EXP631
EXP631 is a centrally acting non-opioid analgesic that targets serotonin and norepinephrine transporters. EXP631 exhibits activity against acute pain induced by chemical stimuli, stress, and electrical stimulation. EXP631 blocks the reuptake of serotonin and norepinephrine. EXP631 can be used in research related to moderate to moderately severe acute and chronic pain.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- CAS No.: 151656-58-5
- Formule: C13H21NOS·1/2C4H4O4
- Masse moléculaire:297.42
-
Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Activité biologique
Description
In Vitro
EXP631 is isolated and structurally identified in rat plasma, confirming its conversion to the N-demethylated metabolite (II). The EI mass spectrum of this metabolite shows a molecular ion peak at m/z 225, and the [M+H]+ peak in its NH3-CI mass spectrum is at m/z 226[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
| Species | Dose | Route | Cmax | Tmax | AUC | T1/2 | Bioavailability | CL | V | Vd |
|---|---|---|---|---|---|---|---|---|---|---|
| Rat[1] | 5.0 mg/kg | i.v. | / | / | 1.11 μg·h/mL | 1.06 h | / | 3.67 L/h/kg | / | 5.63 L/kg |
| Rat[1] | 5.0 mg/kg | p.o. | 0.94 μg/mL | 0.31 h | 1.05 μg·h/mL | 1.44 h | 92 % | / | / | / |
| Rat[1] | 10.0 mg/kg | p.o. | 1.07 μg/mL | 0.75 h | 2.62 μg·h/mL | 1.51 h | 117 % | / | / | / |
| Rat[1] | 20.0 mg/kg | p.o. | 2.26 μg/mL | 1.19 h | 5.84 μg·h/mL | 1.99 h | 131 % | / | / | / |
| Dog[1] | 3.0 mg/kg | i.v. | / | / | 3.14 μg·h/mL | 2.48 h | / | 0.77 L/h/kg | 2.77 L/kg | / |
| Dog[1] | 10.0 mg/kg | p.o. | 2.46 μg/mL | 0.33 h | 8.46 μg·h/mL | 3.49 h | 81 % | / | / | / |
| Dog[1] | 8.0 mg/kg | i.v. | / | / | 10.68 μg·h/mL | 2.58 h | / | 0.62 L/h/kg | 2.29 L/kg | / |
| Dog[1] | 8.0 mg/kg | p.o. | 2.05 μg/mL | 1.38 h | 12.11 μg·h/mL | 5.53 h | 115 % | / | / | / |
Chemical Information
-
CAS No. 151656-58-5
-
Masse moléculaire 297.42
-
Formule C13H21NOS·1/2C4H4O4
-
SMILES
OC(/C=C\C(O)=O)=O.CC(O)(C1(C2=CSC=C2)CCN(CC1)C)C
-
Livraison
Room temperature in continental US; may vary elsewhere.
-
Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Keywords
- EXP631
- 151656-58-5
- EXP 631
- EXP-631
- Serotonin Transporter
- Monoamine Transporter
- animal models
- pressure-induced pain
- serotonin reuptake
- chronic pain
- serotonin transporters
- norepinephrine reuptake
- acute pain
- acute chemically induced pain
- norepinephrine transporters
- electrical-stimulation pain
- Inhibitor
- inhibitor
- inhibit