Bioactivity | Dehydronitrosonisoldipine, a derivative of Nisoldipine (HY-17402), is an irreversible and cell-permeant sterile alpha and TIR motif-containing 1 (SARM1) inhibitor. Dehydronitrosonisoldipine acts mainly by blocking SARM1 activation but not its enzymatic activities. Dehydronitrosonisoldipine inhibits SARM1 and axon degenration (AxD) by covalently modifying cysteines, also inhibits the Vincristine-activated cADPR production in neurons. Dehydronitrosonisoldipine can be used for researching neurodegenerative disorders[1]. |
Target | SARM1, Calcium Channel |
Invitro | Dehydronitrosonisoldipine exhibits an IC50 of 4 μM in the SARM1-dN-expression cells, and decreases the cellular cADPR in cells expressing SARM1, but not in expressing SAM-TIR cells[1]. |
Name | Dehydronitrosonisoldipine |
CAS | 87375-91-5 |
Formula | C20H22N2O5 |
Molar Mass | 370.40 |
Appearance | Solid |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | 4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light) |
Reference | [1]. Li WH, et al. Permeant fluorescent probes visualize the activation of SARM1 and uncover an anti-neurodegenerative drug candidate. Elife. 2021 May 4;10:e67381. [2]. Baranda AB, et al. Instability of calcium channel antagonists during sample preparation for LC-MS-MS analysis of serum samples. Forensic Sci Int. 2006 Jan 6;156(1):23-34. |