CD38 inhibitor 1 is a highly potent inhibitor of CD38, with IC50s of 7.3 nM and 1.9 nM for hCD38 and mouse CD38, respectively [1].
体内研究
The CD38 inhibitor (30 mg/kg; oral administration; 2 and 6 hours) notably increases NAD levels in both liver and muscle tissues [1].
作用机制
CD38 inhibitor 1 binds to catalytically active sites of the target[1].
CD38 inhibitor 1 细胞实验
Cell Line
Concentration
Treated Time
Description
References
GD2-CD28z CAR-T cells
10 μM
72 hours
To evaluate the effect of CD38 inhibition on CAR-T cell differentiation and function, results showed CD38 inhibitors promote central memory cell formation and reduce exhaustion marker expression.
Cell Rep Med. 2024 Feb 20;5(2):101400.
CD19-41BBz CAR-T cells
10 μM
72 hours
To evaluate the effect of CD38 inhibition on CAR-T cell differentiation and function, results showed CD38 inhibitors promote central memory cell formation and reduce exhaustion marker expression.
Cell Rep Med. 2024 Feb 20;5(2):101400.
Limb bud-derived mesenchymal cells
100 nM or 1 μM
14 days
To explore the effects of CD38 inhibition on chondrogenic differentiation, results showed that 78c treatment significantly increased the formation of Alcian Blue-positive chondrogenic nodules.
Orthop Surg. 2022 May;14(5):946-954.
CD38 inhibitor 1 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Mice
Unilateral ureteral obstruction (UUO) model
Oral gavage
200 μg/mouse/day
Six consecutive days, once daily
CD38 inhibition significantly restored NAD+ levels in obstructed kidneys and ameliorated obstruction-induced renal fibrosis, partially through mechanisms involving reduced immune cell recruitment and NF-κB signaling.
Mol Cell Proteomics. 2023 Mar;22(3):100510
C57BL/6 mice
Destabilization of the medial meniscus (DMM) model
Intra-articular injection
6 μg/10μl/knee joint
Four times a week for 6 weeks
To evaluate the protective effect of CD38 inhibitor on cartilage degradation in DMM-induced experimental mice, results showed that 78c treatment significantly reduced cartilage degeneration and subchondral bone sclerosis.
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