SRP-001
SRP-001 is a blood-brain barrier-permeable and orally effective FAAH inhibitor and analgesic. SRP-001 avoids the CYP450-mediated formation of the hepatotoxic metabolite NAPQI, and primarily promotes the synthesis of AM404 in the periaqueductal gray by inhibiting FAAH, thereby modulating the endocannabinoid system and the TRPV1- and CB1 receptor-mediated pain network. SRP-001 can be used for research on pain and fever.
For research use only. We do not sell to patients.
- CAS No.: 2290606-49-2
- Formula: C19H23N3O5S
- Molecular Weight:405.47
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
TRPV1 |
CB1 |
In Vitro
SRP-001 (0.1-100 µM) is a weak hERG blocker in human embryonic kidney cells, producing 21.4% block at 100 µM[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
| Species | Dose | Route | AUC0-t | AUC0-∞ | T1/2 | Tmax | Cmax |
|---|---|---|---|---|---|---|---|
| Dog[3] | 3 mg/kg | i.v. | 2202 ng·h/mL | 2154 ng·h/mL | 0.7 h | 0.08 h | 3249 ng/mL |
| Dog[3] | 10 mg/kg | i.v. | 7524 ng·h/mL | 7544 ng·h/mL | 1.5 h | 0.08 h | 10584 ng/mL |
| Dog[3] | 30 mg/kg | i.v. | 21550 ng·h/mL | 21501 ng·h/mL | 1.0 h | 0.08 h | 34325 ng/mL |
| Dog[3] | 3 mg/kg | p.o. | 889 ng·h/mL | 871 ng·h/mL | 0.5 h | 0.25 h | 1314 ng/mL |
| Dog[3] | 10 mg/kg | p.o. | 4135 ng·h/mL | 4129 ng·h/mL | 1.3 h | 0.25 h | 4142 ng/mL |
| Dog[3] | 30 mg/kg | p.o. | 12219 ng·h/mL | 12323 ng·h/mL | 3.6 h | 0.58 h | 7607 ng/mL |
In Vivo
SRP-001 (32-100 mg/kg; p.o.; single dose) produces dose-dependent analgesic effects in CFA (HY-153808)-induced chronic inflammatory pain in Sprague-Dawley rats, increasing the paw withdrawal thresholds to mechanical and thermal stimuli[1].
SRP-001 (32-100 mg/kg; p.o.; single dose; detection 30 minutes after administration; testing continues until 1 hour after administration) produces significant analgesic effects in the cold-stimulus tail-flick somatic pain model in young CD1 mice and aged C57BL/6 mice (prolonging the latency of tail withdrawal from cold water)[1].
SRP-001 (32-100 mg/kg; p.o.; 25 minutes after dosing, acetic acid is injected, followed by counting for 10 minutes) produces significant analgesic activity (reduced writhing count) in the 0.4% acetic acid-induced abdominal writhing reflex visceral pain model in young CD1 mice and aged C57BL/6 mice[1].
SRP-001 (32-100 mg/kg; p.o.; single administration) produces dose-dependent analgesia in visceral pain models in young and aged male and young female mice, with an ED50 value lower than that of an equimolar dose of ApAP[1].
SRP-001 (75 mg/kg; p.o.; single dose; body temperature measured 2 hours after administration) exhibits antipyretic activity in LPS (HY-D1056)- or yeast-induced febrile CD1 mice, with an effect comparable to that of Acetaminophen (HY-66005)[1].
SRP-001 (32 mg/kg; i.p. single dose) generates AM404 in the midbrain PAG of CFA-induced inflammatory pain Sprague-Dawley rats[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley (female, 2 months)[1]
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Dosage:32 mg/kg, 100 mg/kg
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Administration:p.o.; single dose
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Result:Increased paw withdrawal threshold from 25 g to 32 g (32 mg/kg) and 40 g (100 mg/kg) in eVF testing for CFA-injected left hind paw.
Produced significant analgesia in the Hargreaves thermal sensitivity assay at 100 mg/kg.
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Animal Model:Sprague-Dawley (male, 20 months)[1]
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Dosage:32 mg/kg, 100 mg/kg
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Administration:p.o.; single dose
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Result:Demonstrated comparable antinociceptive activity to ApAP in eVF testing.
Produced significant analgesia in the Hargreaves thermal sensitivity assay at 100 mg/kg.
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Animal Model:CD1 (young male, young female); C57BL/6 (aged male)[1]
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Dosage:32 mg/kg, 100 mg/kg
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Administration:p.o.; single dose; measured 30 minutes post-dose
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Result:Increased tail withdrawal latency to cold stimulation at both 32 mg/kg and 100 mg/kg across all cohorts.
Achieved ED50 values of 59.98 μmol/kg (young male), 44.924 μmol/kg (young female), and 81.64 μmol/kg (aged male), which were lower than corresponding ApAP ED50 values.
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Animal Model:CD1 (young male, young female); C57BL/6 (aged male)[1]
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Dosage:32 mg/kg, 100 mg/kg
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Administration:p.o.; single dose; the number of writhes was continuously counted for 10 minutes starting 5 minutes after acetic acid injection
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Result:Reduced the number of abdominal writhes at both 32 mg/kg and 100 mg/kg across all cohorts.
Achieved ED50 values of 31.068 μmol/kg (young male), 237.039 μmol/kg (young female), and 22.079 μmol/kg (aged male), which were lower than corresponding ApAP ED50 values.
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Animal Model:CD1[1]
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Dosage:75 mg/kg
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Administration:p.o.; single dose; 2 h
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Result:Reduced core body temperature in febrile mice, demonstrating antipyretic efficacy comparable to ApAP.
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Animal Model:CD1 (male)[1]
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Dosage:75 mg/kg
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Administration:p.o.; single dose; 2 h
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Result:Reduced core body temperature in febrile mice, demonstrating antipyretic efficacy comparable to ApAP.
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Animal Model:Sprague-Dawley[3]
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Dosage:32 mg/kg
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Administration:i.p.; single dose
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Result:AM404 production was highest in the midbrain PAG, with peak levels in the CFA and vehicle co-administration groups.
Minimal to undetectable levels were found in animals exposed solely to CFA or vehicle.
Chemical Information
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CAS No. 2290606-49-2
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Molecular Weight 405.47
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Formula C19H23N3O5S
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SMILES
O=C(CNS(=O)(C1=C(C(N(CC)CC)=O)C=CC=C1)=O)NC2=CC=C(C=C2)O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
SRP-001 Related Classifications
HY-182589 Related Classifications
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