AM-0466|AM0466|NaV1.7 Inhibitor

Cas No.:	1642113-59-4
Chemical Name:	1-(3-methoxy-2'-(trifluoromethyl)-[1,1'-biphenyl]-4-yl)-2-oxo-N-(pyrimidin-2-yl)-1,2-dihydroquinoline-6-sulfonamide
Synonyms:	AM-0466; AM 0466; AM0466
SMILES:	O=S(NC1=NC=CC=N1)(C2=CC=C(N(C3=CC=C(C4=CC=CC=C4C(F)(F)F)C=C3OC)C(C=C5)=O)C5=C2)=O
Formula:	C₂₇H₁₉F₃N₄O₄S
M.Wt:	552.528
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

AM-0466 is a potent and selective NaV1.7 Inhibitor (Nav 1.7 IC50 = 21 nM; Nav 1.5 IC50 =>30.0 uM. PXR = 22% @10 uM; CYP 2C9 IC50 = 4.6 uM; CYP3A4 TDI IC50 =>50.0 uM.). AM-0466 Affords Robust in Vivo Activity. AM-0466 demonstrated robust pharmacodynamic activity in a NaV1.7-dependent model of histamine-induced pruritus (itch) and additionally in a capsaicin-induced nociception model of pain without any confounding effect in open-field activity.

MSDS

COA

LOT NO.	DOWNLOAD

2018-0101

Cat. No.	Product name	Field of application
DC71376	ABBV-318	ABBV-318 is a potent Nav1.7/ Nav1.8 blocker, with IC50s of 2.8 μM and 3.8 μM for hNav1.7 and hNav1.8, respectively. ABBV-318 can be used for the research of pain.
DC70672	ORM-11372	ORM‐11372 is a potent and highly selective NCX 1.1 inhibitor, inhibits human NCX 1.1 reverse and forward currents with IC50 of 5 and 6 nM respectively.ORM‐11372 weakly inhibits human cardiac sodium 1.5 (I Na) and hERG KV11.1 currents (I hERG) with IC50 of 23.2 and 10.0 uM.ORM‐11372 decreased both the outward and inward currents of hiPSC‐CMs with IC50 of 4.8 and 5.6 nM respectively, reduced the magnitude of outward I NCX (the reverse mode) in rat primary ventricular CMs with IC50 of 11.3 nM.ORM‐11372 concentration‐dependently inhibited the calcium efflux signa with an IC50 of 142 and 164 nM for experimental conditions increasing intracellular calcium and eliciting NCX forward mode activity, repectively.ORM‐11372 induced positive inotropic effects of 18 ± 6% and 35 ± 8% in anaesthetized rats with myocardial infarctions and in healthy rabbits respectively with no other haemodynamic effects.
DC10386	Tenapanor	Tenapanor is an inhibitor of the Na+/H+ exchanger NHE3 with IC50 values of 5 and 10 nM against human and Rat NHE3, respectively.
DC9162	Ranolazine HCl	Ranolazine(RS-43285) is an antianginal agent with antiarrhythmic properties that achieves its effects via a novel mechanism of action (inhibition of the late phase of the inward sodium current), without affecting heart rate or blood pressure (BP).
DC10834	PF-06869206	PF-06869206 is an Orally Bioavailable Selective Inhibitors of the Sodium-Phosphate Cotransporter NaPi2a (SLC34A1).
DC10038	PF-01247324	PF-01247324 is an orally bioavailable, selective and potent NaV1.8 channel blocker that inhibits that exhibits analgesic efficacy in rodent behavioral models of pain.
DC10529	PF 05089771	PF 05089771 is a Nav1.7 channel blocker extracted from patent WO/2010/079443 A1, compound example 788, has an IC50 of 8.6 nM.
DC9796	Nicainoprolhe(Nicainoprol)	Nicainoprolhe is an antiarrhythmic agent,a fast-sodiumchannel blocking drug (class Ib), also protected isolated rat hearts against reperfusion arrhythmias.
DC8797	Lacosamide	Lacosamide (Vimpat; Erlosamide) is a medication developed for the adjunctive treatment of partial-onset seizures and diabetic neuropathic pain.
DC8124	ETH 2120(Sodium ionophore III)	Ionophore suitable for the assay of sodium activity in blood, plasma, serum. etc. with a solvent polymeric membrane electrode.