Network Version
Redafamdastat Data Sheet
| Product Name: | Redafamdastat |
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|---|---|---|
| CAS No.: | 1020315-31-4 | |
| Cat. No.: | HY-14376 | |
| MWt: | 455.43 | |
| Formula: | C23H20F3N5O2 | |
| Purity : | >98% | |
| Solubility: | DMSO : ≥ 100 mg/mL (219.57 mM) | |
| Mechanisms: | Target: Neurological Disease | |
| Biological Activity: | ||
| Redafamdastat is a highly efficacious and selective FAAH inhibitor with IC50 values is 7.2±0.63 nM and 7.4±0.62 nM for hFAAH and rFAAH, respectively. IC50 & Target:IC50: 7.2±0.63 nM (hFAAH), 7.4±0.62 nM (rFAAH)[1] In Vitro: Redafamdastat inhibits FAAH by a covalent, irreversible mechanism involving carbamylation of the active-site serine nucleophile of FAAH with high in vitro potency (kinact/Ki and IC50 values of 40300 M-1s-1 and 7.2 nM, respectively, for human FAAH). Redafamdastat has exquisite selectivity for FAAH relative to other members of the serine hydrolase superfamily as demonstrated by competitive activity-based protein profiling. Redafamdastat completely inhibits FAAH in human and mouse membrane proteomes at both 10 and 100 μM with no off targets[1]. Redafamdastat is completely selective for FAAH, and none of the other FP-reactive serine hydrolases in the tested tissues are inhibited by Redafamdastat even at 100 μM[2]. In Vivo: Oral administration of Redafamdastat at 0.1 mg/kg results in efficacy comparable to that of naproxen at 10 mg/kg in a rat model of inflammatory pain. Oral administration of Redafamdastat causes a significant inhibition of mechanical allodynia measured after 4 h with a minimum effective dose (MED) of 0.1 mg/kg. Furthermore, at 0.1 mg/kg (p.o.), Redafamdastat inhibits the pain response to a comparable degree as the nonsteroidal anti-inflammatory drug naproxen at 10 mg/kg[1]. FAAH is confirmed to be completely inhibited in mice treated with Redafamdastat at 1 and 10 mg/kg p.o. by competitive activity-based protein profiling (ABPP) study[2]. | ||
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