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.
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- CAS No.: 151656-58-5
- 화학식: C13H21NOS·1/2C4H4O4
- 분자량:297.42
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
제품 설명
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
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CAS No. 151656-58-5
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분자량 297.42
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화학식 C13H21NOS·1/2C4H4O4
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SMILES
OC(/C=C\C(O)=O)=O.CC(O)(C1(C2=CSC=C2)CCN(CC1)C)C
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
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