ara-g

Ara-G is an analog of the nucleoside guanosine and an active metabolite of nelarabine .1,2 Ara-G accumulates in T lymphoblasts and malignant T-lymphoid cells, where it is phosphorylated to produce ara-GTP and incorporated into the DNA.3,1 Ara-G inhibits DNA replication by 92% after 30 minutes when used at a concentration of 50 μM in CEM cells, which are used as a model for human T lymphoblasts.1 It also halts the cell cycle at the sub-G1 phase and induces apoptosis in CEM cells.3 Syngeneic bone marrow containing 6C3HED tumor cells treated with ara-G (100 mM) ex vivo prior to transplantation increases survival of lethally irradiated mice and induces reconstitution of lymphoid, myeloid, and erythroid cell linages.4References1. Leanza, L., Miazzi, C., Ferraro, P., et al. Activation of guanine-β-D-arabinofuranoside and deoxyguanosine to triphosphates by a common pathway blocks T lymphoblasts at different checkpoints. Exp. Cell Res. 316(20), 3443-3453 (2010).2. Lambe, C.U., Averett, D.R., Paff, M.T., et al. 2-Amino-6-methoxypurine arabinoside: An agent for T-cell malignancies. Cancer Res. 55(15), 3352-3356 (1995).3. Rodriguez, C.O., Jr., Stellrecht, C.M., and Gandhi, V. Mechanisms for T-cell selective cytotoxicity of arabinosylguanine. Blood 102(5), 1842-1848 (2003).4. Kurtzberg, J. Guanine arabinoside as a bone marrow-purging agent. Ann. N.Y. Acad. Sci 685(1), 225-236 (1993). Ara-G is an analog of the nucleoside guanosine and an active metabolite of nelarabine .1,2 Ara-G accumulates in T lymphoblasts and malignant T-lymphoid cells, where it is phosphorylated to produce ara-GTP and incorporated into the DNA.3,1 Ara-G inhibits DNA replication by 92% after 30 minutes when used at a concentration of 50 μM in CEM cells, which are used as a model for human T lymphoblasts.1 It also halts the cell cycle at the sub-G1 phase and induces apoptosis in CEM cells.3 Syngeneic bone marrow containing 6C3HED tumor cells treated with ara-G (100 mM) ex vivo prior to transplantation increases survival of lethally irradiated mice and induces reconstitution of lymphoid, myeloid, and erythroid cell linages.4 References1. Leanza, L., Miazzi, C., Ferraro, P., et al. Activation of guanine-β-D-arabinofuranoside and deoxyguanosine to triphosphates by a common pathway blocks T lymphoblasts at different checkpoints. Exp. Cell Res. 316(20), 3443-3453 (2010).2. Lambe, C.U., Averett, D.R., Paff, M.T., et al. 2-Amino-6-methoxypurine arabinoside: An agent for T-cell malignancies. Cancer Res. 55(15), 3352-3356 (1995).3. Rodriguez, C.O., Jr., Stellrecht, C.M., and Gandhi, V. Mechanisms for T-cell selective cytotoxicity of arabinosylguanine. Blood 102(5), 1842-1848 (2003).4. Kurtzberg, J. Guanine arabinoside as a bone marrow-purging agent. Ann. N.Y. Acad. Sci 685(1), 225-236 (1993).

2'-Deoxy-2'-fluoro-6-S-Methyl-6-thio-ara-guanosine is a Nucleoside Derivative - 6-Modified purine nucleoside; Thio-nucleoside; Fluoro-modified nucleoside.

Fmoc-Lys(tBuO-Ara-Glu(AEEA-AEEA)-OtBu)-OH is a derivative of a tert-butyl ether peptide side chain.

A2AR-agonist-1 (N-(2-(1H-Indol-3-yl)ethyl)adenosine) is a potent A2AR and ENT1 agonist (Ki: 4.39 and 3.47 for A2AR and ENT1. It targets the Adenosine A2A Receptor and Adenosine Transporter for Neuroprotection.

Pargyline (Pargylamine) is a monoamine oxidase inhibitor with antihypertensive properties.

L-Aspartic acid (Aspatofort) is a non-essential amino acid in humans, L-Aspartic acid has an overall negative charge and plays an important role in the synthesis of other amino acids and in the citric acid and urea cycles. Asparagine, arginine, lysine, methionine, isoleucine, and some nucleotides are synthesized from aspartic acid. L-Aspartic acid also serves as a neurotransmitter.

(-)-Aspartic acid (L-Homoproline) is an endogenous amino acid existing in invertebrates and vertebrates. It can regulate testosterone synthesis and is an agonist of NMDA receptor.

D-Asparagine monohydrate is an inactive chiral amino acid widely used in biochemical experiments and drug synthesis research.

Methylbenactyzium Bromide (Semulgin) is an anticonvulsant that is the active metabolite of trimethadione.

Z-Asn-OH (N-Cbz-L-asparagine) is a glycine derivative mainly used in peptide synthesis. By protecting the amino group of asparagine, Cbz-Asn-OH prevents unwanted reactions during its synthesis.

L(+)-Asparagine monohydrate is a non-essential amino acid, participate in neurological and metabolic regulation of tissue cell function.

D-Asparagine (H-D-Asn-OH) serves as a nitrogen source for yeast strains and acts as a competitive inhibitor of L-Asparagine hydrolysis with a Ki of 0.24 mM.

Antitubercular agent-30 has antitubercular activity.

Asparagusic acid is unique to asparagus. It is responsible for the odorous urine excreted after eating asparagus. Its derivatives ihydroasparagusic acid have an anti-inflammatory effect.

PPAR agonist 1 is a dual PPAR α/γ agonist used for lowering blood glucose, lipid levels, cholesterol, and body weight.

β3-AR agonist 1 is a highly selective, and orally available agonist of β3-adrenergic receptor (EC50: 18 nM), being inactive to β1-, β2-, and α1A-AR (β1/β3, β2/β3, and α1A/β3>556-fold).

Antitubercular agent-33, a 2-aminothiazole derivative, exhibits potent anti-tubercular activity against Mycobacterium tuberculosis (Mtb) [1].

β3-AR agonist 2 is a potent and selective agonist of β3-adrenergic receptor (β3-AR with an EC50 of 8 nM).

5-HT1AR Agonist 2 (Compound 4f) is a potent agonist of the 5-HT1A receptor with a Ki value of 10.0 nM. It also binds to SERT, D2, and 5-HT6 receptors with Ki values of 2.8 nM, 23 nM, and 192 nM, respectively. Furthermore, this compound demonstrates stability in microsomes and induces hypothermia in mice.

hA3AR agonist 2 is a potent activator of A3AR, with a Ki value of 3.5 nM.

PPAR agonist6 (compound 5a) acts as an agonist for PPAR, exhibiting EC50 values of 3.6 μM and 2.6 μM for PPARα and PPARβ/δ respectively. Additionally, PPAR agonist6 inhibits the transactivation of a TNFα-dependent NF-κB-driven reporter gene in L929 cells [1].

β2AR agonist 2 (compound 8a) is an agonist of the β2-adrenergic receptor (β2AR). It is a saturated azacyclic compound featuring a 4- to 7-membered heterocycle. The compound has a chiral structure in the -R form by incorporating a carbon with a requisite hydroxyl group, which significantly stimulates glucose uptake in skeletal muscle cells, thereby enhancing cellular glucose uptake (GU). β2AR agonist 2 is applicable in the study of type 2 diabetes (T2D).

Antitubercular agent-42(19) is a selective inhibitor of fatty acyl-AMP ligase (FAAL), demonstrating a MIC90 of 1.4 µg/mL against M. tuberculosis H37Rv, and possesses antitubercular activity.

Antitubercular agent-43 (compound A11) is a potent, orally active antitubercular drug. It exhibits high metabolic stability against human and murine cytochrome P450 enzymes. In an acute tuberculosis mouse model, Antitubercular agent-43 demonstrates antibacterial activity.