cd-1 mice

GNF2133 is an effective and selective inhibitor of DYRK1A with IC50s of 6.2 nM. GNF2133 can be used in studies about type 1 diabetes.

VU0360172 is a positive allosteric modulator of mGlu5 receptors (EC50 = 16 nM; Ki = 195 nM).

Menin–KMT2A-IN-1 (Compound 20) is an inhibitor of menin–KMT2A, binding to menin with an IC50 of 8 nM, and disrupting the interaction between menin and lysine methyltransferase 2A (KMT2A). It inhibits hERG channels with an IC50 of 65 μM and suppresses MV4-11 cells with an IC50 of 74 nM. Furthermore, Menin–KMT2A-IN-1 exhibits favorable pharmacokinetic properties in CD-1 mice, with an oral bioavailability of 74%.

KR31173 is an AT1 antagonist with an IC50 of 3.27 nM. When labeled with the 11C isotope, KR31173 can be used as a tracer for positron emission tomography (PET). In mice, KR31173 exhibits favorable biodistribution and pharmacological characteristics. It selectively binds to organs in CD-1 mice known to have a high density of AT1 angiotensin receptors.

Androgen receptor-IN-6 (compound 16) is an orally active and potent inhibitor of the androgen receptor (IC50=0.12 μMin vitro), targeting its disordered N-terminal domain (NTD). It demonstrates good permeability in Caco2 cell membranes and exhibits an oral bioavailability (F/%) of 16% in male CD-1 mice.

GZNL-P36 is an orally active inhibitor of SARS-CoV-2 papain-like protease (PLpro), with an IC50 of 6.45 nM. It effectively inhibits SARS-CoV and its variants, showing an EC50 ranging from 58.2 nM to 2.66 μM. In CD-1 mouse models, GZNL-P36 reaches a maximum plasma concentration (Cmax) of 549 ng/mL, with a half-life (T1/2) of 1.45 hours and a bioavailability of 74.7%. Additionally, GZNL-P36 exhibits antiviral activity in mice infected with SARS-CoV-2 XXB.1.

Influenza A virus-IN-14 (Compound 37) is an inhibitor of the influenza A virus (IAV), effectively suppressing H1N1 with an EC50 of 23 nM. It demonstrates low cytotoxicity, with a CC50 exceeding 100 μM, and reduces cytopathic effects while enhancing the survival rate of Calu3 cells. The compound exhibits synergistic effects with the neuraminidase inhibitor Oseltamivir. However, it shows poor pharmacokinetic properties in CD-1 mice.

WRN inhibitor 10 (Compound P24) is an inhibitor of the Werner helicase WRN, with an IC50 of 1.1 nM. It effectively inhibits the proliferation of SW48 cancer cells, with an IC50 of 39 nM. WRN inhibitor 10 exhibits favorable liver microsomal stability and membrane permeability, and demonstrates good pharmacokinetic properties in CD-1 mice.

PRMT5-MTA-IN-1 (Compound A9a) is an inhibitor of the protein arginine methyltransferase PRMT5-MTA. It suppresses the proliferation of colorectal cancer cells HCT116, both wild-type and MTAP del mutants, with IC50 values of 16 nM and 2.47 μM, respectively. Additionally, PRMT5-MTA-IN-1 demonstrates favorable hepatic microsomal stability, membrane permeability, and pharmacokinetic properties in CD-1 mice.

Amitivir (LY 217896) is an inosine monophosphate dehydrogenase inhibitor. Amitivir inhibits the replication of dividing MDCK cells. Amitivir was associated with asymptomatic rises in serum uric acid levels and was ineffective in modifying the virologic or clinical course of experimental influenza A (H1N1) virus infection.

Fanotaprim is a dihydrofolate reductase (DHFR) inhibitor, suppressing the growth of T. gondii strains with a TgDHFR IC50 of 1.57 ± 0.11 nM, a hDHFR IC50 of 308 ± 71 nM, and a hDHFR to TgDHFR selectivity ratio of 196.

Betamethasone 21-phosphate is a synthetic glucocorticoid.1It prevents increases in macrophage and eosinophil numbers in bronchoalveolar lavage fluid (BALF) and decreases in blood leukocyte numbers in a guinea pig model of parainfluenza-3 viral infection when administered at a dose of 8 mg/kg but does not prevent airway hyperresponsiveness after infection.2Betamethasone 21-phosphate inhibits cell infiltration into the aqueous humor in a rat model of endotoxin-induced uveitis when administered topically or subcutaneously at doses of 0.01-1% or 1 mg/kg, respectively.3It increases maximal lung pressure volume curves in fetal sheep when administered to pregnant ewes at 0.75 gestation at doses of 80 and 170 μg/kg.1Betamethasone 21-phosphate increases body weight, impairs learning and memory, increases anxiolytic behavior, and reduces hippocampal neurogenesis in CD-1 mice but reduces body weight and increases neurogenesis with no effect on anxiety in high-anxiety DBA/2 mice when administered at a dose of approximately 25 mg/kg per day in the drinking water for seven weeks.4Formulations containing betamethasone 12-phosphate and betamethasone acetate have been used in the treatment of severe allergic conditions and a variety of immune-related conditions. 1.Loehle, M., Schwab, M., Kadner, S., et al.Dose-response effects of betamethasone on maturation of the fetal sheep lungAm. J. Obstet. Gynecol.202(2)186.e181-186.e187(2010) 2.Leusink-Muis, A., Ten Broeke, R., Folkerts, G., et al.Betamethasone prevents virus-induced airway inflammation but not airway hyperresponsiveness in guinea pigsClin. Exp. Allergy29(Suppl. 2)82-85(1999) 3.Tsuji, F., Sawa, K., Kato, M., et al.The effects of betamethasone derivatives on endotoxin-induced uveitis in ratExp. Eye Res.64(1)31-36(1997) 4.Aiello, R., Crupi, R., Leo, A., et al.Long-term betamethasone 21-phosphate disodium treatment has distinct effects in CD1 and DBA/2 mice on animal behavior accompanied by opposite effects on neurogenesisBehav. Brain Res.278155-166(2015)

1. Dauricine has pulmonary toxicity, can produce pulmonary injury in CD-1 mice by the metabolism of Dauricine mediated by CYP3A. 2. Dauricinec can pass the blood-brain barrier, and that P-glycoprotein has an important role in the transportation of Dauricine across the blood-brain barrier. 3. Dauricine may has anti-tumor effect, can inhibit tumor cells in urinary system and colon cancer cell proliferation, invasion; induce cell apoptosis by suppressing NF-kappaB activity and the expression profile of its downstream genes.

Orphanin FQ(1-11) TFA, a fragment of orphanin FQ or nociceptin (OFQ/N), acts as a powerful NOP receptor (ORL-1; OP4) agonist with a K i of 55 nM. It lacks affinity for μ, δ, κ1, and κ3 receptors (K i >1000 nM), demonstrating specificity, and exhibits analgesic properties in CD-1 mice [1] [2].

(±)-Pantothenic acid ((±)-Pantothenate), a B-vitamin, is crucial for coenzyme A (CoA) biosynthesis in mammalian cells and protects against valproic acid (VPA)-induced neural tube defects (NTD) in CD-1 mice [1].

VNPP433-3β acts as a molecular glue degrader, targeting the androgen receptor (AR) and its splice variants (AR-Vs) as well as MAP kinase-interacting serine/threonine protein kinase Mnk1/2. It effectively inhibits the proliferation of cancer cells LNCaP, C4-2B, and CWR22Rv1, with GI50 values of 0.2, 0.3, and 0.31 μM, respectively. Additionally, VNPP433-3β shows favorable pharmacokinetics in CD-1 mice and suppresses tumor growth in the CWR22Rv1 xenograft mouse model.

Orphanin FQ(1-11) is a peptide fragment containing amino acids 1-11 of Nociceptin. Orphanin FQ(1-11) is a potent agonist of the ORL1/KOR-3 receptor (Ki = 55 nM) and displays no affinity for opioid receptors, including μ, δ, κ1 and κ3 receptors (Ki >1000 nM). Orphanin FQ(1-11) displays analgesic properties in CD-1 mice.

Orphanin FQ(1-11) acetate(178249-41-7 free base) is a peptide fragment containing amino acids 1-11 of Nociceptin. Orphanin FQ(1-11) acetate(178249-41-7 free base) is a potent agonist of the ORL1/KOR-3 receptor (Ki = 55 nM) and displays no affinity for opioid receptors, including μ, δ, κ1 and κ3 receptors (Ki >1000 nM). Orphanin FQ(1-11) acetate(178249-41-7 free base) displays analgesic properties in CD-1 mice.