1. Metabolic Enzyme/Protease Neuronal Signaling Membrane Transporter/Ion Channel
  2. FAAH Potassium Channel
  3. SRP-001

SRP-001 is an orally active, blood-brain barrier-permeable analgesic and antipyretic agent. SRP-001 reduces the expression level of FAAH, mildly inhibits hERG currents, generates AM404 (HY-101388), and maintains the integrity of hepatic tight junctions. SRP-001 exerts analgesic, antipyretic, and antinociceptive effects.

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SRP-001

SRP-001 Chemical Structure

CAS No. : 2290606-49-2

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Description

SRP-001 is an orally active, blood-brain barrier-permeable analgesic and antipyretic agent. SRP-001 reduces the expression level of FAAH, mildly inhibits hERG currents, generates AM404 (HY-101388), and maintains the integrity of hepatic tight junctions. SRP-001 exerts analgesic, antipyretic, and antinociceptive effects[1].

In Vitro

SRP-001 (100 μM) weakly inhibits hERG current in human embryonic kidney cells, with 100 μM reducing current by 21.4%[1].
SRP-001 (100-5000 μg per plate) does not induce reverse mutations in Salmonella typhimurium or Escherichia coli WP2 uvrA strains, with or without metabolic activation, and is non-mutagenic in the Ames assay[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

SRP-001 (32-100 mg/kg; p.o.; administered cumulatively at 60 min intervals) produces dose-dependent analgesic effects in juvenile male Sprague-Dawley rats with CFA-induced inflammatory pain, and increases their paw withdrawal thresholds to mechanical and thermal stimuli[1].
SRP-001 (32-100 mg/kg; p.o.) exerts analgesic effects in aged male Sprague-Dawley rats with inflammatory pain induced by complete Freund's adjuvant (CFA), and its efficacy is comparable to that of acetaminophen (ApAP) at equivalent doses[1].
SRP-001 (32-100 mg/kg; p.o.; single administration) produces dose-dependent analgesic effects in visceral pain models of juvenile mice, aged male mice, and juvenile female mice[1].
SRP-001 (75 mg/kg; p.o.; single administration) exerts antipyretic activity in yeast-induced febrile male CD1 mice, and its core body temperature-lowering effect is similar to that of 75 mg/kg ApAP[1].
SRP-001 (32 mg/kg; i.p.; single administration) produces higher levels of the analgesic metabolite AM404 in the periaqueductal gray (PAG) of Sprague-Dawley rats than 32 mg/kg of ApAP, which provides support for its antinociceptive mechanism of action[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Sprague-Dawley (male, 2 months)[1]
Dosage: 32 mg/kg, 100 mg/kg
Administration: p.o.; cumulative doses 60 minutes apart
Result: Increased paw withdrawal threshold from 18 g to 40 g (32 mg/kg) and 55 g (100 mg/kg) in eVF testing for CFA-injected left hind paw.
Demonstrated comparable or greater antinociceptive efficacy than ApAP at equivalent doses.
Produced significant analgesia in the Hargreaves thermal sensitivity assay at 100 mg/kg.
Molecular Weight

405.47

Formula

C19H23N3O5S

CAS No.
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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Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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SRP-001
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HY-182589
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