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CM398 is a highly selective, orally active sigma-2 receptor ligand (Ki=0.43 nM), with high sigma-1/sigma-2 selectivity rato (1000-fold). CM398 shows notable affinity for dopamine (Ki=32.90 nM) and serotonin transporters (Ki=244.2 nM). CM398 shows promising anti-inflammatory analgesic effects in the formalin model of inflammatory pain in mice.
| Molecular Weight | 395.49 |
| Formula | C23H29N3O3 |
| CAS Number | 1121931-70-1 |
| Form | Solid |
| Solubility (25°C) | DMSO 250 mg/mL (ultrasonic) |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Sigma Receptor Products |
|---|
| Siramesine hydrochloride
Siramesine (Lu 28-179) hydrochloride is an effective sigma-2 receptor agonist. Siramesine has a nanomolar affinity for sigma-2 receptors (IC50=0.12 nM) and is 140 times more selective for sigma-2 receptors (IC50=17 nM). Siramesine has xC-system inhibitory activity associated with iron death. |
| Siramesine
Siramesine (Lu 28-179) is a potent sigma-2 receptor agonist. Siramesine has a subnanomolar affinity for sigma-2 receptors (IC50=0.12 nM) and exhibits a 140-fold selectivity for sigma-2 receptors over sigma-1 receptors (IC50=17 nM). Siramesine triggers cell death through destabilisation of mitochondria, but not lysosomes. |
| S1RA
S1RA (E-52862) is a potent and selective sigma-1 receptor (σ1R, Ki=17 nM), which showes good selectivity against σ2R (Ki > 1000 nM). |
| Pentoxyverine Citrate
Pentoxyverine citrate is an orally active sigma-1 receptor agonist with Ki values of 41 nM for σ1, 894 nM for σ2, and 75 nM for σ1 in guinea pig brain membranes.Pentoxyverine citrate is also a muscarinic antagonist. |
| Cutamesine dihydrochloride
Cutamesine dihydrochloride (SA4503 dihydrochloride; AGY94806 dihydrochloride) is a novel and selective opioid sigma1 receptor agonist with IC50 of 17.4 nM. |
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