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GDC-0276 is a potent, selective, reversible and orally active NaV1.7 inhibitor with an IC50 value of 0.4 nM. GDC-0276 is well tolerated and exhibits a good pharmacokinetic profile. GDC-0276 has the potential for the treatment of pain and to address shortcomings of existing pain medications, such as addiction and off-target side effects.
| Molecular Weight | 462.58 |
| Formula | C24H31FN2O4S |
| CAS Number | 1494581-70-2 |
| Form | Solid |
| Solubility (25°C) | DMSO 100 mg/mL (ultrasonic) |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Sodium Channel Products |
|---|
| 5-(N,N-Hexamethylene)-amiloride
5-(N,N-Hexamethylene)-amiloride (Hexamethylene amiloride) is a potent Na+/H+ exchanger inhibitor, which decreases the intracellular pH (pHi) and induces apoptosis in leukemic cells. 5-(N,N-Hexamethylene)-amiloride (Hexamethylene amiloride) is also an inhibitor of the HIV-1 Vpu virus ion channel and inhibits mouse hepatitis virus (MHV) replication and human coronavirus 229E (HCoV229E) replication in cultured L929 cells with EC50s of 3.91 μM and 1.34 μM, respectively. |
| HwTx-IV
Huwentoxin-IV (HwTx-IV) is a 35-residue neurotoxin peptide with potential application as a novel analgesic. Huwentoxin-IV, a component of tarantula venom, potently blocks sodium channels and is an attractive scaffold for engineering a Nav1.7-selective molecule. |
| ST-2560
ST-2560 is a selective inhibitor of the NaV1.7 sodium channel with IC50 value of 39 nM in primates with ≥1000-fold selectivity over other isoforms of the human NaV1.x family. |
| A-317567
A-317567 is a potent acid-sensing ion channel 3 (ASIC-3) inhibitor with an IC50 of 1.025 μM. |
| XPC-6444
XPC-6444 is a highly potent, isoform-selective, and CNS-penetrant NaV1.6 inhibitor (IC50=41 nM for hNaV1.6). |
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