FAAH-IN-10
FAAH-IN-10 is a FAAH inhibitor and TRPV1 antagonist, with an IC50 of 0.57 μM against human FAAH. FAAH-IN-10 regulates FAAH activity, antagonizes TRPV1 activity, and exhibits analgesic and anti-inflammatory activities. FAAH-IN-10 does not induce TRPV1-mediated hyperthermia. FAAH-IN-10 can be used for pain-related research.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Formule: C24H25N3O3S
- Masse moléculaire:435.54
-
Stockage:
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]
-
Activité biologique
-
Chemical Information
- Protocole
- Pureté et documentation
- Références
-
Help & FAQs
Activité biologique
Description
IC50 & Target
[1]|
TRPV1 |
In Vitro
FAAH-IN-10 (Compound 31) potently inhibits capsaicin-induced activation of human TRPV1-transfected HEK-293 cells with an IC50 of 18.81 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
FAAH-IN-10 (5-20 mg/kg; i.p.; single dose) demonstrates dose-dependent anti-inflammatory activity in a carrageenan-induced paw edema model, with greater efficacy than AA-5-HT at equivalent and higher doses[1].
FAAH-IN-10 (5 mg/kg; i.p.; single dose) does not induce TRPV1-mediated hyperthermia in mice at therapeutic doses, maintaining stable core body temperature comparable to vehicle controls[1].
FAAH-IN-10 (10-40 mg/kg; i.p.; single dose) produces dose-dependent analgesia mediated by TRPV1 antagonism in a capsaicin-induced pain model[1].
FAAH-IN-10 (30 mg/kg; i.p.; single dose) exerts part of its analgesic effect via FAAH inhibition, as demonstrated by reversal of efficacy with the CB1 receptor antagonist AM251[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Kunming mice (male, 22-35 g)[1]
-
Dosage:10 mg/kg; 20 mg/kg; 30 mg/kg; 40 mg/kg
-
Administration:i.p.; single dose
-
Result:Significantly reduced licking/biting time in both phase I and phase II at 30 mg/kg, with greater efficacy than positive control AA-5-HT.
Reduced phase II licking/biting time in a dose-dependent manner at 10, 20, and 40 mg/kg.
Significantly reduced phase I licking/biting time compared to vehicle at 40 mg/kg.
-
Animal Model:unstated strain[1]
-
Dosage:5 mg/kg; 10 mg/kg; 20 mg/kg
-
Administration:i.p.; single dose
-
Result:Exhibited superior anti-edema effects relative to AA-5-HT (5 mg/kg) at 5, 10, and 20 mg/kg.
Showed a clear dose-response relationship, with escalating doses producing progressively greater inhibition of paw edema.
-
Animal Model:unstated strain[1]
-
Dosage:5 mg/kg; graded unspecified doses
-
Administration:i.p.; single dose
-
Result:Did not produce a statistically significant increase in core body temperature at any time point up to 180 minutes post-injection, unlike BCTC.
Showed no significant differences in rectal temperature between compound 31-treated groups and vehicle group at all assessed time points in follow-up dose-ranging study.
-
Animal Model:Kunming mice (male, 22-35 g)[1]
-
Dosage:10 mg/kg; 20 mg/kg; 40 mg/kg
-
Administration:i.p.; single dose
-
Result:Significantly reduced licking duration in a dose-dependent manner, with greater reductions observed at higher doses.
-
Animal Model:Kunming mice (male, 22-35 g)[1]
-
Dosage:30 mg/kg
-
Administration:i.p.; single dose
-
Result:Significantly shortened formalin-induced phase II licking/biting time compared to vehicle.
Had its analgesic effect reversed by pretreatment with AM251, which significantly prolonged licking/biting duration.
Chemical Information
-
Masse moléculaire 435.54
-
Formule C24H25N3O3S
-
SMILES
O=C(OC1=CC=CC=C1)NCCCC(N2[C@H](C3=NC(C4=CC=CC=C4)=CS3)CCC2)=O
-
Livraison
Room temperature in continental US; may vary elsewhere.
-
Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocole
-
Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
-
Research Protocol for Inflammation-related Diseases
The NLRP3 inflammasome is a cytosolic innate immune signaling platform that integrates priming signals and danger-signal activation to promote caspase-1 activation, maturation of IL-1β and IL-18, and gasdermin D-mediated pyroptotic cell death. The core experimental logic is to determine whether inflammatory disease phenotypes are driven by increased NLRP3 expression, ASC-containing inflammasome assembly, caspase-1 cleavage, GSDMD cleavage, and extracellular release of IL-1β/IL-18 rather than by nonspecific cell injury alone. The pathway is strongly linked to inflammation-related disease phenotypes because monosodium urate crystals activate NALP3/NLRP3 inflammasome signaling in gout-like crystal inflammation, cholesterol crystals activate NLRP3 inflammasomes in atherogenesis models, and DSS-induced intestinal inflammation has been reported to involve NLRP3 inflammasome activity. However, experimental colitis studies also show context-dependent protective effects of NLRP3 inflammasome co
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
FAAH-IN-10 Related Classifications
HY-184331 Related Classifications
Powered by Bioz
Keywords
- FAAH-IN-10
- FAAH
- TRP Channel
- carrageenan-induced paw edema model
- human TRPV1-transfected HEK-293 cells
- mice
- CB receptor
- capsaicin-induced pain model
- human recombinant FAAH enzyme
- human FAAH
- formalin-induced pain model
- transient receptor potential vanilloid type 1
- fatty acid amide hydrolase
- Inhibitor
- inhibitor
- inhibit