2. Immunology/Inflammation Apoptosis
  3. NOD-like Receptor (NLR) Pyroptosis
  4. JT002

JT002 is an orally active and selective NLRP3 inflammasome assembly inhibitor. JT002 reduces NLRP3-dependent proinflammatory cytokine (such as IL-1β, IL-1α, IL-18) production and pyroptosis. JT002 blocks NLRP3 inflammasome complex formation. JT002 reduces airway hyperresponsiveness and airway neutrophilia in mice. JT002 can be used for the study of a variety of inflammatory diseases, such as Muckle-Wells syndrome (MWS).

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

JT002 Chemical Structure

JT002 Chemical Structure

CAS No. : 2238820-43-2

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Based on 1 publication(s) in Google Scholar

JT002 Related Antibodies

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Description

JT002 is an orally active and selective NLRP3 inflammasome assembly inhibitor. JT002 reduces NLRP3-dependent proinflammatory cytokine (such as IL-1β, IL-1α, IL-18) production and pyroptosis. JT002 blocks NLRP3 inflammasome complex formation. JT002 reduces airway hyperresponsiveness and airway neutrophilia in mice. JT002 can be used for the study of a variety of inflammatory diseases, such as Muckle-Wells syndrome (MWS)[1].

In Vitro

In human peripheral blood mononuclear cells (hPBMCs) treated with Lipopolysaccharides (HY-D1056) (LPS) and activated with ATP (HY-B2176), JT002 shows concentration-dependent inhibition of IL-1α, IL-1β and IL-18 production with mean IC50 values of 3 nM, 4 nM and 4 nM, respectively, with no effect on TNFα production[1].
Under LPS plus Nigericin (HY-127019) stimulating conditions, JT002 inhibits IL-1β production from human, mouse and rat PBMCs with mean IC50 values of 6, 25 and 159 nM, respectively[1].
In human and mouse blood stimulated with LPS plus ATP, JT002 shows concentration-dependent inhibition of IL-1β production with mean IC50 values of 100 nM and 94 nM, respectively[1].
JT002 inhibits pyroptosis in LPS plus nigericin stimulated mouse bone-marrow derived macrophages (mBMDMs) as measured by cellular ATP content, with a mean IC50 value of 7 nM[1].
JT002 blocks canonical NLRP3-dependent IL-1β production activated downstream of ATP, Nigericin, cholesterol crystals (CHC) or monosodium urate (MSU) with mean IC50 values of 5 nM, 23 nM, 2 nM and 3 nM, respectively and inhibits non-canonical induced IL-1β production with a mean IC50 value of 30 nM[1].
JT002 shows no inhibition of IL-1β production after NLRP1, NLRC4 or AIM2 activation at concentrations up to 10 µM[1].
JT002 blocks NLRP3 inflammasome complex formation and downstream pathway activation. JT002 inhibits cellular caspase-1 activity with an IC50 of 8 nM in human PBMCs[1].

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

JT002 Related Antibodies
Parmacokinetics[1]
Species Dose SampleTime Route Indicator value Note
Mice 300 mg/kg p.o. AUC 8030 ng·h/mL
Rat 10 mg/kg 1 day i.v. Clearance (CL) 213 μg/mL Age: 6-8 weeks
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 200 mg/kg p.o. AUC 3580 ng·h/mL
Dog 45 mg/kg p.o. AUC 96,500 ng·h/mL
Dog 5 mg/kg 30 i.v. Vd 2.50 L/kg
Mice 10 mg/kg p.o. AUC 4929 ng·h/mL
Cynomolgus Monkey 10 mg/kg 1 day i.v. Clearance (CL) 369 μg/mL
Mice 1 mg/kg i.v. Plasma Concentration 2090±229 ng/mL
Mice 1 mg/kg i.v. Plasma Concentration 11700 ng/mL
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 500 mg/kg p.o. AUC 12400 ng·h/mL
Rat 10 mg/kg i.g. Tmax 4 hr
Dog 50 mg/kg p.o. AUC 61800 ng·h/mL
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
Rat 10 mg/kg p.o. Plasma Concentration 6.41 ng/mL
Rat 10 mg/kg i.g. T1/2 0.82 hr
Rat 2 mg/kg p.o. T1/2 N.D.
Dog 3 mg/kg p.o. Vd 2.50 L/kg
Mice 5 mg/kg 1 h i.v. AUC 14525 ng·h/mL
Mice 10 mg/kg p.o. Plasma Concentration 3543 ng/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
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
Rat 10 mg/kg p.o. T1/2 0.4 hr SD Rats
Dog 50 mg/kg p.o. AUC 61800 ng·h/mL
Mice 1.92 mg/kg i.v. AUC 15,500 ng·h/mL
Mice 2 mg/kg i.v. T1/2 3.21 hr
Pig 10 mg/kg p.o. Bioavailability 0.23 %
Mice 20 mg/kg 1 h p.o. AUC 57916 ng·h/mL
Mice 30 mg/kg i.v. AUC 7922.2 ng·h/mL
Rat 1 mg/kg i.v. AUC 4726 ng·h/mL
Dog 300 mg/kg p.o. Tmax 1.5 hr
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
Rat 5 mg/kg 30 i.v. Clearance (CL) 34.7 mL/min/kg
Rat 500 mg/kg p.o. AUC 8050 ng·h/mL
Cynomolgus Monkey 84 mg/kg p.o. AUC 90900 ng·h/mL
Dog 1 mg/kg i.v. Plasma Concentration 7.0 μg/mL
Dog 1400 mg/kg p.o. AUC 551 μg·h/mL
Rat 7 mg/kg 36 h i.v. T1/2 1.13 hr
Rat 10 mg/kg p.o. T1/2 27 min
Rat 7 mg/kg 36 h p.o. Clearance (CL) 0.54 μg/mL
Rat 45 (female) mg/kg p.o. AUC 181,000 ng·h/mL
Rat 2 mg/kg i.v. AUC 5743.547 mg·h/L
Dog 25 mg/kg p.o. AUC 30500 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 mg/kg i.v. Clearance (CL) 9.02 mL/min/kg
Rat 1 mg/kg i.v. Plasma Concentration 1953 ng/mL
Rat 10 mg/kg p.o. T1/2 2.41 hr
Mice 10 mg/kg p.o. T1/2 2.08 hr
Rat 1 mg/kg i.v. Plasma Concentration 410.82 ng/mL
Rat 10 mg/kg i.p. T1/2 1.90 hr
Dog 1 mg/kg p.o. Tmax 1.0 hr
Rat 10 mg/kg i.v. T1/2 12.89 min
Rat 100 mg/kg p.o. AUC 2000 ng·h/mL
Rat 7 mg/kg 36 h i.p. T1/2 1.22 hr
Rat 1 mg/kg i.v. T1/2 3.4 hr
Mice 10 mg/kg i.v. T1/2 5.15 hr
Rat 1 mg/kg i.v. T1/2 5.82 hr
Rat 100 mg/kg 1 day i.v. AUC 170000 μg·h/mL Age: 6-8 weeks
Mice 1 mg/kg i.v. Clearance (CL) 11.6 mL/min/kg
Dog 12.5 mg/kg p.o. AUC 15200 ng·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. AUC 1997 ng·h/mL
Mice 1.6 mg/kg i.v. Clearance (CL) 7.3417 mL/min/kg
Rat 1.13 (female) mg/kg i.v. AUC 5,110 ng·h/mL
Mice 10 mg/kg p.o. Plasma Concentration 1580±427 ng/mL
Rat 10 mg/kg p.o. T1/2 8.28 hr
Rhesus monkey 2, 10, 50 or repeat 50 mg/kg i.v. Plasma Concentration 1 mg/mL 1 h infusion
Mice 30 mg/kg p.o. AUC 3879.5 ng·h/mL
Rat 3 mg/kg 24 h p.o. T1/2 8.27 hr
Rat 0.4 mg/kg i.v. Clearance (CL) 0.4 L/h/kg
Rat 10 mg/kg i.v. T1/2 2.47±0.14 hr
Mice 500 mg/kg p.o. AUC 12400 ng·h/mL
Dog 25 mg/kg p.o. AUC 30500 ng·h/mL
Rat 1 mg/kg 24 h i.v. T1/2 14.38 hr
Rat 1 mg/kg i.v. Tmax - hr
Rat 10 mg/kg p.o. AUC 8061 ng·h/mL
Dog 10 mg/kg i.v. T1/2 18 min
Mice 5 mg/kg p.o. Bioavailability 45 %
Rat 2.5 mg/kg i.v. Plasma Concentration 1140.35 μg/L
Dog 10 mg/kg p.o. T1/2 34.3 hr
Mice 30 mg/kg p.o. AUC 14716 ng·h/mL
Rat 7 mg/kg 36 h p.o. Tmax 2.25 hr
Cynomolgus Monkey 1.35 mg/kg i.v. AUC 2,100 ng·h/mL
Mice 1 mg/kg i.v. Plasma Concentration 264 ng/mL
Rat 5 mg/kg i.p. AUC 9631 ng·h/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. Plasma Concentration 417 ng/mL
Rat 5 mg/kg p.o. T1/2 5.5 hr
Mice 300 mg/kg p.o. AUC 8030 ng·h/mL
Rat 100 mg/kg p.o. AUC 2000 ng·h/mL
Mice 5 mg/kg i.v. T1/2 13 min
Rat 30 mg/kg i.v. T1/2 2.49±0.07 hr
Mice 100 mg/kg p.o. T1/2 3.74 hr
Cynomolgus Monkey 100 mg/kg 1 day i.v. Clearance (CL) 2560 μg/mL
Mice 30 mg/kg 0.5, 1, 2, 4, 8, 24 h o.a. Tmax 0.5 hr
Rat 200 mg/kg p.o. AUC 3580 ng·h/mL
Mice 1 mg/kg i.v. T1/2 2.42 hr
Rat 5 mg/kg p.o. Tmax 0.5 hr
Rat 20 mg/kg p.o. T1/2 20.33 hr
Dog 1400 mg/kg p.o. Plasma Concentration 130 μg/mL
Rat 2 mg/kg i.v. AUC 257 ng·h/mL
Mice 100 mg/kg p.o. Tmax 4 hr
Rat 7 mg/kg 36 h i.v. AUC 4.09 μg·h/mL
Dog 1 mg/kg i.v. AUC 6,230 ng·h/mL
Mice 10 mg/kg p.o. Plasma Concentration 328 ng/mL
Mice 1 mg/kg i.v. Clearance (CL) 0.82 (9.9) L/h/kg
Rat 1 mg/kg i.v. T1/2 3.9 hr
Cynomolgus Monkey 84 mg/kg p.o. AUC 90900 ng·h/mL
Rat 10 mg/kg i.g. T1/2 7.59 hr
Mice 10 mg/kg p.o. AUC 1602 ng·h/mL
Mice 5 mg/kg 0.25, 0.5, 1, 2, 4, 8, 24 h p.o. T1/2 3.15 hr
Rat 10 mg/kg i.v. Plasma Concentration 1662.94 μg/L
Rat 0.8 mg/kg p.o. Clearance (CL) 1.2 L/h/kg
Rat 1 mg/kg p.o. Tmax 0.31 hr
Mice 30 mg/kg 10 min p.o. Plasma Concentration 2802 ng/mL
Dog 12.5 mg/kg p.o. AUC 15200 ng·h/mL
Mice 3 mg/kg p.o. AUC 5.199 μg·h/mL
Dog 600 mg/kg p.o. Tmax 1.5 hr
Rat 5 mg/kg i.v. Plasma Concentration 1393.22 μg/L
Rat 2 mg/kg i.v. T1/2 2.2 hr SD Rats
Mice 5 mg/kg p.o. Plasma Concentration 5880 ng/mL
Rat 45 (male) mg/kg p.o. AUC 99,600 ng·h/mL
Mice 10 mg/kg p.o. Clearance (CL) 9.02 mL/min/kg
Rat 500 mg/kg p.o. AUC 8050 ng·h/mL
Rat 20 mg/kg p.o. AUC 52.21 ng·h/mL
Mice 10 mg/kg i.g. AUC 0.136 μg·h/mL
Mice 1 mg/kg i.v. AUC 0.424 μg·h/mL
Mice 2 mg/kg 0.25, 0.5, 1, 2, 4, 8, 24 h i.v. T1/2 2.37 hr
Rat 2 mg/kg i.v. T1/2 2.68 hr
Mice 45 mg/kg p.o. AUC 215,000 ng·h/mL
Rat 20 mg/kg p.o. Plasma Concentration 22.45 ng/mL
Rat 5 mg/kg p.o. Clearance (CL) 34.7 mL/min/kg
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
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
Cynomolgus Monkey 30 mg/kg 1 day i.v. Clearance (CL) 876 μg/mL
Mice 30 mg/kg i.p. Plasma Concentration 342.5 ng/mL
Mice 1 mg/kg i.v. Clearance (CL) 43.7 mL/min/kg
Mice 10 mg/kg p.o. Bioavailability 78 %
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
Mice 5 mg/kg 0.25, 0.5, 1, 2, 4, 8, 24 h p.o. Tmax 0.42 hr
Rat 1 mg/kg i.v. AUC 0.714 μg·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
Rat 10 mg/kg p.o. Bioavailability 0.9 %
Rat 5 mg/kg p.o. Plasma Concentration 15.6 μg/mL
Mice 1 mg/kg i.v. Vd 1.76 L/kg
Dog 25 mg/kg p.o. T1/2 3.76 hr
Dog 50 mg/kg p.o. T1/2 3.51 hr
Rat 10 mg/kg i.g. Plasma Concentration 587.67±12.66 ng/mL
Rat 1.13 (female) mg/kg i.v. Clearance (CL) 3.7 mL/min/kg
Rat 1 mg/kg i.v. AUC 8.35 μg·h/mL
Rat 2 mg/kg p.o. Tmax 1.3 hr
Mice 5 mg/kg 1 h i.v. T1/2 3.63 hr
Dog 25 mg/kg p.o. T1/2 3.76 hr
Rat 10 mg/kg i.p. Tmax 0.85 hr
Dog 600 mg/kg p.o. Plasma Concentration 123 μg/mL
Rat 7 mg/kg 36 h p.o. Tmax 2.25 hr
Mice 5 mg/kg p.o. Tmax 1 hr
Rat 100 mg/kg 1 day i.v. Clearance (CL) 2360 μg/mL Age: 6-8 weeks
Mice 10 mg/kg p.o. Tmax 6 hr
Mice 1 mg/kg i.v. Tmax 0.083 hr
Mice 30 mg/kg i.p. AUC 1022 ng·h/mL
Rat 2 mg/kg i.v. Tmax 0.1 hr SD Rats
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 10 mg/kg p.o. AUC 14146±5297 ng·h/mL
Rat 2 mg/kg i.v. Tmax 0.75 hr
Mice 2 mg/kg 0.25, 0.5, 1, 2, 4, 8, 24 h i.v. AUC 437 ng·h/mL
Rat 10 mg/kg p.o. AUC 7689 ng·h/mL
Mice 10 mg/kg p.o. Tmax 0.75 hr
Rat 100 mg/kg p.o. T1/2 1.48 hr
Rat 1 mg/kg i.v. AUC 3869 ng·h/mL
Dog 300 mg/kg p.o. AUC 388 μg·h/mL
Rat 1 mg/kg i.v. Plasma Concentration 10.6 μg/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
Mice 300 mg/kg p.o. T1/2 1.58 hr
Mice 1 mg/kg i.v. AUC 4229±742 ng·h/mL
Dog 300 mg/kg p.o. Plasma Concentration 101 μg/mL
Mice 300 mg/kg p.o. T1/2 1.58 hr
Rat 20 mg/kg 0.25, 0.5, 1, 2, 4, 8, 12, 24 p.o. Plasma Concentration 160 ng/mL
Rat 10 mg/kg i.g. Tmax 0.5 hr
Rhesus monkey 2, 10, 50 or repeat 50 mg/kg i.v. T1/2 326.4 hr 1 h infusion
Cynomolgus Monkey 10 mg/kg 1 day i.v. Tmax 1 hr
Mice 1 mg/kg i.v. Plasma Concentration 2054.53 ng·h/mL
Mice 30 mg/kg p.o. Tmax 3 hr
Dog 10 mg/kg p.o. Plasma Concentration 868 ng/mL
Mice 1 mg/kg i.v. AUC 0.431 μg·h/mL
Rat 5 mg/kg p.o. Tmax 1.2 hr
Mice 5 mg/kg p.o. AUC 2744 ng·h/mL
Rat 100 mg/kg p.o. T1/2 1.48 hr
Mice 10 mg/kg p.o. Vd 1.76 L/kg
Rat 200 mg/kg p.o. T1/2 1.84 hr
Rat 20 mg/kg p.o. Tmax 0.33 hr
Rat 30 mg/kg i.g. Plasma Concentration 1521.25±100.76 ng/mL
Rat 20 mg/kg p.o. AUC 55.68 ng·h/mL
Rat 1 mg/kg i.v. Tmax -
Rat 20 mg/kg p.o. Tmax 0.5 hr
Mice 30 mg/kg 0.5, 1, 2, 4, 8, 24 h o.a. Plasma Concentration 1093.2 μg/mL
Cynomolgus Monkey 100 mg/kg 1 day i.v. Tmax 1 hr
Dog 50 mg/kg p.o. T1/2 3.51 hr
Rat 1 mg/kg 0.083, 0.25, 0.5, 1, 2, 4, 8, 12, 24 h i.v. T1/2 4.3 hr
Mice 3 mg/kg p.o. AUC 5.138 μg·h/mL
Dog 5 mg/kg 30 i.v. T1/2 1.92 hr
Dog 1 mg/kg i.v. Clearance (CL) 3 mL/min/kg
Mice 100 mg/kg p.o. Tmax 4.00 hr
Rat 5 mg/kg 30 i.v. Vd 2.1 L/kg
Pig 10 mg/kg p.o. T1/2 1.7 hr
Rat 0.4 mg/kg i.v. Vd 2.2 L/kg
Mice 500 mg/kg p.o. T1/2 1.9 hr
Dog 10 mg/kg i.v. T1/2 104 min
Dog 45 mg/kg p.o. Plasma Concentration 3,630 ng/mL
Mice 1 mg/kg i.v. Vd 1.9 L/kg
Mice 10 mg/kg p.o. T1/2 0.77 hr
Rat 1.13 (male) mg/kg i.v. Clearance (CL) 7.7 mL/min/kg
Rat 0.8 mg/kg p.o. Vd 3.2 L/kg
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
Rat 1 mg/kg 24 h i.v. Plasma Concentration 106.16 ng/mL
Rat 200 mg/kg p.o. T1/2 1.84 hr
Rat 10 mg/kg p.o. Tmax 0.42 hr
Mice 10 mg/kg i.v. Clearance (CL) 480.8 mL/h/kg
Rat 7 mg/kg 36 h i.v. Clearance (CL) 1.77 L/h/kg
Rat 10 mg/kg i.v. AUC 1.28 mg·h/L
Rat 7 mg/kg 36 h i.v. AUC 4.09 μg·h/mL
Mice 10 mg/kg p.o. T1/2 2.43 hr
Mice 100 mg/kg p.o. AUC 32178 ng·h/mL
Rat 10 mg/kg p.o. Plasma Concentration 173 ng/mL
Rat 10 mg/kg p.o. AUC 0.319 μg·h/mL
Rat 5 mg/kg 0.25, 0.5, 1, 2, 4, 8 and 24 h p.o. Tmax 2.67 hr
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
Rat 30 mg/kg 1 day i.v. Clearance (CL) 695 μg/mL Age: 6-8 weeks
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 1 mg/kg i.v. Tmax 0.083 hr
Dog 12.5 mg/kg p.o. T1/2 4.01 hr
Cynomolgus Monkey 84 mg/kg p.o. T1/2 4.84 hr
Mice 10 mg/kg p.o. Plasma Concentration 3677.25 ng/mL
Rat 10 mg/kg i.v. MRT 3.65±0.30 hr
Rat 10 mg/kg i.v. T1/2 46.80 min
Mice 1.92 mg/kg i.v. Clearance (CL) 2.1 mL/min/kg
Rat 45 (female) mg/kg p.o. Plasma Concentration 15,600 ng/mL
Rat 7 mg/kg 36 h i.p. AUC 3.38 μg·h/mL
Mice 1.6 mg/kg i.v. T1/2 6.65 hr
Cynomolgus Monkey 30 mg/kg 1 day i.v. Tmax 1 hr
Rat 500 mg/kg p.o. T1/2 2.03 hr
Mice 30 mg/kg i.v. AUC 7905.7 ng·h/mL
Rat 2 mg/kg i.v. AUC 5747.104 mg·h/L
Rat 45 (male) mg/kg p.o. Plasma Concentration 12,000 ng/mL
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
Rat 7 mg/kg 36 h p.o. T1/2 1.04 hr
Mice 1 mg/kg i.v. Vd 0.843 L/kg
Rat 5 mg/kg p.o. Vd 2.1 L/kg
Mice 10 mg/kg i.g. AUC 0.138 μg·h/mL
Rat 10 mg/kg p.o. Plasma Concentration 1366.5 ng/mL SD Rats
Rat 1 mg/kg i.v. Tmax 0.033 hr
Rat 5 mg/kg i.v. AUC 0.76 mg·h/L
Mice 45 mg/kg p.o. Plasma Concentration 26,300 ng/mL
Mice 20 mg/kg 1 h p.o. Bioavailability 99.6 %
Mice 1 mg/kg i.v. AUC 8160 ng·h/mL
Dog 1 mg/kg i.v. T1/2 1.1 hr
Cynomolgus Monkey 84 mg/kg p.o. T1/2 4.84 hr
Dog 1400 mg/kg p.o. Tmax 3 hr
Rat 5 mg/kg i.p. Plasma Concentration 1966 ng/mL
Rat 2 mg/kg i.v. AUC 258 ng·h/mL
Rat 3 mg/kg 24 h p.o. Tmax 0.5 hr
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
Dog 3 mg/kg p.o. T1/2 1.92 hr
Dog 1 mg/kg p.o. Plasma Concentration 4.0 μg/mL
Rat 30 mg/kg i.v. MRT 3.86±0.06 hr
Mice 30 mg/kg p.o. AUC 3854.7 ng·h/mL
Rat 10 mg/kg i.g. Tmax 5.53 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. AUC 2765 ng·h/mL
Mice 10 mg/kg p.o. AUC 20320 ng·h/mL
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 1 mg/kg p.o. Plasma Concentration 3.99 ng/mL
Mice 500 mg/kg p.o. T1/2 1.90 hr
Dog 100 mg/kg p.o. AUC 171 μg·h/mL
Rat 100 mg/kg p.o. Plasma Concentration 1200 ng/mL
Mice 30 mg/kg 0.5, 1, 2, 4, 8, 24 h o.a. T1/2 7.5 hr
Rat 30 mg/kg 1 day i.v. Tmax 1 hr Age: 6-8 weeks
Mice 300 mg/kg p.o. Plasma Concentration 7290 ng/mL
Rat 200 mg/kg p.o. Plasma Concentration 2650 ng/mL
Rat 7 mg/kg 36 h i.v. Clearance (CL) 1.77 L/h/kg
Mice 1.6 mg/kg i.v. Plasma Concentration 3486.7 ng/mL
Rat 100 mg/kg p.o. Plasma Concentration 1200 ng/mL
Dog 1 mg/kg i.v. Vd 2.3 L/kg
Rat 10 mg/kg i.v. AUC 1.29 mg·h/L
Rat 10 mg/kg i.g. T1/2 2.53±0.12 hr
Rat 500 mg/kg p.o. Plasma Concentration 6460 ng/mL
Mice 45 mg/kg p.o. Bioavailability 59%
Rat 10 mg/kg i.g. Plasma Concentration 1900 ng/mL
Rat 10 mg/kg i.p. Plasma Concentration 5205 ng/mL
Rat 10 mg/kg 1 day i.v. Tmax 1.0 hr Age: 6-8 weeks
Rat 30 mg/kg i.v. AUC 107,689.72±6779.70 ng/L.h
Rat 7 mg/kg 36 h p.o. T1/2 1.04 hr
Rat 20 mg/kg p.o. Plasma Concentration 29.7 ng/mL
Rat 2 mg/kg p.o. Clearance (CL) 11.4 mL/min/kg
Rat 10 mg/kg p.o. AUC 3212 ng·h/mL
Rat 500 mg/kg p.o. Plasma Concentration 6460 ng/mL
Cynomolgus Monkey 10 mg/kg 1 day i.v. AUC 30400 μg·h/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 300 mg/kg p.o. Plasma Concentration 7290 ng/mL
Rat 7 mg/kg 36 h i.v. Clearance (CL) 2.23 L/kg
Mice 1 mg/kg i.v. T1/2 2.47 hr
Mice 10 mg/kg i.g. MRT 5.76 hr
Rat 20 mg/kg p.o. MRT 7.60 hr
Cynomolgus Monkey 1.35 mg/kg i.v. Vd 1.6 L/kg
Mice 500 mg/kg p.o. Plasma Concentration 10600 ng/mL
Mice 2 mg/kg i.v. Vd 1.02 L/kg
Rat 20 mg/kg i.g. AUC 0.28 mg·h/L
Rat 30 mg/kg i.g. T1/2 2.57±0.09 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. Plasma Concentration 600 ng/mL
Mice 1 mg/kg i.v. T1/2 0.59 hr
Mice 10 mg/kg p.o. MRT 5.23 hr
Rat 1.13 (male) mg/kg i.v. Vd 0.34 L/kg
Mice 1 mg/kg i.v. Vd 0.90 L/kg
Rat 10 mg/kg i.v. Vd 1.62 L/kg
Cynomolgus Monkey 84 mg/kg p.o. Plasma Concentration 18800 ng/mL
Cynomolgus Monkey 84 mg/kg p.o. Plasma Concentration 18800 ng/mL
Rat 3 mg/kg 24 h p.o. Plasma Concentration 37.94 ng/mL
Dog 25 mg/kg p.o. Plasma Concentration 7080 ng/mL
Dog 12.5 mg/kg p.o. Plasma Concentration 3600 ng/mL
Mice 10 mg/kg p.o. T1/2 1.2 hr
Dog 10 mg/kg i.v. Vd 3.17 L/kg
Dog 12.5 mg/kg p.o. Plasma Concentration 3600 ng/mL
Rat 10 mg/kg i.v. AUC 34,263.98±1100.87 ng/L.h
Rat 1 mg/kg i.v. T1/2 1.91 hr
Mice 1 mg/kg i.v. AUC 4245±745 ng·h/mL
Mice 10 mg/kg p.o. AUC 19689.35 ng·h/mL
Rat 2 mg/kg i.v. MRT 1.74 hr
Rat 1 mg/kg i.v. AUC 0.1674 μg·h/mL
Rat 1 mg/kg i.v. Clearance (CL) 6.7 mL/min/kg
Rat 10 mg/kg i.g. Plasma Concentration 726 ng/mL
Rat 20 mg/kg 0.25, 0.5, 1, 2, 4, 8, 12, 24 p.o. Bioavailability 2.1 %
Mice 30 mg/kg i.p. T1/2 3.24 hr
Rat 0.4 mg/kg i.v. T1/2 6.2 hr
Rat 5 mg/kg i.p. Clearance (CL) 524.9 mL/h/kg
Dog 50 mg/kg p.o. Plasma Concentration 13200 ng/mL
Mice 100 mg/kg p.o. Plasma Concentration 15.17 ng/mL
Dog 5 mg/kg 30 i.v. Bioavailability 51.3 %
Mice 10 mg/kg i.v. Vd 3.56 L/kg
Dog 1 mg/kg i.v. AUC 10.6 μg·h/mL
Rat 1 mg/kg p.o. T1/2 9.49 hr
Pig 10 mg/kg p.o. T1/2 2.83 hr
Rat 10 mg/kg p.o. AUC 771 ng·h/mL SD Rats
Dog 3 mg/kg p.o. Bioavailability 51.3 %
Mice 30 mg/kg i.v. Plasma Concentration 19300 ng/mL
Rat 5 mg/kg p.o. Plasma Concentration 356 ng/mL
Rat 5 mg/kg 0.25, 0.5, 1, 2, 4, 8 and 24 h p.o. Plasma Concentration 256.40 ng/mL
Rat 5 mg/kg i.v. AUC 0.77 mg·h/L
Mice 10 mg/kg p.o. AUC 14173±5307 ng·h/mL
Dog 25 mg/kg p.o. Plasma Concentration 7080 ng/mL
Mice 1 mg/kg i.v. MRT 1.22 hr
Mice 10 mg/kg p.o. T1/2 2.47 hr
Mice 5 mg/kg p.o. AUC 35700 ng·h/mL
Rat 1.13 (female) mg/kg i.v. Vd 1 L/kg
Mice 20 mg/kg 1 h p.o. T1/2 2.70 hr
Rat 2.5 mg/kg i.v. AUC 0.48 mg·h/L
Mice 10 mg/kg p.o. Plasma Concentration 1923.7 ng/mL
Mice 10 mg/kg p.o. T1/2 2.73 hr
Rat 20 mg/kg p.o. AUC 0.0246 μg·h/mL
Rat 1 mg/kg i.v. AUC 0.780 μg·h/mL
Rat 5 mg/kg 30 i.v. T1/2 2.31 hr
Rat 2 mg/kg i.v. Plasma Concentration 53.13 ng/mL
Mice 1 mg/kg i.v. AUC 3135.27 ng·h/mL
Cynomolgus Monkey 100 mg/kg 1 day i.v. AUC 240000 μg·h/mL
Mice 1 mg/kg i.v. AUC 8620 ng·h/mL
Mice 5 mg/kg 0.25, 0.5, 1, 2, 4, 8, 24 h p.o. Plasma Concentration 137 ng·h/mL
Dog 45 mg/kg p.o. Bioavailability 34%
Rat 5 mg/kg p.o. T1/2 2.31 hr
Dog 50 mg/kg p.o. Plasma Concentration 13200 ng/mL
Rat 200 mg/kg p.o. Plasma Concentration 2650 ng/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. T1/2 2.6 hr
Rat 0.8 mg/kg p.o. T1/2 3.1 hr
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 %
Rat 5 mg/kg p.o. T1/2 23.4 hr
Rat 10 mg/kg p.o. T1/2 2.10 hr
Mice 2 mg/kg 0.25, 0.5, 1, 2, 4, 8, 24 h i.v. MRT 0.4 hr
Dog 10 mg/kg p.o. AUC 15420 ng·h/mL
Mice 1 mg/kg i.v. T1/2 1.6 hr
Rat 2 mg/kg i.v. MRT 0.804 hr
Rat 45 (male) mg/kg p.o. Bioavailability 95%
Mice 3 mg/kg p.o. T1/2 3.63 hr
Rat 1 mg/kg 24 h i.v. AUC 121.54 ng·h/mL
Mice 1 mg/kg i.v. MRT 1.90 hr
Rat 45 (female) mg/kg p.o. Bioavailability 89%
Rat 1 mg/kg i.v. T1/2 2.8 hr
Rat 7 mg/kg 36 h p.o. Plasma Concentration 0.54 μg/mL
Rat 1 mg/kg i.v. Plasma Concentration 1050 ng/mL
Rat 10 mg/kg p.o. Plasma Concentration 1296 ng/mL
Mice 30 mg/kg p.o. Plasma Concentration 4840 ng/mL
Mice 5 mg/kg p.o. Plasma Concentration 1570 ng/mL
Mice 1.92 mg/kg i.v. Vd 0.34 L/kg
Rat 100 mg/kg 1 day i.v. Tmax 1 hr Age: 6-8 weeks
Dog 1 mg/kg p.o. T1/2 1.4 hr
Mice 500 mg/kg p.o. Plasma Concentration 10600 ng/mL
Dog 5 mg/kg 30 i.v. Clearance (CL) 23.7 mL/min/kg
Rat 1 mg/kg i.v. AUC 358 ng·h/mL
Mice 30 mg/kg i.v. Clearance (CL) 63.11 mL/min/kg
Rat 7 mg/kg 36 h p.o. AUC 3.38 μg·h/mL
Rat 20 mg/kg 0.25, 0.5, 1, 2, 4, 8, 12, 24 p.o. T1/2 7.1 hr
Dog 10 mg/kg p.o. Bioavailability 33.9 %
Rat 5 mg/kg 0.25, 0.5, 1, 2, 4, 8 and 24 h p.o. AUC 1377.38 ng·h/mL
Rat 20 mg/kg p.o. AUC 0.0214 μg·h/mL
Mice 1 mg/kg i.v. AUC 181 ng·h/mL
Rat 2 mg/kg i.v. T1/2 0.746 hr
Rat 500 mg/kg p.o. Tmax 0.083 hr
Dog 25 mg/kg p.o. Tmax 1.5 hr
Mice 10 mg/kg p.o. AUC 820 ng·h/mL
Rat 1 mg/kg i.v. AUC 0.1652 μg·h/mL
Rat 10 mg/kg i.v. AUC 34,341.50±908.33 ng/L.h
Rat 10 mg/kg p.o. MRT 0.5 hr SD Rats
Dog 12.5 mg/kg p.o. Tmax 2.0 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 i.g. MRT 1.65 hr
Rat 30 mg/kg i.g. MRT 5.37±0.32 hr
Rat 1 mg/kg i.v. Vd 2.25 L/kg
Rat 1 mg/kg i.v. T1/2 5.45 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 %
Rat 0.4 mg/kg i.v. AUC 3.1 kg·h/L
Mice 100 mg/kg p.o. Vd 4.97 L/kg
Dog 3 mg/kg p.o. Clearance (CL) 23.7 mL/min/kg
Mice 1 mg/kg i.v. T1/2 0.26 hr
Rat 500 mg/kg p.o. Tmax 0.083 hr
Mice 30 mg/kg 0.5, 1, 2, 4, 8, 24 h o.a. AUC 3088.3 ng·h/mL
Dog 50 mg/kg p.o. Tmax 2.0 hr
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 %
Mice 10 mg/kg p.o. MRT 4.34 hr
Mice 1.6 mg/kg i.v. AUC 3.6375 μg·h/mL
Rat 5 mg/kg 30 i.v. Bioavailability 49.8 %
Rat 20 mg/kg p.o. AUC 0.9504 μg·h/mL
Rat 2.5 mg/kg i.v. MRT 0.62 hr
Rat 10 mg/kg p.o. Bioavailability 5.13 %
Rat 5 mg/kg p.o. AUC 59.2 μg·h/mL
Rat 30 mg/kg i.v. AUC 108,414.07±5853.89 ng/L.h
Mice 500 mg/kg p.o. Tmax 0.25 hr
Mice 5 mg/kg p.o. AUC 37200 ng·h/mL
Mice 10 mg/kg i.g. T1/2 3.84 hr
Rat 20 mg/kg p.o. MRT 11.67 hr
Dog 1 mg/kg i.v. Clearance (CL) 1.8 mL/min/kg
Mice 10 mg/kg p.o. Bioavailability 99.0 %
Rat 10 mg/kg i.v. MRT 0.80 hr
Dog 50 mg/kg p.o. Tmax 2.0 hr
Mice 1 mg/kg i.v. Bioavailability 99.0 %
Mice 1 mg/kg i.v. T1/2 3.55±0.17 hr
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.g. AUC 29.3 μg·h/mL
Mice 20 mg/kg 1 h p.o. Tmax 0.33 hr
Mice 30 mg/kg p.o. Clearance (CL) 123.9 mL/min/kg
Rat 10 mg/kg p.o. AUC 8.22 ng·h/mL
Mice 2 mg/kg 0.25, 0.5, 1, 2, 4, 8, 24 h i.v. Clearance (CL) 79.8 mL/min/kg
Dog 25 mg/kg p.o. Tmax 1.5 hr
Rat 5 mg/kg i.v. MRT 0.72 hr
Mice 1 mg/kg i.v. AUC 3138.30 ng·h/mL
Rat 2 mg/kg i.v. AUC 0.1042 μg·h/mL
Rat 2 mg/kg p.o. Vd -
Rat 5 mg/kg p.o. Bioavailability 49.8 %
Mice 2 mg/kg i.v. Clearance (CL) 4.80 mL/min/kg
Rat 100 mg/kg p.o. Tmax 0.17 hr
Mice 1 mg/kg i.v. T1/2 1.50 hr
Mice 5 mg/kg p.o. Tmax 1.5 hr
Cynomolgus Monkey 84 mg/kg p.o. Tmax 2.7 hr
Cynomolgus Monkey 84 mg/kg p.o. Tmax 2.7 hr
Rat 1 mg/kg i.v. AUC 16.2 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 10 mg/kg p.o. T1/2 3.47 hr
Rat 7 mg/kg 36 h i.v. T1/2 1.13 hr
Mice 30 mg/kg i.p. AUC 1326 ng·h/mL
Pig 10 mg/kg p.o. Clearance (CL) 1.27 kg·h/L
Rat 7 mg/kg 36 h i.v. Vd 2.23 L/kg
Rat 1.13 (female) mg/kg i.v. T1/2 3.9 hr
Rat 200 mg/kg p.o. Tmax 0.083 hr
Dog 1 mg/kg p.o. AUC 11.6 μg·h/mL
Mice 10 mg/kg p.o. Plasma Concentration 4697 ng/mL
Mice 1 mg/kg i.v. AUC 1482 ng·h/mL
Rat 1.13 (male) mg/kg i.v. T1/2 2.3 hr
Rat 200 mg/kg p.o. Tmax 0.083 hr
Rat 5 mg/kg p.o. AUC 1.683 μg·h/mL
Dog 1 mg/kg i.v. T1/2 15 hr
Mice 3 mg/kg p.o. Plasma Concentration 1085.0 ng/mL
Mice 500 mg/kg p.o. Tmax 0.25 hr
Mice 5 mg/kg 0.25, 0.5, 1, 2, 4, 8, 24 h p.o. MRT 2.32 hr
Rat 20 mg/kg i.g. AUC 0.32 mg·h/L
Rat 1 mg/kg 24 h i.v. AUC 153.12 ng·h/mL
Cynomolgus Monkey 1.35 mg/kg i.v. T1/2 2.2 hr
Rat 2 mg/kg i.v. MRT 1.95 hr
Rat 7 mg/kg 36 h p.o. AUC 1.70 μg·h/mL
Mice 1.92 mg/kg i.v. T1/2 2.6 hr
Mice 300 mg/kg p.o. Tmax 0.25 hr
Rat 5 mg/kg i.p. T1/2 5.2 hr
Rat 100 mg/kg p.o. Tmax 0.17 hr
Mice 300 mg/kg p.o. Tmax 0.25 hr
Mice 10 mg/kg i.v. AUC 20800 ng·h/mL
Dog 12.5 mg/kg p.o. Tmax 2.0 hr
Rat 10 mg/kg i.v. Clearance (CL) 32.26 mL/min/kg
Rat 10 mg/kg i.p. AUC 12.099 ng·h/mL
Mice 10 mg/kg p.o. T1/2 2.51±0.06 hr
Mice 10 mg/kg p.o. AUC 29708 ng·h/mL
Rat 2 mg/kg i.v. MRT 1.7 hr SD Rats
Mice 1 mg/kg i.v. T1/2 1.45 hr
Mice 10 mg/kg p.o. Bioavailability 45.8 %
Rat 1 mg/kg i.v. Tmax 0.17 hr
Mice 10 mg/kg i.g. Tmax 1 hr
Rat 100 mg/kg p.o. Bioavailability 2.94 %
Dog 1 mg/kg p.o. Bioavailability 100 %
Mice 100 mg/kg p.o. Clearance (CL) 0.92 L/h/kg
Rat 2 mg/kg i.v. AUC 0.1053 μg·h/mL
Mice 1 mg/kg i.v. Bioavailability 32.08 %
Mice 1 mg/kg i.v. MRT 1.83 hr
Rat 200 mg/kg p.o. Bioavailability 2.62 %
Mice 300 mg/kg p.o. Bioavailability 5.06 %
Rat 200 mg/kg p.o. Bioavailability 2.62 %
Mice 500 mg/kg p.o. Bioavailability 4.69 %
Rat 2 mg/kg i.v. T1/2 3.86 hr
Cynomolgus Monkey 84 mg/kg p.o. Bioavailability 48.3 %
Rat 5 mg/kg p.o. Clearance (CL) - mL/min/kg
Mice 10 mg/kg p.o. Bioavailability 137 %
Rat 1 mg/kg i.v. T1/2 0.43 hr
Rat 100 mg/kg p.o. Bioavailability 2.94 %
Mice 30 mg/kg p.o. MRT 1.2 hr
Mice 1.6 mg/kg i.v. AUC 3.5712 μg·h/mL
Rat 20 mg/kg p.o. AUC 0.2884 μg·h/mL
Rat 1 mg/kg i.v. Bioavailability -
Rat 20 mg/kg p.o. T1/2 7.36 hr
Rat 5 mg/kg 0.25, 0.5, 1, 2, 4, 8 and 24 h p.o. Bioavailability 54.25 %
Rat 5 mg/kg p.o. AUC 2.715 μg·h/mL
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 %
Mice 1 mg/kg i.v. Vd 0.536 L/kg
Rat 20 mg/kg p.o. T1/2 1.27 hr
Dog 25 mg/kg p.o. Bioavailability 83.5 %
Rat 5 mg/kg i.p. Tmax 0.5 hr
Rat 0.8 mg/kg p.o. Plasma Concentration 0.09 mg/mL
Rat 20 mg/kg i.g. MRT 5.86 hr
Rat 0.4 mg/kg i.v. Plasma Concentration 0.23 mg/mL
Mice 1 mg/kg i.v. Clearance (CL) 4.01±0.76 mL/min/kg
Rat 10 mg/kg p.o. MRT 0.81 hr
Rat 3 mg/kg 24 h p.o. AUC 157.95 ng·h/mL
Rat 1 mg/kg i.v. MRT 0.70 hr
Mice 1 mg/kg i.v. AUC 183 ng·h/mL
Mice 10 mg/kg p.o. MRT 3.71 hr
Dog 12.5 mg/kg p.o. Bioavailability 83.1 %
Rat 1 mg/kg i.v. Clearance (CL) 1.0 mL/min/kg
Mice 10 mg/kg p.o. Tmax 2 hr
Mice 10 mg/kg p.o. AUC 825 ng·h/mL
Mice 30 mg/kg i.v. MRT 0.4 hr
Mice 3 mg/kg p.o. Tmax 0.670 hr
Mice 30 mg/kg i.p. Tmax 1.5 hr
Mice 5 mg/kg 0.25, 0.5, 1, 2, 4, 8, 24 h p.o. Bioavailability 12.6 %
Cynomolgus Monkey 84 mg/kg p.o. Bioavailability 48.3 %
Rat 500 mg/kg p.o. Bioavailability 2.36 %
Rat 2 mg/kg p.o. Bioavailability 59 %
Pig 10 mg/kg p.o. AUC 19.77 ng·h/mL
Mice 500 mg/kg p.o. Bioavailability 4.69 %
Dog 25 mg/kg p.o. Bioavailability 83.5 %
Rat 1 mg/kg 24 h i.v. MRT 13.39 hr
Dog 1 mg/kg i.v. Vd 0.2 L/kg
Dog 50 mg/kg p.o. Bioavailability 84.7 %
Mice 2 mg/kg i.v. Plasma Concentration 4642 ng/mL
Rat 2 mg/kg i.v. Clearance (CL) 0.354 L/h/kg
Rat 30 mg/kg i.g. AUC 11,273.22±703.84 ng/L.h
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
Dog 12.5 mg/kg p.o. Bioavailability 83.1 %
Rat 10 mg/kg i.p. MRT 1.71 hr
Mice 300 mg/kg p.o. Bioavailability 5.06 %
Rat 10 mg/kg p.o. Clearance (CL) 2.5 L/h/kg SD Rats
Rat 10 mg/kg p.o. Tmax 1.50 hr
Mice 1 mg/kg i.v. Plasma Concentration 898.0 ng/mL
Dog 50 mg/kg p.o. Bioavailability 84.7 %
Rat 20 mg/kg 0.25, 0.5, 1, 2, 4, 8, 12, 24 p.o. Tmax 1.4 hr
Rat 1 mg/kg i.v. Clearance (CL) 99.79 mL/min/kg
Rat 20 mg/kg p.o. Bioavailability 0.65 %
Mice 10 mg/kg p.o. MRT 2.0 hr
Rat 10 mg/kg i.p. Clearance (CL) 0.83 L/h/kg
Rat 5 mg/kg p.o. Bioavailability 73.2 %
Rat 20 mg/kg i.g. Bioavailability 10.26 %
Rat 10 mg/kg p.o. Bioavailability 0.62 %
Rat 2 mg/kg i.v. Tmax 0.083 hr
Mice 10 mg/kg p.o. Bioavailability 62.80 %
Mice 30 mg/kg p.o. T1/2 1.00 hr
Mice 1 mg/kg i.v. Vd 0.66 L/kg
Rat 20 mg/kg p.o. MRT 4.42 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
Mice 10 mg/kg i.g. Plasma Concentration 159 ng/mL
Rat 2 mg/kg i.v. MRT 1.66 hr
Mice 30 mg/kg i.p. MRT 3.15 hr
Mice 30 mg/kg i.v. T1/2 1.97 hr
Rat 10 mg/kg i.g. Vd 8.29 L/kg
Rat 2 mg/kg i.v. Bioavailability 26.7 % SD Rats
Mice 2 mg/kg i.v. AUC 7631 ng·h/mL
Rat 0.4 mg/kg i.v. Bioavailability 76 %
Mice 100 mg/kg p.o. AUC 0.11 ng·h/mL
Rat 20 mg/kg p.o. Tmax 3.71 hr
Mice 1 mg/kg i.v. Clearance (CL) 91 mL/min/kg
Rat 1 mg/kg i.v. Clearance (CL) 20 mL/min/kg
Rat 3 mg/kg 24 h p.o. MRT 8.78 hr
Rat 1 mg/kg 24 h i.v. Bioavailability 100 %
Mice 1 mg/kg i.v. Tmax 0.1 hr
Rat 10 mg/kg i.g. AUC 3202.48±80.91 ng/L.h
Pig 10 mg/kg p.o. Plasma Concentration 2.13 ng/mL
Rat 5 mg/kg 0.25, 0.5, 1, 2, 4, 8 and 24 h p.o. Clearance (CL) 65.85 mL/min/kg
Mice 5 mg/kg p.o. Vd 1.12 L/kg
Rat 0.8 mg/kg p.o. Bioavailability 80 %
Mice 10 mg/kg p.o. Bioavailability 33.4%
Mice 1 mg/kg i.v. Clearance (CL) 1.99 mL/min/kg
Rat 1 mg/kg i.v. Vd 0.2 L/kg
Mice 1.6 mg/kg i.v. Tmax 0.0833 hr
Mice 30 mg/kg i.p. MRT 5.34 hr
Mice 5 mg/kg p.o. Clearance (CL) 2.27 mL/min/kg
Rat 10 mg/kg i.g. Bioavailability 9.34±0.07 %
Rat 20 mg/kg p.o. Clearance (CL) 429.44 L/h/kg
Rat 20 mg/kg p.o. MRT 27.77 hr
Rat 1 mg/kg i.v. Bioavailability - %
Mice 30 mg/kg p.o. Tmax 0.100 hr
Rat 2 mg/kg i.v. Clearance (CL) 6.80 L/h/kg
Mice 100 mg/kg p.o. MRT 7.30 hr
Pig 10 mg/kg p.o. Tmax 3.07 hr
Rat 30 mg/kg i.g. Bioavailability 10.47±0.10 %
Rat 10 mg/kg i.g. AUC 1.442 μg·h/mL
Mice 30 mg/kg i.v. Tmax 0.083 hr
Rat 2 mg/kg i.v. MRT 190.8 hr
Rat 3 mg/kg 24 h p.o. Clearance (CL) 0.018993 mg·h/L
Mice 10 mg/kg p.o. Bioavailability 45 %
Mice 1 mg/kg i.v. MRT 2.32 hr
Mice 1 mg/kg i.v. MRT 0.66 hr
Mice 30 mg/kg p.o. Brain-to-Plasma Ratio 0.52 (4h) %
Rat 20 mg/kg p.o. Clearance (CL) 123.87 L/h/kg
Rat 3 mg/kg 24 h p.o. Bioavailability 34.4 %
Mice 5 mg/kg p.o. MRT 5.58 hr
Mice 30 mg/kg i.v. Brain-to-Plasma Ratio 0.23 (4h) %
Rat 2 mg/kg i.v. Vz 38.01 L/kg
Mice 1 mg/kg i.v. Vd 0.0036 L/kg
Rat 20 mg/kg p.o. Vz 4480.43 L/kg
Rat 10 mg/kg i.g. AUC 1.449 μg·h/mL
Pig 10 mg/kg p.o. MRT 6.53 hr
Rat 2 mg/kg i.v. Clearance (CL) 19.56 L/h/kg
Mice 30 mg/kg i.v. Brain-to-Plasma Ratio 0.56 (2h) %
Mice 5 mg/kg p.o. Bioavailability 87.6 %
Rat 20 mg/kg p.o. Plasma Concentration 8.37 ng/mL
Rat 10 mg/kg i.g. Bioavailability 26.3 %
Rat 2 mg/kg i.v. Bioavailability 27.38 %
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
Mice 30 mg/kg i.v. Vz 10.74 L/kg
Mice 30 mg/kg p.o. Bioavailability 49 %
Rat 20 mg/kg p.o. Bioavailability 2.15 %
Rat 20 mg/kg i.v. T1/2 0.65 hr pure
Mice 30 mg/kg p.o. Vz 10.96 L/kg
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

JT002 (30 mg/kg; oral gavage; once daily; 30 days) in the Nlrp3A350V/+CreT knock-in mice (mimicking human Muckle-Wells syndrome) prevents body weight loss, reduces liver inflammation and fibrosis, decreases liver alanine aminotransferase levels, and normalizes circulating white blood cell and neutrophil counts[1].
JT002 (2.5-25 mg/kg; oral gavage; once daily; from Day 23-29) in ovalbumin (OVA)-sensitized, OVA-challenged, and induced regulatory T cell (iTreg)-transferred CD8a-/- mice (mimicking IL-17-dependent neutrophilic asthma). The 25 mg/kg dose of JT002 significantly reduces airway hyperresponsiveness and airway neutrophilia, decreases submucosal inflammatory cell infiltration, reduces the concentrations of IL-6 and IL-17 in bronchoalveolar lavage fluid, and increases the INFγ concentration. The 2.5 mg/kg dose of JT002 has no significant effect[1].
JT002 (2.5 mg/kg and 25 mg/kg; oral gavage; once daily; 4 days) in female C57BL6/J mice (a model of ozone - induced neutrophilic asthma). The 25 mg/kg dose of JT002 prevents ozone-induced airway hyperresponsiveness, significantly reduces the number of neutrophils in bronchoalveolar lavage fluid, and reduces airway epithelial desquamation. The 2.5 mg/kg dose of JT002 has no significant effect[1].

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

Animal Model: Nlrp3A350V/+CreT knock-in mice (male and female, 6-8 weeks ol)[1].
Dosage: 30 mg/kg
Administration: Oral gavage, once daily, for 30 days starting on Day 1
Result: Prevented body weight loss.
Significantly reduced the liver weight as a percentage of body weight.
Serum levels of alanine aminotransferase were decreased.
Hepatic expression of pro-inflammatory and profibrotic genes was downregulated.
Animal Model: CD8a-/- C57BL6/j female mice (6-8 weeks old). The mice were sensitized by intraperitoneal injection of 20 μg OVA emulsified in 2.25 mg alum hydroxide on Days 0 and 14, and then received aerosol challenges with 1% OVA in PBS for 20 min each day on three consecutive days (Days 26-28)[1].
Dosage: 2.5 mg/kg and 25 mg/kg
Administration: Oral gavage, once daily, from Day 23-29
Result: The high dose significantly decreased airway hyperresponsiveness and airway neutrophilia, visibly decreased submucosal inflammatory cell infiltration, decreased the concentrations of BAL IL-6 and IL-17, and increased BAL INFγ concentrations.
Animal Model: Female C57BL6/J mice (8-12 weeks old). Mice were exposed to 1.0 ppm of O3 for 3 h[1].
Dosage: 2.5 mg/kg and 25 mg/kg
Administration: Oral gavage, once daily, for 4 days
Result: The high dose prevented ozone-induced airway hyperresponsiveness, significantly reduced BAL fluid neutrophil numbers, and visibly reduced the appearance of epithelial cells in the airway lumen
Clinical Trial
Molecular Weight

432.49

Formula

C20H24N4O5S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(NS(=O)(C1=C(OC[C@@H](OC)C2)N2N=C1)=O)NC3=C(CCC4)C4=CC5=C3CCC5
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 (231.22 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 2.3122 mL 11.5610 mL 23.1219 mL
5 mM 0.4624 mL 2.3122 mL 4.6244 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
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Concentration
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Volume
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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    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (5.78 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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
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 2.3122 mL 11.5610 mL 23.1219 mL 57.8048 mL
5 mM 0.4624 mL 2.3122 mL 4.6244 mL 11.5610 mL
10 mM 0.2312 mL 1.1561 mL 2.3122 mL 5.7805 mL
15 mM 0.1541 mL 0.7707 mL 1.5415 mL 3.8537 mL
20 mM 0.1156 mL 0.5780 mL 1.1561 mL 2.8902 mL
25 mM 0.0925 mL 0.4624 mL 0.9249 mL 2.3122 mL
30 mM 0.0771 mL 0.3854 mL 0.7707 mL 1.9268 mL
40 mM 0.0578 mL 0.2890 mL 0.5780 mL 1.4451 mL
50 mM 0.0462 mL 0.2312 mL 0.4624 mL 1.1561 mL
60 mM 0.0385 mL 0.1927 mL 0.3854 mL 0.9634 mL
80 mM 0.0289 mL 0.1445 mL 0.2890 mL 0.7226 mL
100 mM 0.0231 mL 0.1156 mL 0.2312 mL 0.5780 mL
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JT002 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:

JT0022238820-43-2JT 002JT-002NOD-like Receptor (NLR)Pyroptosisinflammationairway hyperresponsivenessneutrophiliaIL-1βIL-1αIL-18NLRP3 inflammasomeInhibitorinhibitorinhibit

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