T8380

Bendamustine (SDX105) for the treatment of Non-Hodgkin Lymphomas and Chronic Lymphocytic Leukemia

6-Biotin-17-NAD+ sodium (Biotin-LC-NAD+ sodium) is a biotinylated derivative of NAD+ and can be used to measure NADH dehydrogenase activity.

ε-NAADP+ is a fluorescent derivative of NAADP, known for inducing calcium mobilization. It effectively induces calcium release in sea urchin egg homogenates with an EC50 of 5 µM. The compound exhibits excitation and emission maxima at 275 nm and 410 nm, respectively. Notably, its emission intensity increases three-fold when dissolved in DMSO.

TNP-ATP, a derivative of ATP, acts as an antagonist to the purinergic P2Y1, P2X3, and P2X2/3 receptors, demonstrating selectivity by showing lower inhibitory concentrations (IC50 = 6, 0.9, 7 nM, respectively) compared to the P2X2, P2X4, and P2X7 receptors (IC50 = 2, 15.2, >30 µM, respectively) in HEK293 cells expressing these human receptors. It effectively diminishes acetic acid-induced calcium influx in 1321N1 cells targeting P2X3 and P2X2/3 receptors (IC50 = 100 and 62 nM, respectively) and alleviates pain in a mouse model of visceral pain (ED50 = 6.35 µmol/kg). Moreover, TNP-ATP exhibits a notable fluorescence characteristic, with an emission peak at 547 nm after excitation at 403 nm, which enhances four-fold and shifts to 538 nm when bound to the insulin-degrading enzyme (IDE).

UDP-β-S, serving as a specific agonist for the purinergic P2Y6 receptor, effectively promotes inositol phosphate accumulation in 1321N1 cells containing P2Y6 receptors, with an EC50 value of 28 nM. This selectivity is evident when compared to its effects on cells expressing P2Y1, P2Y2, or P2Y4 receptors, where a concentration of 10 µM is used. Additionally, at a concentration of 1 µM, UDP-β-S stimulates DNA synthesis in isolated rat aorta smooth muscle cells.

5-(3'-Hydroxyphenyl)-γ-Valerolactone (3'-OH-PVL) is a major phenolic catabolite produced from the fermentation of flavan-3-ols (such as catechin and epicatechin) by the gut microbiota. The compound serves as a key biomarker for investigating the biotransformation pathways and stoichiometry of dietary polyphenols within the colon, enabling the assessment of bioavailability and the potential health contributions of flavan-3-ols with varying degrees of polymerization through monitoring its production levels.

Rp-Adenosine-5'-O-(1-thiodiphosphate) (Rp-ADP-α-S), a sulfur-containing isomer of the nucleotide derivative ADP-α-S, acts as an inhibitor of phosphorylase kinase with an inhibition constant (Ki) of 0.53 µM. This compound also induces aggregation in isolated human platelets with an effective concentration (EC50) of 20 µM and promotes relaxation in guinea pig taenia coli that has been precontracted with carbamoylcholine, with an EC50 of 58.9 µM.

Sp-Adenosine-5'-O-(1-thiodiphosphate) (Sp-ADP-α-S), an isomer of the sulfur-containing nucleotide derivative ADP-α-S, functions as an inhibitor of phosphorylase kinase with an inhibition constant (Ki) of 0.53 µM. This compound also promotes aggregation of isolated human platelets with an effective concentration (EC50) of 20 µM and induces relaxation in carbamoylcholine-precontracted guinea pig taenia coli with an EC50 of 58.9 µM.

Rp-Adenosine-5'-O-(1-thiotriphosphate) (Rp-ATP-α-S), a sulfur-containing nucleotide derivative isomer and a purinergic P2Y1 receptor agonist, promotes calcium mobilization in HEK293 cells expressing the human P2Y1 receptor (EC50 = 75 nM). This compound exhibits binding affinity to washed isolated human platelets (Ki = 156 nM) and attenuates ADP-induced aggregation in human platelet-rich plasma (PRP; pA2 = 4.74), as well as inhibits cAMP production triggered by prostaglandin E1 (PGE1) in human PRP (pA2 = 5.26). Furthermore, it triggers relaxation in carbamoylcholine-constricted guinea pig taenia coli strips (EC50 = 56 nM). Rp-ATP-α-S also contributes to the synthesis of cyclic dinucleotides, recognized by bacterial riboswitches.

Sp-Adenosine-5'-O-(1-thiotriphosphate) (Sp-ATP-α-S), an isomer of the ATP-α-S sulfur-containing nucleotide derivative and a purinergic P2Y1 receptor agonist, effectively increases calcium mobilization in HEK293 cells harboring the P2Y1 receptor with an EC50 of 9.4 nM for the human receptor. It also inhibits ADP-induced human isolated platelet aggregation with a Ki value of 4 μM and prompts relaxation in carbamoylcholine-tightened guinea pig taenia coli, achieving an EC50 of 426 nM.