Stavudine is a nucleoside analog that inhibits reverse transcriptase and has in vitro activity against HIV.Target: HIV RT; NRTIsStavudine is a dideoxynucleoside analog that inhibits reverse transcriptase and has in vitro activity against HIV. Stavudine is an analog of thymidine. It is phosphorylated by cellular kinases into active triphosphate. Stavudine triphosphate inhibits the HIV reverse transcriptase by competing with natural substrate, thymidine triphosphate. It also causes termination of DNA synthesis by incorporating into it [1]. Mice were treated for 2 weeks with stavudine d4T (500 mg/kg/day), L-carnitine (200 mg/kg/day) or both drugs concomitantly. Body fatness was assessed by dual energy X-ray absorptiometry, and investigations were performed in plasma, liver, muscle and WAT. D4T reduced the gain of body adiposity, WAT leptin, whole body FAO and plasma ketone bodies, and increased liver triglycerides and plasma aminotransferases with mild ultrastructural abnormalities in hepatocytes [2].Clinical indications: HIV-1 infection FDA Approved Date: June 24, 1994 Toxicity: peripheral neuropathy; lipodystrophy
HBV Seq2 aa:179-186 serve as effective motifs for CTL response in H-2b system after in vitro restimulation of the primed T cells. HBV Seq2 aa:179-186 is a novel epitope identified on the surface antigen of hepatitis B virus[1].
Tenofovir diphosphate disodium is an antiretroviral agent and an inhibitor of DNA polymerases. Tenofovir diphosphate disodium is a substrate of HIV-1 reverse transcriptase (RT). Tenofovir diphosphate disodium can be used for the research of Aids[1].
Amylmetacresol is a local anesthetic and possesses antiviral (such HIV) effect. Amylmetacresol has the potential for the study in sore throat[1].
L-2'-Fd4C, is an l-nucleoside analogue. L-2'-Fd4C has anti-human immunodeficiency virus (HIV) and anti-hepatitis B virus (HBV) activity[1].
Raltegravir (potassium salt) is a potent integrase (IN) inhibitor, used to treat HIV infection.
3-Deazaadenosine (hydrochloride) is an inhibitor of S-adenosylhomocysteine hydrolase, with a Ki of 3.9 µM; 3-Deazaadenosine has anti-inflammatory, anti-proliferative and anti-HIV activity.
Vicriviroc maleate is a potent, selective, oral bioavailable and CNS penetrated antagonist of CCR5, with a Ki of 2.5 nM, and also inhibits HIV-1 in PBMC cells, with IC90s of 3.3 nM (JrFL), 2.8 nM (ADA-M), 1.8 nM (301657), 4.9 nM (JV1083) and 10 nM (RU 570).
F1839-I is a compound that can be isolated from Stachybotrys. F1839-I has weak cytotoxicity and anti-HIV activity with an IC50 value of 15.6 μM[1].
NBD-556 is small molecule mimetic of CD4, NBD-556 recognizes the HIV-1 envelope protein gp120 and induces restructuring of gp120 analogous to CD4 binding.IC50 Value: Target: HIVNBD-556 N-phenyl-N′-(2,2,6,6-tetramethyl-piperidin-4-yl)-oxalamide analogs as a novel class of human immunodeficiency virus type 1 (HIV-1) entry inhibitors that block the gp120–CD4 interaction. Human immunodeficiency virus (HIV-1) interaction with the primary receptor, CD4, induces conformational changes in the viral envelope glycoproteins that allow binding to the CCR5 second receptor and virus entry into the host cell. The small molecule NBD-556 mimics CD4 by binding the gp120 exterior envelope glycoprotein, moderately inhibiting virus entry into CD4-expressing target cells and enhancing CCR5 binding and virus entry into CCR5-expressing cells lacking CD4.
Inophyllum B ((+)-Inophyllum B) is a potent HIV Reverse Transcriptase inhibitor with an IC50 value of 38 nM. Inophyllum B inhibits HIV-1 (IC50=1.4 μM) in vitro cell culture. Inophyllum B can be isolated from the acetone extract of the giant African snail, Achatina fulica[1].
Celgosivir hydrochloride (MDL 28574A) is an α-glucosidase I inhibitor; inhibits bovine viral diarrhoea virus (BVDV) with an IC50 of 1.27 μM in in vitro assay.
HIV-1 inhibitor-51, a non-nucleoside reverse transcriptase inhibitor (NNRTI), exhibits outstanding antiviral activity against WT HIV-1 (IIIB) and a panel of mutant strains. HIV-1 inhibitor-51 has high binding affinity (KD=2.50 μM) and inhibitory activity (IC50=0.03 μM) to WT HIV-1 RT. HIV-1 inhibitor-51 has EC50s of 2.22-53.3 nM for mutant strains(L100I, K103N, Y181C, Y188L, E138K, F227L + V106A, RES056)[1].
HIV-1 inhibitor-3 is a HIV infection inhibitor extracted from patent US2018360927[1].
Pentoxifylline-d6 (BL-191-d6) is the deuterium labeled Pentoxifylline. Pentoxifylline (BL-191), a haemorheological agent, is an orally active non-selective phosphodiesterase (PDE) inhibitor, with immune modulation, anti-inflammatory, hemorheological, anti-fibrinolytic and anti-proliferation effects. Pentoxifylline can be used for the research of peripheral vascular disease, cerebrovascular disease and a number of other conditions involving a defective regional microcirculation[1][2][3].
Daurichromenic acid is a chromene, which can be isolated from the leaves and twigs of Rhododendron dauricum. Daurichromenic acid has potent anti-HIV activity with an EC50 value of 0.00567 μg/mL[1].
Cenicriviroc is a dual CCR2/CCR5 antagonist, also inhibits both HIV-1 and HIV-2, and displays potent anti-inflammatory and antiinfective activity.
β-Rubromycin is a potent and selective inhibitor of human immunodeficiency virus-1 (HIV-1) RNA-directed DNA polymeras (reverse transcriptase). β-Rubromycin is a class of quinone antibacterials[1].
Nelfinavir-d3 (AG1341-d3) is the deuterium labeled Nelfinavir. Nelfinavir (AG-1341) is a potent and orally bioavailable HIV-1 protease inhibitor (Ki=2 nM) for HIV infection. Nelfinavir is a broad-spectrum, anticancer agent[1][2][3].
Fasudil (HA-1077; AT877) hydrochloride semihydrate is a nonspecific RhoA/ROCK inhibitor and also has inhibitory effect on protein kinases, with an Ki of 0.33 μM for ROCK1, IC50s of 0.158 μM and 4.58 μM, 12.30 μM, 1.650 μM for ROCK2 and PKA, PKC, PKG, respectively. Fasudil hydrochloride semihydrate is also a potent Ca2+ channel antagonist and vasodilator[1][2][3].