2-APB
2-APB (CAS 524-95-8) is a cell-permeable antagonist of Ins(1,4,5)P3-induced calcium release. It inhibits calcium mobilization mediated by the intracellular IP3 receptor (IP3R), an essential component in Ca2+ signaling events such as calcium oscillations and waves. In rat cerebellar microsomes, 2-APB inhibits Ins(1,4,5)P3-induced Ca2+ release with an IC50 of 42 μM. Additionally, it blocks TRPC channels, including TRPC3, TRPC5 (IC50 = 20 μM in HEK-293 cells), and TRPC6. 2-APB is widely utilized in research focusing on intracellular calcium dynamics, channel modulation studies, and oxidative stress-related cell injury.
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| Physical Appearance | A solid |
| Storage | Store at RT |
| M.Wt | 225.1 |
| Cas No. | 524-95-8 |
| Formula | C14H16BNO |
| Solubility | insoluble in H2O; ≥27.85 mg/mL in EtOH; ≥9.4 mg/mL in DMSO |
| Chemical Name | 2-((diphenylboryl)oxy)ethanamine |
| SDF | Download SDF |
| Canonical SMILES | NCCOB(C1=CC=CC=C1)C2=CC=CC=C2 |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Cell experiment:[1] | |
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Cell lines |
Mouse pancreatic acinar cells |
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Reaction Conditions |
10 ~ 100 μM 2-APB |
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Applications |
In mouse pancreatic acinar cells, 2-APB significantly inhibited store-operated Ca2+ (SOC) channel-mediated Ca2+ entry at low concentrations (~ 30 μM). At higher concentrations (~ 100 μM), 2-APB exerted multiple paradoxical effects including inhibition of InsP3-induced Ca2+ release and direct stimulation of Ca2+ release. |
| Animal experiment:[2] | |
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Animal models |
Adult male Sprague-Dawley rats, 250 ~ 300 g |
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Dosage form |
2 or 4 mg/kg Administered intraperitoneally |
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Applications |
In rats with ischemia-reperfusion (I/R) induced testicular injury, 2-APB significantly increased mean levels of superoxide dismutase, total antioxidant capacity and glutathione, and reduced mean malondialdehyde and DNA fragmentation levels, which suggested the antiapoptotic and antioxidative effects of 2-APB. |
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Note |
The technical data provided above is for reference only. |
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References: 1. Choi KJ, Kim KS, Kim SH, et al. Caffeine and 2-aminoethoxydiphenyl borate (2-APB) have different ability to inhibit intracellular calcium mobilization in pancreatic acinar cell. The Korean Journal of Physiology & Pharmacology, 2010, 14(2): 105-111. 2. Sari E, Aksit H, Erken HA, et al. Protective effect of 2-APB on testicular ischemia-reperfusion injury in rats. The Journal of Urology, 2015, 193(3): 1036-1041. |
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