturbance. Eicosadienoic acids are converted by desaturases, in vivo, to eicosatrienoic acids, which are potent vasodilators.

Ethyl 2-oxo-2-(thiophen-2-yl)acetate is a useful organic compound for research related to life sciences. The catalog number is T65159 and the CAS number is 4075-58-5.

O-PHOSPHO-L-SERINE is an ester of serine and phosphate, which are normal metabolites in human biofluids.O-phospho-L-serine is a phagocytosis inhibitor that inhibits glial cell proliferation and cone cell regeneration after photodamage.

2,4-Di-tert-butylphenol is a common toxic secondary metabolite produced by various groups of organisms.

alpha-Spinasterol glucoside is a natural product for research related to life sciences. The catalog number is TMA1799 and the CAS number is 1745-36-4.

Methyl cis-13-docosenoate is a natural product.