• Search chemicals, activators, Inhibitors, APIs, intermediates and raw materials.

1221443-94-2 (A-1165442)

1

Identification

A-1165442 A-1165442
Name A-1165442
Formula C22H20ClF2N3O2
MW 431.86
CAS No. 1221443-94-2
EINECS
Smiles O=C(NC1=CC=CC2=C1C=C(C)N=C2)N[[email protected]]3C4=CC=C(Cl)C=C4OC(CF)(CF)C3
Synonyms A 1165442;A1165442;1-[(4R)-7-Chloro-2,2-bis(fluoromethyl)-3,4-dihydro-2H-chromen-4-yl]-3-(3-methylisoquinolin-5-yl)urea; (R)-1-(7-chloro-2,2-bis(fluoromethyl)chroman-4-yl)-3-(3-methylisoquinolin-5-yl)urea
InChI InChI=1S/C22H20ClF2N3O2/c1-13-7-17-14(10-26-13)3-2-4-18(17)27-21(29)28-19-9-22(11-24,12-25)30-20-8-15(23)5-6-16(19)20/h2-8,10,19H,9,11-12H2,1H3,(H2,27,28,29)/t19-/m1/s1
2

Introduction

Background Information

A-1165442 is a potent, competitive and orally available <b>TRPV1</b> antagonist with an <b>IC<sub>50</sub></b> of 9 nM for human TRPV1. IC50 & Target: IC50: 9 nM (human TRPV1)<sup>[1]</sup> <i><b>In Vitro:</b></i> A-1165442 displays potent, competitive antagonism at recombinant human TRPV1 activated by capsaicin (IC<sub>50</sub>=9 nM) and incomplete blockade of acid-evoked response (62% block at 30 μM). 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 μM) in a broad screening panel (n=74, CEREP) of cell-surface receptors, ion channels, and enzymes<sup>[1]</sup>. <i><b>In Vivo:</b></i> 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 ED<sub>50</sub> of 9.5 μmol/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 ED<sub>50</sub> of 35 μmol/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<sup>[1]</sup>. ......by MedChemexpress Co., Ltd.
3

Protocol(Only for Reference)

Cell Experiment

Animal Experiment

4

Physical and Chemical Properties

Appearance: EBNumber:EB000072463

Storage condition

Solubility

DMSO:10 mM by MedChemexpress Co., Ltd.
5

Mechanism and Indication

Signaling Pathways Membrane Transporter/Ion Channel
Target TRP Channel
Research Area
Indications
6

Clinical Information

Product Name Sponsor & Collaborators Indications Start Date End Date Phase
A-1165442 - No Development Reported
7

Safety Data of A-1165442

8

Spectral Information

9

Suppliers List

Company Price and Availability Country/Region
MedChemexpress Co., Ltd. USA
Shanghai Haoyuan Chemexpress Co., Ltd. China
10

Related Products

Other Forms of 1221443-94-2

Name CAS No Formula MW

Recommended Compounds in TRP Channel

Name CAS No Formula MW
SN 2 823218-99-1 C17H21NO 255.35
SB 366791 472981-92-3 C16H14ClNO2 287.74
Nonivamide 2444-46-4 C17H27NO3 293.4
Tramadol (hydrochloride) 36282-47-0 C16H26ClNO2 299.84
Probenecid 57-66-9 C13H19NO4S 285.36
TRPC6 inhibitor 1333207-63-8 C21H24Cl3N3O 440.79
Imperatorin 482-44-0 C16H14O4 270.28
TRCP6 inhibitor 1333210-07-3 C21H22ClN3O 367.87
Capsazepine 138977-28-3 C19H21ClN2O2S 376.9
Mifamurtide 83461-56-7 C59H109N6O19P 1237.5
Rosiglitazone 122320-73-4 C18H19N3O3S 357.43
D3263 HCl salt 1008763-54-9 C21H32ClN3O3 409.95
D-3263 947257-66-1 C21H31N3O3 373.49
Chembridge 5861528 332117-28-9 C19H23N5O3 369.42
HC-030031 349085-38-7 C18H21N5O3 355.39
ABT 239 460746-46-7 C22H22N2O 330.42
Icilin 36945-98-9 C16H13N3O4 311.29
AMG 517 659730-32-2 C20H13F3N4O2S 430.4
SB-705498 501951-42-4 C17H16BrF3N4O 429.23
Capsaicin 404-86-4 C18H27NO3 305.41

Recommended Compounds in Same Indication

Name CAS No Formula MW
11

Route of Synthesis

12

References

Protocol Reference

13

More Information

A-1165442

Tags: buy 1221443-94-2 IC50 | 1221443-94-2 price | 1221443-94-2 cost | 1221443-94-2 solubility | 1221443-94-2 purchase | 1221443-94-2 manufacturer | 1221443-94-2 research buy | 1221443-94-2 order | 1221443-94-2 MSDS | 1221443-94-2 chemical structure | 1221443-94-2 Storage condition | 1221443-94-2 molecular weight | 1221443-94-2 mw | 1221443-94-2 datasheet | 1221443-94-2 supplier | 1221443-94-2 cell line | 1221443-94-2 NMR | 1221443-94-2 MS | 1221443-94-2 IR | 1221443-94-2 solubility | 1221443-94-2 Safe information | 1221443-94-2 Qc and Spectral Information | 1221443-94-2 Clinical Information | 1221443-94-2 Clinical Trial | 1221443-94-2 Route of Synthesis | 1221443-94-2 storage condition | 1221443-94-2 diseases and conditions | 1221443-94-2 flash point | 1221443-94-2 boiling point | 1221443-94-2 melting point | 1221443-94-2 storage condition | 1221443-94-2 brand