A-1165442

Hersteller MedChem Express
Kategorie
Typ Inhibitors
Specific against other
Menge 10mg
ArtNr HY-12428-10mg
Eclass 6.1 30220300
Eclass 9.0 32160605
Lieferbar
CAS No.
1221443-94-2
Purity
>98%
MW
431, 8629
Formula
C22H20ClF2N3O2
Solubility
DMSO:10 mM
Clinical Phase
No Development Reported
Signalling Pathway
Membrane Transporter/Ion Channel
Target
TRP Channel
Biological Description
A-1165442 is a potent, competitive and orally available TRPV1 antagonist with an IC50 of 9 nM for human TRPV1. IC50 & Target: IC50: 9 nM (human TRPV1)[1] In Vitro: A-1165442 displays potent, competitive antagonism at recombinant human TRPV1 activated by capsaicin (IC50=9 nM) and incomplete blockade of acid-evoked response (62% block at 30 uM). A-1165442 possesses excellent selectivity (>100-fold) versus other members of the TRP family (TRPA1, TRPM8, TRPV2, TRPV3) and other receptors expressed in peripheral sensory neurons including P2X2/3, Cav2.2, Nav channels, and KCNQ2/3. A-1165442 shows minimal cross-reactivity upon evaluation (10 uM) in a broad screening panel (n=74, CEREP) of cell-surface receptors, ion channels, and enzymes[1]. In Vivo: A-1165442 exhibits excellent pharmacological selectivity, has a favorable pharmacokinetic profile, and demonstrates good efficacy against osteoarthritis pain in rodents. Oral administration of A-1165442 prevents capsaicin-induced nocifensive behaviors in rats, with an ED50 of 9.5 umol/kg corresponding to plasma concentration of 420 ng/mL (970 nM). A single dose of A-1165442 produces a robust effect on grip force, with an ED50 of 35 umol/kg measured 1 h postdosing. Repeated dosing of A-1165442 results in an increase in potency relative to acute analgesic efficacy. No significant changes in core body temperature is observed in conscious rats dosed with A-1165442 and this temperature-neutral profile is maintained in conscious dogs[1].
Menge: 10mg
Lieferbar: In stock
Listenpreis: 752,86 €
Preis: 752,86 €
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