Nerigliatin

Investigational

Details

Stereochemistry	ACHIRAL
Molecular Formula	C22H20N6O4
Molecular Weight	432.432
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

SMILES

CN(C)C(=O)C1=NC=C(OC2=CC(=CC3=C2C=C(C)O3)C(=O)NC4=NC=C(C)N=C4)C=N1

InChI

InChIKey=MASKQITXHVYVFL-UHFFFAOYSA-N

InChI=1S/C22H20N6O4/c1-12-8-24-19(11-23-12)27-21(29)14-6-17-16(5-13(2)31-17)18(7-14)32-15-9-25-20(26-10-15)22(30)28(3)4/h5-11H,1-4H3,(H,24,27,29)

HIDE SMILES / InChI

Approval Year

Targets

Targets

Primary Target	Pharmacology	Condition	Potency
Glucokinase 2	Activator 1,447		0.19 µM [EC50]

C_max

Value	Dose	Analyte	Population
38.22 ng/mL	10 mg single, oral	PF-04937319 plasma	Homo sapiens
69.49 ng/mL	30 mg single, oral	PF-04937319 plasma	Homo sapiens
119.4 ng/mL	50 mg single, oral	PF-04937319 plasma	Homo sapiens
245.4 ng/mL	100 mg single, oral	PF-04937319 plasma	Homo sapiens
449.3 ng/mL	300 mg single, oral	PF-04937319 plasma	Homo sapiens
57.73 ng/mL	10 mg 1 times / day multiple, oral	PF-04937319 plasma	Homo sapiens
122.3 ng/mL	30 mg 1 times / day multiple, oral	PF-04937319 plasma	Homo sapiens
234.1 ng/mL	50 mg 1 times / day multiple, oral	PF-04937319 plasma	Homo sapiens
421.5 ng/mL	100 mg 1 times / day multiple, oral	PF-04937319 plasma	Homo sapiens
970.6 ng/mL	300 mg 1 times / day multiple, oral	PF-04937319 plasma	Homo sapiens
51.09 ng/mL	10 mg 1 times / day steady-state, oral	PF-04937319 plasma	Homo sapiens
79.3 ng/mL	30 mg 1 times / day steady-state, oral	PF-04937319 plasma	Homo sapiens
171.3 ng/mL	50 mg 1 times / day steady-state, oral	PF-04937319 plasma	Homo sapiens
251.5 ng/mL	100 mg 1 times / day steady-state, oral	PF-04937319 plasma	Homo sapiens
555.9 ng/mL	300 mg 1 times / day steady-state, oral	PF-04937319 plasma	Homo sapiens

AUC

Value	Dose	Analyte	Population
407 ng × h/mL	10 mg single, oral	PF-04937319 plasma	Homo sapiens
867.7 ng × h/mL	30 mg single, oral	PF-04937319 plasma	Homo sapiens
1456 ng × h/mL	50 mg single, oral	PF-04937319 plasma	Homo sapiens
2749 ng × h/mL	100 mg single, oral	PF-04937319 plasma	Homo sapiens
6034 ng × h/mL	300 mg single, oral	PF-04937319 plasma	Homo sapiens
458 ng × h/mL	10 mg 1 times / day steady-state, oral	PF-04937319 plasma	Homo sapiens
928.7 ng × h/mL	30 mg 1 times / day steady-state, oral	PF-04937319 plasma	Homo sapiens
1889 ng × h/mL	50 mg 1 times / day steady-state, oral	PF-04937319 plasma	Homo sapiens
3167 ng × h/mL	100 mg 1 times / day steady-state, oral	PF-04937319 plasma	Homo sapiens
7446 ng × h/mL	300 mg 1 times / day steady-state, oral	PF-04937319 plasma	Homo sapiens

T_1/2

Value	Dose	Analyte	Population
6.563 h	10 mg 1 times / day steady-state, oral	PF-04937319 plasma	Homo sapiens
6.884 h	30 mg 1 times / day steady-state, oral	PF-04937319 plasma	Homo sapiens
6.348 h	50 mg 1 times / day steady-state, oral	PF-04937319 plasma	Homo sapiens
6.96 h	100 mg 1 times / day steady-state, oral	PF-04937319 plasma	Homo sapiens
8.479 h	300 mg 1 times / day steady-state, oral	PF-04937319 plasma	Homo sapiens

F_unbound

Value	Dose	Co-administered	Analyte	Population
31%	single, unknown		PF-04937319 plasma	Homo sapiens

Show entries

Name

Type

Language

PF-04937319

Preferred Name

English

Nerigliatin

Common Name

English

2-Pyrimidinecarboxamide, N,N-dimethyl-5-[[2-methyl-6-[[(5-methyl-2-pyrazinyl)amino]carbonyl]-4-benzofuranyl]oxy]-

Systematic Name

English

nerigliatin [INN]

Common Name

English

N,N-Dimethyl-5-[[2-methyl-6-[[(5-methyl-2-pyrazinyl)amino]carbonyl]-4-benzofuranyl]oxy]-2-pyrimidinecarboxamide

Systematic Name

English

Showing 1 to 5 of 5 entries

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Show entries

Code System

Code

Type

Description

DRUG BANK

DB15009

PRIMARY

EPA CompTox

DTXSID801336892

PRIMARY

PUBCHEM

46916694

PRIMARY

NCI_THESAURUS

C203200

PRIMARY

SMS_ID

300000041330

PRIMARY

Showing 1 to 5 of 8 entries

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SUBSTANCE RECORD


					7E99B9ZM19

Nerigliatin

SMILES

InChI

Approval Year

Targets

Cmax

AUC

T1/2

Funbound

C_max

T_1/2

F_unbound