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Firategrast (SB 683699) is an orally active and specific α4β1 α4β7 integrin antagonist that reduces the transport of lymphocytes into the central nervous system (CNS) and decreases multiple sclerosis (MS) activity. It is used in relapsing-remitting multiple sclerosis, associated with modest reductions in CD4, CD8, and CD19 lymphocyte counts in cerebrospinal fluid.

1. Naringenin trimethyl ether (5,7,4'-Trimethoxyflavanone) shows significant molluscicidal activity with a median lethal concentration (LC(5)) of 3.9 μg mL.

Hepsulfam is an anticancer agent. It also displays excellent antileukemic activity (a median IC50: 0.91 μg mL in a panel of different tumors).

Sulfoxaflor (GF 2032) is an agonist of nAChR1 and nAChR2 subtypes and a systemic insecticide that acts on the insect central nervous system. Sulfoxaflor was found to have some effects on peripheral blood lymphocytes and is used to control sap-feeding insects such as brown planthopper, whitefly, peach aphid, and cotton aphid.

Anti-MRSA agent 19 (Compound 1) is an antibiotic that exhibits activity against Staphylococcus aureus. It is active against 40 clinical isolates from the CDC, representing diverse bacterial species with various resistance factors, including resistance to vancomycin, aminoglycoside tetracycline, and oxazolidinone (median MIC=4 μg mL).

R-82913 is a RNA-directed DNA polymerase inhibitor. R 82913 reduce 5-HT2 receptor-mediated DOI-head-shakes in mice. R82913 inhibited the replication of thirteen different strains of HIV-1 in CEM cells with a median IC50 of 0.15 microM. R82913 was 20-fold

PACAP-related peptide (PRP) is an endogenous 29-amino acid peptide that belongs to the secretin/glucagon superfamily of peptides, which includes secretin , glucagon , glucagon-like peptide-1 , GLP-2 , and pituitary adenylate cyclase-activating polypeptide . It is expressed in rat hypothalamus as well as within the nerves of the median eminence, the anterior pituitary, bed nucleus of the stria terminalis, cerebellum, cerebral cortex, and amygdala. PRP is also expressed in vaginal, uterine cervical, uterine horn, fallopian tube, and ovarian tissues from the rat female genital tract and is present in extracts of male testis tissue.

β-Endorphin (1-27) is an endogenous peptide that binds to μ-, δ-, and κ-opioid receptors (Kis = 5.31, 6.17, and 39.82 nM, respectively, in COS-1 cells expressing rat receptors). It binds to rat and mouse brain membrane preparations (IC50s = 1.1 and 5.7 nM, respectively) and induces chemotaxis of human monocytes in vitro when used at a concentration of 1 nM. Intracerebroventricular administration of β-endorphin (1-27) increases the latency to tail withdrawal in response to thermal stimulation in mice with a median antinociceptive dose (AD50) of 1,500 pmol per animal. It inhibits antinociception induced by β-endorphin in mice in response to thermal stimuli when administered at a dose of 65 pmol per animal. In rats, β-endorphin (1-27) does not affect drug-associated place preference when administered at doses up to 20 μg, i.c.v., but inhibits β-endorphin-induced place preference when administered at a dose of 10 μg per animal.

AMP423 is a naphthyl derivative of 2-cyanoaziridine-1-carboxamide with structural similarity to the pro-oxidant anti-tumor agent imexon. AMP423 was active in SCID mice bearing 8226 S myeloma and SU-DHL-6 B-cell lymphoma tumors, with a median tumor growth delay (T-C) of 21 days (P = 0.0002) and 5 days (P = 0.004), respectively, and a median tumor growth inhibition (T C) of 33.3% (P = 0.03) and 82% (P = 0.01), respectively. In non-tumor-bearing mice, AMP423 was not myelosuppressive.

N 0745 inhibits 2-[125I]-iodomelatonin binding to median eminence pars tuberalis membranes with an affinity similar to that of melatonin.

Territrem B is a mycotoxin that irreversibly inhibits acetylcholinesterase (AChE). It is toxic to mice, inducing tremors with a median tremulous dose of 0.21 mg kg.

PROTAC Hemagglutinin Degrader-1 (Compound V3) is a potent degrader of influenza hemagglutinin (HA) with a median degradation concentration of 1.44 μM and broad-spectrum anti-influenza virus activity [1].

PROTAC BTK Degrader-3 is a potent degrader of Bruton's tyrosine kinase (BTK), with a DC50 (median degradation concentration) of 10.9 nM in Mino cells, and shows promise for research into B-cell malignancies, such as chronic lymphoid malignancies [1].

Huwentoxin I (HWTX-I) is a peptide toxin that inhibits voltage-gated sodium channels and N-type calcium channels. It effectively blocks sodium channels in rat hippocampus and cockroach dorsal unpaired median (DUM) neurons, with IC50 values of 66.1 nM and 4.80 nM, respectively [1].

Thromboxane B2 (TXB2) is a compound significantly released from aggregating platelets and undergoes metabolic transformation during circulation into 11-dehydro TXB2 and 2,3-dinor TXB2. The latter, 2,3-dinor TXB2, serves as a prevalent urinary metabolite of TXB2 and acts as an indicator for in vivo TXA2 synthesis. Studies have shown that in healthy male volunteers, the median excretion rate of 2,3-dinor TXB2 is measured at 10.3 ng/hour, equivalent to 138 pg/mg of creatinine.

Angelylalkannin, a naphthoquinone compound isolated from the roots of Alkanna tinctoria, exhibits significant antiproliferative effects on human colon cancer cells HCT-116 and SW-480. The median inhibitory concentration (IC50) of Angelylalkannin is 4.76 mM for HCT-116 cells and 7.03 mM for SW-480 cells. Similar to alkannin, Angelylalkannin induces cell cycle arrest in the G1 phase and cell apoptosis at concentrations ranging from 1-10 mM.

8-Geranyloxypsoralen inhibits α2-secretase (BACE1) activity in non-competitive manner, with the IC(50) values <25.0 μM, it can induce vasorelaxation on rat arterial tissues. 8-Geranyloxypsoralen possesses nematicidal activities, the median lethal concentrations (LC(50)) is 188.3 mg L against B. xylophilus and is 117.5 mg L against P. redivivus.

Fumitremorgen B is a mycotoxin, it exhibits a certain degree of genotoxicity, it can cause DNA damage in human lymphocytes; it shows an inhibitory activity on the cell cycle progression of mouse tsFT210 cells in the M phase, with the MIC value of 26.1 mic