hiv-in-9

HIV-IN-9 (Compound 2b) is an HIV inhibitor with an IC50 of 6.65 μg mL, showing high binding affinity for HIV-RT, and inhibits cytochrome P450 isoenzymes CYP3A4, CYP1A2, CYP2C1, and CYP2D6 [1].

HIV-1 protease-IN-9 (compound 5b), a potent HIV-1 protease inhibitor, exhibits strong antiviral efficacy with a dissociation constant (K_i) of 0.028 nM and a half-maximal inhibitory concentration (IC_50) of 66.8 nM [1].

Mavorixafor trihydrochloride is a selective and orally available CXCR4 antagonist (IC50: 13 nM against CXCR4 125I-SDF binding) and also inhibits the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells and PBMCs (IC50s: 1 and 9 nM).

CDK9-IN-1 is a selective and potent CDK9 inhibitor with antiviral activity used in the study of PRRSV infections.

AMD-070 hydrochloride is a CXCR4 antagonist, is useful for Anti HIV.

5,6-dimethyl-2-Thiouracil is a heterocyclic building block that has been used in the synthesis of anti-HIV-1 pyrimidinones.1 It has also been used as an internal standard for the quantification of thyreostats, including 2-thiouracil, in bovine plasma.2 |1. Navrotskii, M.B. Synthesis and anti-HIV-1 activity of new 2-[(2-phthalimidoethyl)thio]-4(3H)-pyrimidinone derivatives. Pharm. Chem. J. 39(9), 466-467 (2005).|2. Schmidt, K.S. In-house validation and factorial effect analysis of a liquid chromatography-tandem mass spectrometry method for the determination of thyreostats in bovine blood plasma. Anal. Bioanal. Chem. 406(3), 735-743 (2014).

Funalenone is a phenalenone originally isolated from A. niger. It inhibits HIV-1 integrase (IC50 = 10 μM) and HIV-1 replication in human peripheral blood cells transformed by murine leukemia virus (HPB-M(a); IC50 = 1.7 μM) but is less cytotoxic to mammalian HPB-M(a) cells (IC50 = 87 μM). Funalenone selectively inhibits matrix metalloproteinase-1 (MMP-1; IC50 = 170 μM) over MMP-2 and MMP-9, which it inhibits by 18.3 and 38.2%, respectively, when used at a concentration of 400 μM. It also inhibits the bacterial cell wall synthesis enzymes MraY and MurG (IC50s = 25.5 μM in a membrane plate assay) and inhibits growth of S. aureus with a MIC value of 64 μg mL.

HIV-1 inhibitor-15 (compound 9d) is a potent, broad-spectrum inhibitor targeting HIV-1, with EC50 values of 1.7 nM against HIV-1 WT, 4 nM against L100I, 2 nM against K103N, 6 nM against Y181C, and 9 nM against E138K. It exhibits high efficacy, favorable solubility, safety profiles, and oral bioavailability [1].

HIV-IN-8 (Compound 9) is an HIV inhibitor that suppresses HIV replication with an effective concentration (EC50) of 13 μg mL [1].

Tat-HA-NR2B9, comprising an HIV-1 Tat transduction domain fragment, an influenza virus hemagglutinin (HA) epitope-tag, and the C-terminal 9 amino acids of NR2B (NR2B9c), has demonstrated efficacy in reducing infarct size and enhancing neurological function following ischemia-induced cerebral injury in rats [1].

Mavorixafor (AMD-070) is an effective and selective antagonist of CXCR4, with an IC50 value of 13 nM against CXCR4 125I-SDF binding. Mavorixafor inhibits the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells (IC50 = 1 nM) and PBMCs (IC50 = 9 nM).