2. Membrane Transporter/Ion Channel
  3. Sodium Channel
  4. PF 04531083

PF 04531083 is an orally active and selective NaV1.8 blocker with an IC50 of 0.7 μM. PF 04531083 is a blood-brain barrier (BBB) penetrant compound. PF 04531083 can be used for the research of respiratory system and neuropathic/inflammatory pain.

For research use only. We do not sell to patients.

PF 04531083

PF 04531083 Chemical Structure

CAS No. : 1079400-07-9

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Customer Review

Based on 1 publication(s) in Google Scholar

PF 04531083 Related Antibodies

Top Publications Citing Use of Products

View All Sodium Channel Isoform Specific Products:

View All Isoforms
Nav1.1 Nav1.2 Nav1.3 Nav1.4 Nav1.5 Nav1.6 Nav1.7 Nav1.8 Nav1.9

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

PF 04531083 is an orally active and selective NaV1.8 blocker with an IC50 of 0.7 μM. PF 04531083 is a blood-brain barrier (BBB) penetrant compound. PF 04531083 can be used for the research of respiratory system and neuropathic/inflammatory pain[1][2][3].

IC50 & Target[1]

Nav1.8

 

Cellular Effect
Cell Line Type Value Description References
HEK293 IC50
0.19 μM
Compound: 13
Inhibition of human Nav1.8/beta1 expressed in HEK293 cells by manual patch clamp electrophysiology
Inhibition of human Nav1.8/beta1 expressed in HEK293 cells by manual patch clamp electrophysiology
[PMID: 26101568]
HEK293 IC50
0.7 μM
Compound: 13
Inhibition of human Nav1.8 expressed in HEK293 cells assessed as reduction in blue fluorescent signal by VSP-FRET assay
Inhibition of human Nav1.8 expressed in HEK293 cells assessed as reduction in blue fluorescent signal by VSP-FRET assay
[PMID: 26101568]
HEK293 IC50
36 μM
Compound: 13
Inhibition of human Nav1.7 expressed in HEK293 cells by FRET assay
Inhibition of human Nav1.7 expressed in HEK293 cells by FRET assay
[PMID: 26101568]
HEK293 IC50
37 μM
Compound: 13
Inhibition of human Nav1.1 expressed in HEK293 cells by IonWorks Quattro selectivity assay
Inhibition of human Nav1.1 expressed in HEK293 cells by IonWorks Quattro selectivity assay
[PMID: 26101568]
HEK293 IC50
37 μM
Compound: 13
Inhibition of human Nav1.5 expressed in HEK293 cells by IonWorks Quattro selectivity assay
Inhibition of human Nav1.5 expressed in HEK293 cells by IonWorks Quattro selectivity assay
[PMID: 26101568]
In Vitro

PF 04531083 (1 μM) stimulates baseline activity by ~50% and the firing response to 10% CO2 in chemosensitive retrotrapezoid nucleus (RTN) neuron in a slice from a Tcf4tr/+ mice[3].
PF 04531083 blocks human Nav1.8, hNav1.1, hNav1.5, hNav1.7, TTX-r rat DRG, TTX-R hDRG, hERG with IC50 values of 0.19, 37, 37, 36, 0.54, 0.2, >30 μM, respectively[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

PF 04531083 Related Antibodies
Parmacokinetics
Species Dose SampleTime Route Indicator value Note
Rat 10 mg/kg i.p. T1/2 1.90 hr
Cynomolgus Monkey 30 mg/kg 1 day i.v. Clearance (CL) 876 μg/mL
Mice 30 mg/kg p.o. AUC 3879.5 ng·h/mL
Cynomolgus Monkey 10 mg/kg 1 day i.v. Clearance (CL) 369 μg/mL
Rat 500 mg/kg p.o. AUC 8050 ng·h/mL
Rat 200 mg/kg p.o. AUC 3580 ng·h/mL
Mice 1 mg/kg i.v. T1/2 2.42 hr
Rat 20 mg/kg p.o. T1/2 20.33 hr
Dog 25 mg/kg p.o. AUC 30500 ng·h/mL
Mice 5 mg/kg p.o. Bioavailability 45 %
Rat 0.8 mg/kg p.o. Clearance (CL) 1.2 L/h/kg
Rat 45 (female) mg/kg p.o. AUC 181,000 ng·h/mL
Rat 500 mg/kg p.o. AUC 8050 ng·h/mL
Mice 10 mg/kg i.g. AUC 0.136 μg·h/mL
Rat 45 (male) mg/kg p.o. AUC 99,600 ng·h/mL
Rat 10 mg/kg p.o. AUC 8061 ng·h/mL
Rat 1 mg/kg 24 h i.v. T1/2 14.38 hr
Mice 1 mg/kg i.v. Clearance (CL) 9.02 mL/min/kg
Mice 10 mg/kg p.o. AUC 1602 ng·h/mL
Rat 1 mg/kg 0.083, 0.25, 0.5, 1, 2, 4, 8, 12, 24 h i.v. AUC 7016 ng·h/mL
Rat 20 mg/kg 0.25, 0.5, 1, 2, 4, 8, 12, 24 p.o. AUC 2946 ng·h/mL
Rat 30 mg/kg i.g. Tmax 4 hr
Mice 1.92 mg/kg i.v. AUC 15,500 ng·h/mL
Rat 5 mg/kg i.p. AUC 9631 ng·h/mL
Pig 10 mg/kg p.o. Bioavailability 0.23 %
Rat 100 mg/kg 1 day i.v. AUC 170000 μg·h/mL Age: 6-8 weeks
Rat 1 mg/kg i.v. T1/2 3.4 hr
Rat 7 mg/kg 36 h i.v. AUC 4.09 μg·h/mL
Cynomolgus Monkey 100 mg/kg 1 day i.v. Clearance (CL) 2560 μg/mL
Mice 2 mg/kg 0.25, 0.5, 1, 2, 4, 8, 24 h i.v. T1/2 2.37 hr
Dog 50 mg/kg p.o. AUC 61800 ng·h/mL
Rat 2 mg/kg i.v. AUC 257 ng·h/mL
Mice 1 mg/kg i.v. Plasma Concentration 2090±229 ng/mL
Dog 45 mg/kg p.o. AUC 96,500 ng·h/mL
Rat 10 mg/kg p.o. T1/2 27 min
Rat 10 mg/kg p.o. Plasma Concentration 6.41 ng/mL
Rat 3 mg/kg 24 h p.o. T1/2 8.27 hr
Rat 2 mg/kg i.v. T1/2 2.2 hr SD Rats
Rat 0.4 mg/kg i.v. Clearance (CL) 0.4 L/h/kg
Mice 5 mg/kg p.o. Plasma Concentration 5880 ng/mL
Rat 10 mg/kg i.v. T1/2 2.47±0.14 hr
Mice 10 mg/kg p.o. Plasma Concentration 328 ng/mL
Dog 3 mg/kg p.o. Vd 2.50 L/kg
Rat 1 mg/kg i.v. T1/2 3.9 hr
Rat 2 mg/kg i.v. AUC 5743.547 mg·h/L
Dog 25 mg/kg p.o. AUC 30500 ng·h/mL
Mice 10 mg/kg p.o. Plasma Concentration 3543 ng/mL
Rat 7 mg/kg 36 h p.o. Clearance (CL) 0.54 μg/mL
Rat 10 mg/kg 1 day i.v. Clearance (CL) 213 μg/mL Age: 6-8 weeks
Rat 10 mg/kg i.g. T1/2 0.82 hr
Dog 50 mg/kg p.o. AUC 61800 ng·h/mL
Rat 1 mg/kg i.v. T1/2 5.82 hr
Mice 300 mg/kg p.o. AUC 8030 ng·h/mL
Mice 10 mg/kg i.v. T1/2 5.15 hr
Mice 1 mg/kg i.v. Clearance (CL) 11.6 mL/min/kg
Mice 20 mg/kg 1 h p.o. AUC 57916 ng·h/mL
Rat 200 mg/kg p.o. AUC 3580 ng·h/mL
Dog 300 mg/kg p.o. Tmax 1.5 hr
Mice 5 mg/kg 0.25, 0.5, 1, 2, 4, 8, 24 h p.o. T1/2 3.15 hr
Rat 1 mg/kg p.o. Tmax 0.31 hr
Rat 7 mg/kg 36 h i.v. T1/2 1.13 hr
Dog 600 mg/kg p.o. Tmax 1.5 hr
Dog 12.5 mg/kg p.o. AUC 15200 ng·h/mL
Rat 2.5 mg/kg i.v. Plasma Concentration 1140.35 μg/L
Mice 3 mg/kg 5 min, 15 min, 30 min, 1 h, 2 h, 4 h, 6 h, 8 h, 24 h p.o. AUC 1997 ng·h/mL
Dog 10 mg/kg p.o. T1/2 34.3 hr
Mice 3 mg/kg p.o. AUC 5.199 μg·h/mL
Rat 1.13 (female) mg/kg i.v. AUC 5,110 ng·h/mL
Rat 5 mg/kg i.v. Plasma Concentration 1393.22 μg/L
Rat 3 mg/kg 5 min, 15 min, 30 min, 1 h, 2 h, 4 h, 6 h, 8 h, 24 h p.o. Plasma Concentration 417 ng/mL
Rat 5 mg/kg p.o. Tmax 0.5 hr
Rat 5 mg/kg 0.25, 0.5, 1, 2, 4, 8 and 24 h p.o. T1/2 3.32 hr
Rat 20 mg/kg i.g. Plasma Concentration 64.64 μg/L
Mice 500 mg/kg p.o. AUC 12400 ng·h/mL
Cynomolgus Monkey 1 mg/kg 5 min, 15 min, 30 min, 1 h, 2 h, 4 h, 6 h, 8 h, 24 h i.v. Vd 8.1 L/kg
Mice 1 mg/kg 5 min, 15 min, 30 min, 1 h, 2 h, 4 h, 6 h, 8 h, 24 h i.v. Clearance (CL) 19 mL/min/kg
Mice 10 mg/kg p.o. Bioavailability 78 %
Mice 30 mg/kg 0.5, 1, 2, 4, 8, 24 h o.a. Tmax 0.5 hr
Dog 1400 mg/kg p.o. Plasma Concentration 130 μg/mL
Dog 10 mg/kg i.v. T1/2 18 min
Mice 1 mg/kg i.v. Plasma Concentration 11700 ng/mL
Dog 1 mg/kg i.v. Plasma Concentration 7.0 μg/mL
Rat 2 mg/kg p.o. T1/2 N.D.
Rat 10 mg/kg i.g. T1/2 7.59 hr
Mice 100 mg/kg p.o. Tmax 4 hr
Dog 1 mg/kg i.v. AUC 6,230 ng·h/mL
Mice 10 mg/kg p.o. AUC 4929 ng·h/mL
Rat 10 mg/kg 1 day i.v. AUC 16200 μg·h/mL Age: 6-8 weeks
Rat 30 mg/kg 1 day i.v. AUC 51100 μg·h/mL Age: 6-8 weeks
Rat 1 mg/kg 5 min, 15 min, 30 min, 1 h, 2 h, 4 h, 6 h, 8 h, 24 h i.v. Vd 2.9 mL/min/kg
Mice 5 mg/kg i.v. T1/2 13 min
Mice 500 mg/kg p.o. AUC 12400 ng·h/mL
Cynomolgus Monkey 84 mg/kg p.o. AUC 90900 ng·h/mL
Rat 5 mg/kg p.o. Clearance (CL) 34.7 mL/min/kg
Mice 30 mg/kg i.p. Plasma Concentration 342.5 ng/mL
Mice 100 mg/kg p.o. T1/2 3.74 hr
Mice 1 mg/kg i.v. Clearance (CL) 43.7 mL/min/kg
Rat 30 mg/kg i.v. T1/2 2.49±0.07 hr
Mice 10 mg/kg p.o. T1/2 2.08 hr
Cynomolgus Monkey 84 mg/kg p.o. AUC 90900 ng·h/mL
Rat 10 mg/kg p.o. T1/2 2.41 hr
Dog 100 mg/kg p.o. Tmax 1.5 hr
Rat 1.13 (male) mg/kg i.v. AUC 2,630 ng·h/mL
Rat 1 mg/kg i.v. Plasma Concentration 410.82 ng/mL
Mice 1 mg/kg i.v. Clearance (CL) 0.82 (9.9) L/h/kg
Mice 300 mg/kg p.o. AUC 8030 ng·h/mL
Rat 100 mg/kg p.o. AUC 2000 ng·h/mL
Rhesus monkey 2, 10, 50 or repeat 50 mg/kg i.v. Plasma Concentration 1 mg/mL 1 h infusion
Rat 5 mg/kg p.o. T1/2 5.5 hr
Mice 1 mg/kg i.v. Plasma Concentration 264 ng/mL
Mice 2 mg/kg i.v. T1/2 3.21 hr
Dog 5 mg/kg 30 i.v. Vd 2.50 L/kg
Dog 1 mg/kg p.o. Tmax 1.0 hr
Rat 10 mg/kg p.o. T1/2 0.4 hr SD Rats
Mice 30 mg/kg i.v. AUC 7922.2 ng·h/mL
Rat 10 mg/kg i.v. Plasma Concentration 1662.94 μg/L
Rat 10 mg/kg i.v. T1/2 12.89 min
Rat 7 mg/kg 36 h i.p. T1/2 1.22 hr
Mice 10 mg/kg p.o. Plasma Concentration 1580±427 ng/mL
Dog 12.5 mg/kg p.o. AUC 15200 ng·h/mL
Mice 30 mg/kg 10 min p.o. Plasma Concentration 2802 ng/mL
Mice 1.6 mg/kg i.v. Clearance (CL) 7.3417 mL/min/kg
Rat 1 mg/kg i.v. AUC 4726 ng·h/mL
Cynomolgus Monkey 1.35 mg/kg i.v. AUC 2,100 ng·h/mL
Rat 10 mg/kg p.o. T1/2 8.28 hr
Rat 5 mg/kg 30 i.v. Clearance (CL) 34.7 mL/min/kg
Rat 1 mg/kg i.v. Tmax - hr
Rat 20 mg/kg p.o. AUC 52.21 ng·h/mL
Cynomolgus Monkey 3 mg/kg 5 min, 15 min, 30 min, 1 h, 2 h, 4 h, 6 h, 8 h, 24 h p.o. AUC 1289 ng·h/mL
Mice 1 mg/kg i.v. AUC 0.424 μg·h/mL
Mice 5 mg/kg 1 h i.v. AUC 14525 ng·h/mL
Mice 10 mg/kg p.o. Clearance (CL) 9.02 mL/min/kg
Rat 2 mg/kg i.v. T1/2 2.68 hr
Mice 45 mg/kg p.o. AUC 215,000 ng·h/mL
Dog 1400 mg/kg p.o. AUC 551 μg·h/mL
Rat 100 mg/kg p.o. AUC 2000 ng·h/mL
Rat 20 mg/kg p.o. Plasma Concentration 22.45 ng/mL
Rat 1 mg/kg i.v. Plasma Concentration 1953 ng/mL
Rat 10 mg/kg i.g. Tmax 4 hr
Mice 30 mg/kg p.o. AUC 14716 ng·h/mL
Rat 7 mg/kg 36 h p.o. Tmax 2.25 hr
Mice 500 mg/kg p.o. T1/2 1.90 hr
Dog 12.5 mg/kg p.o. T1/2 4.01 hr
Dog 10 mg/kg i.v. T1/2 104 min
Pig 10 mg/kg p.o. T1/2 1.7 hr
Rat 0.4 mg/kg i.v. Vd 2.2 L/kg
Rat 100 mg/kg p.o. T1/2 1.48 hr
Rat 1 mg/kg i.v. AUC 3869 ng·h/mL
Dog 3 mg/kg p.o. T1/2 1.92 hr
Rat 5 mg/kg 0.25, 0.5, 1, 2, 4, 8 and 24 h p.o. Tmax 2.67 hr
Rat 7 mg/kg 36 h i.v. AUC 4.09 μg·h/mL
Rat 1 mg/kg 0.083, 0.25, 0.5, 1, 2, 4, 8, 12, 24 h i.v. Clearance (CL) 142.5 mL/h/kg
Mice 100 mg/kg p.o. AUC 32178 ng·h/mL
Mice 10 mg/kg p.o. Tmax 6 hr
Cynomolgus Monkey 10 mg/kg 1 day i.v. Tmax 1 hr
Cynomolgus Monkey 100 mg/kg 1 day i.v. Tmax 1 hr
Dog 1 mg/kg i.v. T1/2 1.1 hr
Dog 1400 mg/kg p.o. Tmax 3 hr
Mice 10 mg/kg i.g. AUC 0.138 μg·h/mL
Rat 100 mg/kg p.o. T1/2 1.48 hr
Rat 1 mg/kg i.v. AUC 0.714 μg·h/mL
Rat 0.8 mg/kg p.o. Vd 3.2 L/kg
Rat 7 mg/kg 36 h p.o. Tmax 2.25 hr
Rat 100 mg/kg 1 day i.v. Clearance (CL) 2360 μg/mL Age: 6-8 weeks
Mice 1 mg/kg 5 min, 15 min, 30 min, 1 h, 2 h, 4 h, 6 h, 8 h, 24 h i.v. Vd 2.7 L/kg
Mice 1 mg/kg i.v. Plasma Concentration 2054.53 ng·h/mL
Rat 10 mg/kg p.o. AUC 7689 ng·h/mL
Mice 300 mg/kg p.o. T1/2 1.58 hr
Mice 1 mg/kg i.v. AUC 4229±742 ng·h/mL
Rat 2 mg/kg i.v. AUC 258 ng·h/mL
Rat 1 mg/kg i.v. Plasma Concentration 10.6 μg/mL
Rat 200 mg/kg p.o. T1/2 1.84 hr
Mice 10 mg/kg p.o. Vd 1.76 L/kg
Rat 1 mg/kg 24 h i.v. Plasma Concentration 106.16 ng/mL
Rat 20 mg/kg p.o. Tmax 0.33 hr
Mice 10 mg/kg p.o. T1/2 2.43 hr
Mice 5 mg/kg p.o. AUC 2744 ng·h/mL
Mice 300 mg/kg p.o. T1/2 1.58 hr
Rat 5 mg/kg p.o. Tmax 1.2 hr
Rat 2 mg/kg i.v. AUC 5747.104 mg·h/L
Rat 10 mg/kg i.v. MRT 3.65±0.30 hr
Rat 10 mg/kg p.o. Bioavailability 0.9 %
Rat 30 mg/kg i.v. MRT 3.86±0.06 hr
Mice 5 mg/kg 1 h i.v. T1/2 3.63 hr
Rat 45 (male) mg/kg p.o. Plasma Concentration 12,000 ng/mL
Rat 45 (female) mg/kg p.o. Plasma Concentration 15,600 ng/mL
Rat 5 mg/kg i.p. Plasma Concentration 1966 ng/mL
Dog 600 mg/kg p.o. Plasma Concentration 123 μg/mL
Rat 7 mg/kg 36 h p.o. T1/2 1.04 hr
Rat 10 mg/kg i.p. Tmax 0.85 hr
Rat 10 mg/kg p.o. Tmax 0.42 hr
Mice 1 mg/kg i.v. Vd 0.843 L/kg
Mice 5 mg/kg p.o. Tmax 1 hr
Rat 2 mg/kg i.v. Tmax 0.1 hr SD Rats
Cynomolgus Monkey 30 mg/kg 1 day i.v. Tmax 1 hr
Rat 30 mg/kg i.g. Plasma Concentration 1521.25±100.76 ng/mL
Rat 500 mg/kg p.o. T1/2 2.03 hr
Mice 1 mg/kg i.v. AUC 349.3 ng·h/mL
Dog 12.5 mg/kg p.o. T1/2 4.01 hr
Mice 5 mg/kg 0.25, 0.5, 1, 2, 4, 8, 24 h p.o. Tmax 0.42 hr
Mice 1 mg/kg i.v. Tmax 0.083 hr
Dog 25 mg/kg p.o. T1/2 3.76 hr
Dog 50 mg/kg p.o. T1/2 3.51 hr
Rat 5 mg/kg 30 i.v. Vd 2.1 L/kg
Mice 10 mg/kg p.o. AUC 14146±5297 ng·h/mL
Cynomolgus Monkey 1 mg/kg 5 min, 15 min, 30 min, 1 h, 2 h, 4 h, 6 h, 8 h, 24 h i.v. Clearance (CL) 19 mL/min/kg
Mice 1 mg/kg i.v. AUC 8160 ng·h/mL
Dog 50 mg/kg p.o. T1/2 3.51 hr
Rat 5 mg/kg i.v. AUC 0.76 mg·h/L
Cynomolgus Monkey 84 mg/kg p.o. T1/2 4.84 hr
Mice 45 mg/kg p.o. Plasma Concentration 26,300 ng/mL
Rat 7 mg/kg 36 h i.v. Clearance (CL) 1.77 L/h/kg
Mice 1.92 mg/kg i.v. Clearance (CL) 2.1 mL/min/kg
Mice 1 mg/kg i.v. Vd 1.9 L/kg
Rat 1 mg/kg i.v. AUC 8.35 μg·h/mL
Rat 1.13 (male) mg/kg i.v. Clearance (CL) 7.7 mL/min/kg
Rat 2 mg/kg p.o. Tmax 1.3 hr
Mice 30 mg/kg p.o. AUC 3854.7 ng·h/mL
Dog 25 mg/kg p.o. T1/2 3.76 hr
Mice 1.6 mg/kg i.v. T1/2 6.65 hr
Rat 2.5 mg/kg i.v. AUC 0.48 mg·h/L
Rat 500 mg/kg p.o. T1/2 2.03 hr
Rat 7 mg/kg 36 h i.p. AUC 3.38 μg·h/mL
Rat 10 mg/kg i.g. Plasma Concentration 587.67±12.66 ng/mL
Rat 30 mg/kg 1 day i.v. Clearance (CL) 695 μg/mL Age: 6-8 weeks
Mice 30 mg/kg i.v. AUC 7905.7 ng·h/mL
Rat 10 mg/kg i.g. Tmax 5.53 hr
Cynomolgus Monkey 84 mg/kg p.o. T1/2 4.84 hr
Rat 5 mg/kg p.o. Plasma Concentration 15.6 μg/mL
Rat 3 mg/kg 5 min, 15 min, 30 min, 1 h, 2 h, 4 h, 6 h, 8 h, 24 h p.o. AUC 2765 ng·h/mL
Mice 10 mg/kg p.o. Plasma Concentration 3677.25 ng/mL
Mice 1 mg/kg i.v. Vd 1.76 L/kg
Mice 2 mg/kg i.v. MRT 3.50 hr
Dog 600 mg/kg p.o. AUC 507 μg·h/mL
Rat 20 mg/kg i.g. Tmax 3.38 hr
Rat 10 mg/kg p.o. Plasma Concentration 173 ng/mL
Rat 10 mg/kg p.o. AUC 0.319 μg·h/mL
Dog 1 mg/kg p.o. Plasma Concentration 4.0 μg/mL
Dog 45 mg/kg p.o. Plasma Concentration 3,630 ng/mL
Rat 10 mg/kg i.v. T1/2 46.80 min
Rat 10 mg/kg i.g. Tmax 0.5 hr
Rat 10 mg/kg p.o. Plasma Concentration 1366.5 ng/mL SD Rats
Dog 300 mg/kg p.o. Plasma Concentration 101 μg/mL
Mice 10 mg/kg p.o. AUC 20320 ng·h/mL
Rat 1 mg/kg p.o. Plasma Concentration 3.99 ng/mL
Mice 10 mg/kg i.v. Clearance (CL) 480.8 mL/h/kg
Rat 1 mg/kg i.v. Tmax 0.083 hr
Rat 20 mg/kg p.o. AUC 55.68 ng·h/mL
Rat 1 mg/kg i.v. Tmax -
Mice 30 mg/kg 0.5, 1, 2, 4, 8, 24 h o.a. Plasma Concentration 1093.2 μg/mL
Dog 100 mg/kg p.o. AUC 171 μg·h/mL
Cynomolgus Monkey 3 mg/kg 5 min, 15 min, 30 min, 1 h, 2 h, 4 h, 6 h, 8 h, 24 h p.o. Plasma Concentration 111 ng/mL
Dog 10 mg/kg p.o. Plasma Concentration 868 ng/mL
Rat 20 mg/kg p.o. Tmax 0.5 hr
Rat 1 mg/kg 5 min, 15 min, 30 min, 1 h, 2 h, 4 h, 6 h, 8 h, 24 h i.v. Clearance (CL) 20 mL/min/kg
Dog 100 mg/kg p.o. Plasma Concentration 49.1 μg/mL
Cynomolgus Monkey 1.35 mg/kg i.v. Clearance (CL) 11 mL/min/kg
Mice 20 mg/kg 1 h p.o. Bioavailability 99.6 %
Mice 500 mg/kg p.o. T1/2 1.9 hr
Mice 10 mg/kg p.o. T1/2 0.77 hr
Mice 2 mg/kg 0.25, 0.5, 1, 2, 4, 8, 24 h i.v. AUC 437 ng·h/mL
Rat 1 mg/kg 0.083, 0.25, 0.5, 1, 2, 4, 8, 12, 24 h i.v. T1/2 4.3 hr
Dog 5 mg/kg 30 i.v. T1/2 1.92 hr
Mice 100 mg/kg p.o. Tmax 4.00 hr
Rat 2 mg/kg i.v. Tmax 0.75 hr
Rat 1.13 (female) mg/kg i.v. Clearance (CL) 3.7 mL/min/kg
Rat 20 mg/kg 0.25, 0.5, 1, 2, 4, 8, 12, 24 p.o. Plasma Concentration 160 ng/mL
Mice 10 mg/kg p.o. Tmax 0.75 hr
Rat 10 mg/kg i.v. AUC 1.28 mg·h/L
Dog 1 mg/kg i.v. Clearance (CL) 3 mL/min/kg
Rhesus monkey 2, 10, 50 or repeat 50 mg/kg i.v. T1/2 326.4 hr 1 h infusion
Rat 3 mg/kg 24 h p.o. Tmax 0.5 hr
Rat 200 mg/kg p.o. T1/2 1.84 hr
Mice 30 mg/kg i.p. AUC 1022 ng·h/mL
Rat 5 mg/kg p.o. Vd 2.1 L/kg
Mice 3 mg/kg p.o. AUC 5.138 μg·h/mL
Mice 1 mg/kg i.v. AUC 0.431 μg·h/mL
Mice 30 mg/kg p.o. Tmax 3 hr
Dog 300 mg/kg p.o. AUC 388 μg·h/mL
Mice 3 mg/kg 5 min, 15 min, 30 min, 1 h, 2 h, 4 h, 6 h, 8 h, 24 h p.o. T1/2 3.8 hr
Rat 1 mg/kg i.v. Tmax 0.033 hr
Rat 1 mg/kg i.v. T1/2 1.91 hr
Rat 45 (female) mg/kg p.o. Bioavailability 89%
Rat 500 mg/kg p.o. Plasma Concentration 6460 ng/mL
Rat 20 mg/kg 0.25, 0.5, 1, 2, 4, 8, 12, 24 p.o. Bioavailability 2.1 %
Rat 10 mg/kg i.v. AUC 1.29 mg·h/L
Mice 30 mg/kg i.v. Plasma Concentration 19300 ng/mL
Rat 1 mg/kg i.v. T1/2 2.8 hr
Mice 500 mg/kg p.o. Plasma Concentration 10600 ng/mL
Rat 10 mg/kg p.o. Plasma Concentration 1296 ng/mL
Rat 7 mg/kg 36 h i.v. Clearance (CL) 1.77 L/h/kg
Rat 2.5 mg/kg i.v. AUC 0.48 mg·h/L
Rat 3 mg/kg 5 min, 15 min, 30 min, 1 h, 2 h, 4 h, 6 h, 8 h, 24 h p.o. T1/2 2.6 hr
Rat 7 mg/kg 36 h i.v. Clearance (CL) 2.23 L/kg
Rat 1 mg/kg i.v. Clearance (CL) 6.7 mL/min/kg
Dog 10 mg/kg i.v. Vd 3.17 L/kg
Mice 45 mg/kg p.o. Bioavailability 59%
Mice 10 mg/kg p.o. T1/2 1.2 hr
Dog 12.5 mg/kg p.o. Plasma Concentration 3600 ng/mL
Cynomolgus Monkey 84 mg/kg p.o. Plasma Concentration 18800 ng/mL
Rat 2 mg/kg i.v. Plasma Concentration 53.13 ng/mL
Rat 2 mg/kg i.v. Plasma Concentration 894 ng/mL SD Rats
Cynomolgus Monkey 30 mg/kg 1 day i.v. AUC 77200 μg·h/mL
Mice 20 mg/kg 1 h p.o. T1/2 2.70 hr
Rat 2 mg/kg p.o. Clearance (CL) 11.4 mL/min/kg
Mice 300 mg/kg p.o. Plasma Concentration 7290 ng/mL
Dog 3 mg/kg p.o. Bioavailability 51.3 %
Rat 1 mg/kg p.o. T1/2 9.49 hr
Rat 5 mg/kg i.p. Clearance (CL) 524.9 mL/h/kg
Rat 10 mg/kg p.o. AUC 771 ng·h/mL SD Rats
Rat 3 mg/kg 24 h p.o. Plasma Concentration 37.94 ng/mL
Mice 30 mg/kg i.p. T1/2 3.24 hr
Rat 10 mg/kg i.g. T1/2 2.53±0.12 hr
Mice 1 mg/kg i.v. AUC 8620 ng·h/mL
Rat 10 mg/kg i.v. AUC 34,263.98±1100.87 ng/L.h
Mice 3 mg/kg p.o. T1/2 3.63 hr
Mice 5 mg/kg p.o. Plasma Concentration 1570 ng/mL
Rat 5 mg/kg i.v. AUC 0.77 mg·h/L
Mice 1.92 mg/kg i.v. Vd 0.34 L/kg
Rat 5 mg/kg 0.25, 0.5, 1, 2, 4, 8 and 24 h p.o. Plasma Concentration 256.40 ng/mL
Rat 200 mg/kg p.o. Plasma Concentration 2650 ng/mL
Rat 5 mg/kg p.o. T1/2 2.31 hr
Dog 10 mg/kg p.o. AUC 15420 ng·h/mL
Rat 10 mg/kg 1 day i.v. Tmax 1.0 hr Age: 6-8 weeks
Mice 1 mg/kg i.v. T1/2 1.6 hr
Rat 5 mg/kg p.o. T1/2 23.4 hr
Cynomolgus Monkey 10 mg/kg 1 day i.v. AUC 30400 μg·h/mL
Rat 10 mg/kg i.p. Plasma Concentration 5205 ng/mL
Rat 30 mg/kg i.v. AUC 107,689.72±6779.70 ng/L.h
Rat 100 mg/kg p.o. Plasma Concentration 1200 ng/mL
Rat 200 mg/kg p.o. Plasma Concentration 2650 ng/mL
Mice 1 mg/kg i.v. T1/2 2.47 hr
Rat 10 mg/kg i.g. Plasma Concentration 726 ng/mL
Rat 1 mg/kg 24 h i.v. AUC 121.54 ng·h/mL
Mice 30 mg/kg 0.5, 1, 2, 4, 8, 24 h o.a. T1/2 7.5 hr
Mice 300 mg/kg p.o. Plasma Concentration 7290 ng/mL
Rat 30 mg/kg 1 day i.v. Tmax 1 hr Age: 6-8 weeks
Mice 100 mg/kg p.o. Plasma Concentration 15.17 ng/mL
Rat 20 mg/kg p.o. MRT 7.60 hr
Dog 12.5 mg/kg p.o. Plasma Concentration 3600 ng/mL
Rat 20 mg/kg i.g. AUC 0.28 mg·h/L
Mice 3 mg/kg 5 min, 15 min, 30 min, 1 h, 2 h, 4 h, 6 h, 8 h, 24 h p.o. Plasma Concentration 600 ng/mL
Dog 5 mg/kg 30 i.v. Bioavailability 51.3 %
Dog 1 mg/kg i.v. AUC 10.6 μg·h/mL
Mice 5 mg/kg p.o. AUC 35700 ng·h/mL
Pig 10 mg/kg p.o. T1/2 2.83 hr
Rat 5 mg/kg p.o. Plasma Concentration 356 ng/mL
Mice 2 mg/kg i.v. Vd 1.02 L/kg
Dog 1 mg/kg p.o. T1/2 1.4 hr
Cynomolgus Monkey 1.35 mg/kg i.v. Vd 1.6 L/kg
Mice 10 mg/kg p.o. AUC 14173±5307 ng·h/mL
Rat 30 mg/kg i.g. T1/2 2.57±0.09 hr
Mice 500 mg/kg p.o. Plasma Concentration 10600 ng/mL
Rat 7 mg/kg 36 h p.o. T1/2 1.04 hr
Rat 5 mg/kg 30 i.v. T1/2 2.31 hr
Rat 0.8 mg/kg p.o. T1/2 3.1 hr
Rat 1 mg/kg i.v. AUC 0.780 μg·h/mL
Rat 10 mg/kg p.o. T1/2 2.10 hr
Rat 100 mg/kg 1 day i.v. Tmax 1 hr Age: 6-8 weeks
Cynomolgus Monkey 3 mg/kg 5 min, 15 min, 30 min, 1 h, 2 h, 4 h, 6 h, 8 h, 24 h p.o. Bioavailability 50 %
Mice 10 mg/kg p.o. T1/2 2.73 hr
Cynomolgus Monkey 100 mg/kg 1 day i.v. AUC 240000 μg·h/mL
Mice 10 mg/kg i.g. MRT 5.76 hr
Rat 10 mg/kg i.g. Plasma Concentration 1900 ng/mL
Mice 1.6 mg/kg i.v. Plasma Concentration 3486.7 ng/mL
Rat 100 mg/kg p.o. Plasma Concentration 1200 ng/mL
Mice 10 mg/kg p.o. MRT 5.23 hr
Dog 45 mg/kg p.o. Bioavailability 34%
Mice 1 mg/kg i.v. T1/2 0.59 hr
Rat 45 (male) mg/kg p.o. Bioavailability 95%
Mice 1 mg/kg i.v. MRT 1.22 hr
Rat 1 mg/kg i.v. AUC 0.1674 μg·h/mL
Rat 1.13 (male) mg/kg i.v. Vd 0.34 L/kg
Mice 1 mg/kg i.v. AUC 3135.27 ng·h/mL
Mice 1 mg/kg i.v. AUC 4245±745 ng·h/mL
Rat 10 mg/kg i.v. Vd 1.62 L/kg
Mice 10 mg/kg p.o. AUC 19689.35 ng·h/mL
Cynomolgus Monkey 84 mg/kg p.o. Plasma Concentration 18800 ng/mL
Dog 25 mg/kg p.o. Plasma Concentration 7080 ng/mL
Mice 2 mg/kg 0.25, 0.5, 1, 2, 4, 8, 24 h i.v. MRT 0.4 hr
Mice 1 mg/kg i.v. MRT 1.90 hr
Rat 1.13 (female) mg/kg i.v. Vd 1 L/kg
Rat 2 mg/kg i.v. MRT 1.74 hr
Mice 10 mg/kg i.v. Vd 3.56 L/kg
Mice 10 mg/kg p.o. T1/2 2.47 hr
Mice 1 mg/kg i.v. Vd 0.90 L/kg
Rat 0.4 mg/kg i.v. T1/2 6.2 hr
Mice 5 mg/kg 0.25, 0.5, 1, 2, 4, 8, 24 h p.o. Plasma Concentration 137 ng·h/mL
Mice 10 mg/kg p.o. Plasma Concentration 1923.7 ng/mL
Dog 50 mg/kg p.o. Plasma Concentration 13200 ng/mL
Dog 25 mg/kg p.o. Plasma Concentration 7080 ng/mL
Rat 7 mg/kg 36 h p.o. Plasma Concentration 0.54 μg/mL
Rat 20 mg/kg p.o. AUC 0.0246 μg·h/mL
Rat 20 mg/kg p.o. Plasma Concentration 29.7 ng/mL
Rat 10 mg/kg p.o. AUC 3212 ng·h/mL
Rat 1 mg/kg i.v. Plasma Concentration 1050 ng/mL
Rat 500 mg/kg p.o. Plasma Concentration 6460 ng/mL
Mice 30 mg/kg p.o. Plasma Concentration 4840 ng/mL
Rat 2 mg/kg i.v. MRT 0.804 hr
Dog 1 mg/kg i.v. Vd 2.3 L/kg
Dog 50 mg/kg p.o. Plasma Concentration 13200 ng/mL
Rat 1 mg/kg i.v. AUC 16.2 μg·h/mL
Rat 5 mg/kg p.o. AUC 59.2 μg·h/mL
Rat 20 mg/kg p.o. MRT 11.67 hr
Rat 10 mg/kg i.v. MRT 0.80 hr
Rat 7 mg/kg 36 h p.o. AUC 1.70 μg·h/mL
Mice 3 mg/kg p.o. Plasma Concentration 1085.0 ng/mL
Mice 300 mg/kg p.o. Tmax 0.25 hr
Dog 3 mg/kg p.o. Clearance (CL) 23.7 mL/min/kg
Rat 5 mg/kg 0.25, 0.5, 1, 2, 4, 8 and 24 h p.o. AUC 1377.38 ng·h/mL
Mice 500 mg/kg p.o. Tmax 0.25 hr
Mice 2 mg/kg i.v. Clearance (CL) 4.80 mL/min/kg
Rat 5 mg/kg p.o. Bioavailability 49.8 %
Rat 100 mg/kg p.o. Tmax 0.17 hr
Pig 10 mg/kg p.o. Clearance (CL) 1.27 kg·h/L
Rat 200 mg/kg p.o. Tmax 0.083 hr
Rat 7 mg/kg 36 h p.o. AUC 3.38 μg·h/mL
Mice 30 mg/kg i.v. Clearance (CL) 63.11 mL/min/kg
Mice 10 mg/kg p.o. Tmax 0.3 hr
Mice 3 mg/kg 5 min, 15 min, 30 min, 1 h, 2 h, 4 h, 6 h, 8 h, 24 h p.o. Bioavailability 76 %
Rat 5 mg/kg 30 i.v. Bioavailability 49.8 %
Rat 20 mg/kg p.o. AUC 0.9504 μg·h/mL
Rat 10 mg/kg p.o. AUC 8.22 ng·h/mL
Mice 1.92 mg/kg i.v. T1/2 2.6 hr
Dog 25 mg/kg p.o. Tmax 1.5 hr
Rat 100 mg/kg p.o. Tmax 0.17 hr
Rat 5 mg/kg i.v. MRT 0.72 hr
Rat 2 mg/kg i.v. T1/2 0.746 hr
Mice 1 mg/kg i.v. AUC 3138.30 ng·h/mL
Rat 2.5 mg/kg i.v. MRT 0.62 hr
Mice 2 mg/kg 0.25, 0.5, 1, 2, 4, 8, 24 h i.v. Clearance (CL) 79.8 mL/min/kg
Mice 10 mg/kg p.o. MRT 4.34 hr
Rat 0.8 mg/kg p.o. AUC 1.0 kg·h/L
Rat 10 mg/kg i.g. MRT 4.57±0.09 hr
Rat 10 mg/kg p.o. Bioavailability 5.13 %
Mice 1.6 mg/kg i.v. AUC 3.6375 μg·h/mL
Mice 300 mg/kg p.o. Tmax 0.25 hr
Mice 1 mg/kg i.v. AUC 181 ng·h/mL
Mice 5 mg/kg 0.25, 0.5, 1, 2, 4, 8, 24 h p.o. MRT 2.32 hr
Rat 20 mg/kg p.o. AUC 0.0214 μg·h/mL
Rat 7 mg/kg 36 h i.v. T1/2 1.13 hr
Rat 500 mg/kg p.o. Tmax 0.083 hr
Rat 10 mg/kg i.g. MRT 1.65 hr
Rat 20 mg/kg 0.25, 0.5, 1, 2, 4, 8, 12, 24 p.o. T1/2 7.1 hr
Dog 5 mg/kg 30 i.v. Clearance (CL) 23.7 mL/min/kg
Rat 1 mg/kg i.v. Vd 2.25 L/kg
Mice 10 mg/kg p.o. Bioavailability 99.0 %
Mice 100 mg/kg p.o. Vd 4.97 L/kg
Dog 12.5 mg/kg p.o. Tmax 2.0 hr
Mice 1 mg/kg i.v. T1/2 3.55±0.17 hr
Rat 2 mg/kg i.v. MRT 1.95 hr
Cynomolgus Monkey 1.35 mg/kg i.v. T1/2 2.2 hr
Rat 1 mg/kg 24 h i.v. AUC 153.12 ng·h/mL
Rat 2 mg/kg i.v. AUC 0.1042 μg·h/mL
Rat 1.13 (female) mg/kg i.v. T1/2 3.9 hr
Rat 10 mg/kg i.g. AUC 29.3 μg·h/mL
Mice 10 mg/kg p.o. AUC 19702.46 ng·h/mL
Cynomolgus Monkey 3 mg/kg 5 min, 15 min, 30 min, 1 h, 2 h, 4 h, 6 h, 8 h, 24 h p.o. T1/2 10 hr
Rat 10 mg/kg i.v. Clearance (CL) 32.26 mL/min/kg
Mice 10 mg/kg p.o. T1/2 2.51±0.06 hr
Mice 10 mg/kg p.o. AUC 820 ng·h/mL
Rat 10 mg/kg p.o. MRT 0.5 hr SD Rats
Rat 10 mg/kg i.v. AUC 34,341.50±908.33 ng/L.h
Mice 10 mg/kg p.o. Plasma Concentration 4697 ng/mL
Dog 1 mg/kg p.o. AUC 11.6 μg·h/mL
Mice 30 mg/kg i.p. AUC 1326 ng·h/mL
Rat 1.13 (male) mg/kg i.v. T1/2 2.3 hr
Mice 1 mg/kg i.v. AUC 1482 ng·h/mL
Rat 1 mg/kg i.v. AUC 0.1652 μg·h/mL
Rat 200 mg/kg p.o. Tmax 0.083 hr
Cynomolgus Monkey 84 mg/kg p.o. Tmax 2.7 hr
Rat 3 mg/kg 5 min, 15 min, 30 min, 1 h, 2 h, 4 h, 6 h, 8 h, 24 h p.o. Bioavailability 118 %
Mice 10 mg/kg i.v. AUC 20800 ng·h/mL
Dog 12.5 mg/kg p.o. Tmax 2.0 hr
Mice 1 mg/kg i.v. T1/2 0.26 hr
Mice 30 mg/kg p.o. Clearance (CL) 123.9 mL/min/kg
Rat 10 mg/kg i.p. AUC 12.099 ng·h/mL
Mice 30 mg/kg 0.5, 1, 2, 4, 8, 24 h o.a. AUC 3088.3 ng·h/mL
Rat 1 mg/kg i.v. AUC 358 ng·h/mL
Mice 5 mg/kg p.o. AUC 37200 ng·h/mL
Rat 10 mg/kg p.o. T1/2 3.47 hr
Rat 5 mg/kg p.o. AUC 1.683 μg·h/mL
Rat 3 mg/kg 24 h p.o. AUC 141.01 ng·h/mL
Rat 2 mg/kg i.v. AUC 1028.2 ng·h/mL SD Rats
Mice 1 mg/kg i.v. T1/2 3.21 hr
Rat 30 mg/kg i.v. AUC 108,414.07±5853.89 ng/L.h
Dog 10 mg/kg p.o. Bioavailability 33.9 %
Cynomolgus Monkey 84 mg/kg p.o. Tmax 2.7 hr
Mice 5 mg/kg p.o. Tmax 1.5 hr
Rat 20 mg/kg i.g. AUC 0.32 mg·h/L
Rat 2 mg/kg p.o. Vd -
Mice 20 mg/kg 1 h p.o. Tmax 0.33 hr
Rat 30 mg/kg i.g. MRT 5.37±0.32 hr
Mice 10 mg/kg i.g. T1/2 3.84 hr
Dog 1 mg/kg i.v. Clearance (CL) 1.8 mL/min/kg
Mice 1 mg/kg i.v. Bioavailability 99.0 %
Rat 1 mg/kg i.v. T1/2 5.45 hr
Rat 0.4 mg/kg i.v. AUC 3.1 kg·h/L
Dog 50 mg/kg p.o. Tmax 2.0 hr
Rat 7 mg/kg 36 h i.v. Vd 2.23 L/kg
Mice 1 mg/kg i.v. T1/2 1.50 hr
Rat 500 mg/kg p.o. Tmax 0.083 hr
Dog 25 mg/kg p.o. Tmax 1.5 hr
Rat 5 mg/kg i.p. T1/2 5.2 hr
Mice 500 mg/kg p.o. Tmax 0.25 hr
Dog 1 mg/kg i.v. T1/2 15 hr
Dog 50 mg/kg p.o. Tmax 2.0 hr
Rat 10 mg/kg p.o. Tmax 1.50 hr
Rat 5 mg/kg 0.25, 0.5, 1, 2, 4, 8 and 24 h p.o. Bioavailability 54.25 %
Rat 10 mg/kg p.o. Clearance (CL) 2.5 L/h/kg SD Rats
Rat 20 mg/kg 0.25, 0.5, 1, 2, 4, 8, 12, 24 p.o. Tmax 1.4 hr
Mice 2 mg/kg 0.25, 0.5, 1, 2, 4, 8, 24 h i.v. Vd 1.802 L/kg
Mice 5 mg/kg p.o. T1/2 5.63 hr
Rat 500 mg/kg p.o. Bioavailability 2.36 %
Dog 12.5 mg/kg p.o. Bioavailability 83.1 %
Rat 1 mg/kg i.v. Tmax 0.17 hr
Rat 20 mg/kg p.o. AUC 0.2884 μg·h/mL
Mice 30 mg/kg i.v. MRT 0.4 hr
Mice 3 mg/kg p.o. Tmax 0.670 hr
Mice 1 mg/kg i.v. Bioavailability 32.08 %
Mice 1 mg/kg i.v. MRT 1.83 hr
Rat 10 mg/kg i.p. MRT 1.71 hr
Rat 1 mg/kg i.v. MRT 0.70 hr
Rat 1 mg/kg i.v. Bioavailability -
Mice 30 mg/kg p.o. MRT 1.2 hr
Mice 10 mg/kg p.o. AUC 825 ng·h/mL
Rat 2 mg/kg p.o. Bioavailability 59 %
Dog 1 mg/kg p.o. Bioavailability 100 %
Mice 10 mg/kg p.o. Bioavailability 45.8 %
Rat 30 mg/kg i.g. AUC 11,273.22±703.84 ng/L.h
Mice 300 mg/kg p.o. Bioavailability 5.06 %
Rat 100 mg/kg p.o. Bioavailability 2.94 %
Dog 25 mg/kg p.o. Bioavailability 83.5 %
Mice 1.6 mg/kg i.v. AUC 3.5712 μg·h/mL
Mice 2 mg/kg i.v. Plasma Concentration 4642 ng/mL
Rat 2 mg/kg i.v. T1/2 3.86 hr
Rat 2 mg/kg i.v. MRT 1.7 hr SD Rats
Rat 500 mg/kg p.o. Bioavailability 2.36 %
Rat 200 mg/kg p.o. Bioavailability 2.62 %
Rat 200 mg/kg p.o. Bioavailability 2.62 %
Mice 1 mg/kg i.v. Vd 0.536 L/kg
Rat 2 mg/kg i.v. Clearance (CL) 0.354 L/h/kg
Rat 10 mg/kg i.g. Clearance (CL) 116 mL/min/kg
Rat 10 mg/kg i.g. AUC 3201.38±82.07 ng/L.h
Mice 500 mg/kg p.o. Bioavailability 4.69 %
Mice 100 mg/kg p.o. Clearance (CL) 0.92 L/h/kg
Mice 30 mg/kg i.p. Tmax 1.5 hr
Rat 20 mg/kg p.o. T1/2 1.27 hr
Rat 20 mg/kg i.g. MRT 5.86 hr
Mice 1 mg/kg i.v. Clearance (CL) 4.01±0.76 mL/min/kg
Dog 1 mg/kg i.v. Vd 0.2 L/kg
Dog 50 mg/kg p.o. Bioavailability 84.7 %
Rat 1 mg/kg 24 h i.v. MRT 13.39 hr
Mice 1 mg/kg i.v. Plasma Concentration 898.0 ng/mL
Rat 3 mg/kg 24 h p.o. AUC 157.95 ng·h/mL
Rat 0.4 mg/kg i.v. Plasma Concentration 0.23 mg/mL
Dog 50 mg/kg p.o. Bioavailability 84.7 %
Mice 10 mg/kg i.g. Tmax 1 hr
Rat 5 mg/kg i.p. Tmax 0.5 hr
Rat 0.8 mg/kg p.o. Plasma Concentration 0.09 mg/mL
Pig 10 mg/kg p.o. AUC 19.77 ng·h/mL
Mice 10 mg/kg p.o. Bioavailability 137 %
Rat 1 mg/kg i.v. T1/2 0.43 hr
Cynomolgus Monkey 84 mg/kg p.o. Bioavailability 48.3 %
Mice 1 mg/kg i.v. AUC 183 ng·h/mL
Mice 10 mg/kg p.o. MRT 3.71 hr
Mice 5 mg/kg 0.25, 0.5, 1, 2, 4, 8, 24 h p.o. Bioavailability 12.6 %
Mice 10 mg/kg p.o. AUC 29708 ng·h/mL
Rat 10 mg/kg p.o. MRT 0.81 hr
Mice 10 mg/kg p.o. Tmax 2 hr
Rat 1 mg/kg i.v. Clearance (CL) 1.0 mL/min/kg
Dog 25 mg/kg p.o. Bioavailability 83.5 %
Cynomolgus Monkey 84 mg/kg p.o. Bioavailability 48.3 %
Mice 1 mg/kg i.v. T1/2 1.45 hr
Rat 20 mg/kg p.o. T1/2 7.36 hr
Rat 5 mg/kg p.o. Clearance (CL) - mL/min/kg
Rat 2 mg/kg i.v. AUC 0.1053 μg·h/mL
Rat 100 mg/kg p.o. Bioavailability 2.94 %
Mice 500 mg/kg p.o. Bioavailability 4.69 %
Mice 300 mg/kg p.o. Bioavailability 5.06 %
Rat 5 mg/kg p.o. AUC 2.715 μg·h/mL
Dog 12.5 mg/kg p.o. Bioavailability 83.1 %
Rat 1 mg/kg i.v. Vd 0.2 L/kg
Rat 20 mg/kg p.o. MRT 4.42 hr
Mice 1 mg/kg i.v. Vd 0.66 L/kg
Rat 2 mg/kg i.v. Bioavailability 26.7 % SD Rats
Mice 1 mg/kg i.v. Clearance (CL) 1.99 mL/min/kg
Rat 2 mg/kg i.v. Tmax 0.083 hr
Mice 1 mg/kg i.v. Tmax 0.1 hr
Rat 10 mg/kg p.o. Vd 1.4 L/kg SD Rats
Rat 30 mg/kg i.g. AUC 11,328.84±574.48 ng/L.h
Rat 3 mg/kg 24 h p.o. MRT 8.78 hr
Rat 10 mg/kg p.o. Bioavailability 0.62 %
Mice 5 mg/kg p.o. Vd 1.12 L/kg
Mice 10 mg/kg p.o. MRT 2.0 hr
Rat 20 mg/kg p.o. Tmax 3.71 hr
Rat 20 mg/kg p.o. Bioavailability 0.65 %
Rat 5 mg/kg 0.25, 0.5, 1, 2, 4, 8 and 24 h p.o. Clearance (CL) 65.85 mL/min/kg
Rat 10 mg/kg i.p. Clearance (CL) 0.83 L/h/kg
Rat 1 mg/kg i.v. Clearance (CL) 99.79 mL/min/kg
Mice 10 mg/kg p.o. Bioavailability 62.80 %
Mice 30 mg/kg p.o. T1/2 1.00 hr
Rat 1 mg/kg i.v. Clearance (CL) 20 mL/min/kg
Mice 1 mg/kg i.v. Clearance (CL) 91 mL/min/kg
Rat 2 mg/kg i.v. MRT 1.66 hr
Mice 2 mg/kg i.v. AUC 7631 ng·h/mL
Rat 0.8 mg/kg p.o. Bioavailability 80 %
Mice 1.6 mg/kg i.v. Tmax 0.0833 hr
Mice 100 mg/kg p.o. AUC 0.11 ng·h/mL
Rat 0.4 mg/kg i.v. Bioavailability 76 %
Mice 30 mg/kg i.p. MRT 3.15 hr
Mice 30 mg/kg i.v. T1/2 1.97 hr
Pig 10 mg/kg p.o. Plasma Concentration 2.13 ng/mL
Rat 10 mg/kg i.g. AUC 3202.48±80.91 ng/L.h
Rat 20 mg/kg i.g. Bioavailability 10.26 %
Mice 10 mg/kg i.g. Plasma Concentration 159 ng/mL
Rat 1 mg/kg 24 h i.v. Bioavailability 100 %
Mice 10 mg/kg p.o. Bioavailability 33.4%
Rat 5 mg/kg p.o. Bioavailability 73.2 %
Rat 10 mg/kg i.g. Vd 8.29 L/kg
Mice 1 mg/kg i.v. MRT 0.66 hr
Rat 10 mg/kg i.g. AUC 1.442 μg·h/mL
Rat 1 mg/kg i.v. Bioavailability - %
Rat 20 mg/kg p.o. Clearance (CL) 429.44 L/h/kg
Rat 2 mg/kg i.v. MRT 190.8 hr
Mice 30 mg/kg p.o. Tmax 0.100 hr
Mice 5 mg/kg p.o. Clearance (CL) 2.27 mL/min/kg
Mice 30 mg/kg i.v. Tmax 0.083 hr
Rat 10 mg/kg i.g. Bioavailability 9.34±0.07 %
Rat 20 mg/kg p.o. MRT 27.77 hr
Mice 1 mg/kg i.v. MRT 2.32 hr
Mice 30 mg/kg i.p. MRT 5.34 hr
Mice 10 mg/kg p.o. Bioavailability 45 %
Pig 10 mg/kg p.o. Tmax 3.07 hr
Rat 30 mg/kg i.g. Bioavailability 10.47±0.10 %
Mice 100 mg/kg p.o. MRT 7.30 hr
Rat 2 mg/kg i.v. Clearance (CL) 6.80 L/h/kg
Rat 3 mg/kg 24 h p.o. Clearance (CL) 0.018993 mg·h/L
Mice 1 mg/kg i.v. Vd 0.0036 L/kg
Mice 30 mg/kg i.v. Brain-to-Plasma Ratio 0.23 (4h) %
Mice 5 mg/kg p.o. MRT 5.58 hr
Rat 20 mg/kg p.o. Clearance (CL) 123.87 L/h/kg
Rat 2 mg/kg i.v. Vz 38.01 L/kg
Mice 30 mg/kg p.o. Brain-to-Plasma Ratio 0.52 (4h) %
Pig 10 mg/kg p.o. MRT 6.53 hr
Rat 2 mg/kg i.v. Clearance (CL) 19.56 L/h/kg
Rat 3 mg/kg 24 h p.o. Bioavailability 34.4 %
Rat 20 mg/kg p.o. Vz 4480.43 L/kg
Rat 10 mg/kg i.g. AUC 1.449 μg·h/mL
Mice 30 mg/kg p.o. Brain-to-Plasma Ratio 0.58 (2h) %
Rat 2 mg/kg i.v. Plasma Concentration 318.2 ng/mL
Rat 10 mg/kg i.g. Bioavailability 26.3 %
Mice 5 mg/kg p.o. Bioavailability 87.6 %
Rat 20 mg/kg p.o. Plasma Concentration 8.37 ng/mL
Mice 30 mg/kg i.v. Brain-to-Plasma Ratio 0.56 (2h) %
Rat 2 mg/kg i.v. Bioavailability 27.38 %
Mice 30 mg/kg i.v. Vz 10.74 L/kg
Rat 20 mg/kg p.o. Bioavailability 2.15 %
Mice 30 mg/kg p.o. Bioavailability 49 %
Mice 30 mg/kg p.o. Vz 10.96 L/kg
Rat 20 mg/kg i.v. T1/2 0.65 hr pure
Rat 20 mg/kg i.v. Plasma Concentration 19.67 mg/L pure
Rat 20 mg/kg i.v. AUC 2.81 mg·h/L pure
Rat 20 mg/kg i.v. Vd 6.74 L/kg pure
Rat 20 mg/kg i.v. Clearance (CL) 7.20 L/h/kg pure
Rat 5.8 mg/kg i.v. T1/2 0.69 hr ext
Rat 5.8 mg/kg i.v. AUC 0.95 mg/h/L ext
Rat 5.8 mg/kg i.v. Vd 7.12 L/kg ext
Rat 5.8 mg/kg i.v. Clearance (CL) 9.17 L/h/kg ext
Rat 5.8 mg/kg i.v. Plasma Concentration 4.86 mg/L ext
Rat 50 mg/kg i.p. Tmax 0.04 hr
Rat 50 mg/kg i.p. Plasma Concentration 17.6 mg/L
Rat 50 mg/kg i.p. T1/2 0.67 hr
Rat 50 mg/kg i.p. AUC 5.29 mg/h/L
Rat 50 mg/kg i.p. Vd 9.98 L/kg
Rat 50 mg/kg i.p. Clearance (CL) 10.92 L/h/kg
Rat 50 mg/kg i.p. Bioavailability 75.3 %
In Vivo

PF 04531083 (1 mg/kg, i.v.; or 2 mg/kg, p.o.) is a low clearance compound with good bioavailability ∼60% in rats[2].
PF 04531083 (40 mg/kg; 1.5 h) is efficacious in the tibial nerve transection (TNT) induced mechanical allodynia model in rat[2].
PF 04531083 inhibits native tetrodotoxin-resistant (TTX-R) currents in rodent dorsal root ganglion (DRG) neurons with an IC50 of 0.54 μM[2].
PF 04531083 (40 mg/kg; 1.5 h) improves baseline breathing in Tcf4tr/+ mice[3].
PF 04531083 (30 min before test) improves behavioral abnormalities associated with Pitt-Hopkins syndrome (PTHS) in Tcf4tr/+ mice[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Tcf4+/+ and Tcf4tr/+ mice [3]
Dosage: 40 mg/kg
Administration: Intraperitoneal injection (i.p.), 1.5 h before test
Result: Decreased episodes of hyperventilation, increased the occurrence of spontaneous sighs, diminished duration of post-sigh apnea and improved the CO2 minute ventilatory response in Tcf4tr/+ mice.
Showed stable respiratory activity in Tcf4+/+ mice.
Showed a robust increase in respiratory activity (62.5% increase in minute ventilation from 3 to 7% CO2) in Tcf4tr/+ pups.
Clinical Trial
Molecular Weight

357.79

Formula

C17H16ClN5O2
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

ClC1=CC=C(OC)C=C1C2=C(N=C(NC(C3=CC=NN3C)=O)C=C2)N
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (279.49 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7949 mL 13.9747 mL 27.9494 mL
5 mM 0.5590 mL 2.7949 mL 5.5899 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (5.81 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.08 mg/mL (5.81 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 98.96%

SDS (392 KB)

COA (254 KB) HNMR (273 KB) LCMS (267 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.7949 mL 13.9747 mL 27.9494 mL 69.8734 mL
5 mM 0.5590 mL 2.7949 mL 5.5899 mL 13.9747 mL
10 mM 0.2795 mL 1.3975 mL 2.7949 mL 6.9873 mL
15 mM 0.1863 mL 0.9316 mL 1.8633 mL 4.6582 mL
20 mM 0.1397 mL 0.6987 mL 1.3975 mL 3.4937 mL
25 mM 0.1118 mL 0.5590 mL 1.1180 mL 2.7949 mL
30 mM 0.0932 mL 0.4658 mL 0.9316 mL 2.3291 mL
40 mM 0.0699 mL 0.3494 mL 0.6987 mL 1.7468 mL
50 mM 0.0559 mL 0.2795 mL 0.5590 mL 1.3975 mL
60 mM 0.0466 mL 0.2329 mL 0.4658 mL 1.1646 mL
80 mM 0.0349 mL 0.1747 mL 0.3494 mL 0.8734 mL
100 mM 0.0279 mL 0.1397 mL 0.2795 mL 0.6987 mL
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PF 04531083 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PF 045310831079400-07-9PF04531083PF-04531083Sodium ChannelNa channelsNa+ channelsinflammationrespiratoryblood-brain barrierInhibitorinhibitorinhibit

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