GLyT2-IN-3
GLyT2-IN-3 is a potent GlyT2 inhibitor with a KD of 23.7 nM. GLyT2-IN-3 inhibits GlyT2-mediated glycine uptake with an IC50 of 19.4 nM. GLyT2-IN-3 shows broad-spectrum antinociceptive effects in three pain models, does not induce sedative effects or motor coordination impairment in mice, and exhibits favorable pharmacokinetic properties in rats with an oral bioavailability of 88.57%, GLyT2-IN-3 can be used for the study of neuropathic pain.
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- CAS. Nr.: 2789716-24-9
- Formel: C23H31N3O4
- Molecular Weight:413.51
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Chemical Information
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Biologische Aktivität
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GlyT2 23.7 nM (Kd) |
GLyT2-IN-3 (compound 14) binds to GlyT2 with a KD of 23.7 nM, a ka of 13.5 × 103 M-1s-1 and a kd of 3.20 × 10-4 s-1[1].
GLyT2-IN-3 shows a distinct binding pose in the GlyT1 pocket compared to the selective GlyT1 inhibitor SSR504734 (HY-10715) in molecular docking[1].
GLyT2-IN-3 (0-10000 nM; 30 min preincubation; 30 min uptake) inhibits GlyT2-mediated 3H-glycine uptake in HEK293 cells stably expressing human GlyT2 with an IC50 of 19.4 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
GLyT2-IN-3 (10, 20, 30 mg/kg; s.c.; single dose) in Paclitaxel (HY-B0015)-induced neuropathic pain ICR mice dose-dependently reverses mechanical allodynia, with an ED50 of 12.17 mg/kg[1].
GLyT2-IN-3 (25 mg/kg; s.c.; single dose) in ICR mice produces a 61% inhibition rate in the acetic acid-induced writhing test[1].
GLyT2-IN-3 (36 mg/kg; s.c.; single dose, three times the ED50 in the paclitaxel-induced CIPN model) does not change locomotor activity in the open-field test compared with the vehicle control, and fails to affect the rotarod fall latency at 30, 60, 90 and 120 min post-administration in ICR mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Formalin test (Phase II) in ICR mice (20-32 g, both sexes)[1]
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Dosage:12.5, 25, 50 mg/kg
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Administration:s.c.; single dose
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Result:Showed an ED50 of 30.5 mg/kg.
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Animal Model:Acetic acid-induced abdominal constriction test in ICR mice (20-32 g, both sexes)[1]
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Dosage:12.5, 25, 50 mg/kg
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Administration:s.c.; single dose
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Result:Showed an ED50 of 26.0 mg/kg.
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Animal Model:Paclitaxel-induced CIPN model in ICR mice (20-32 g, both sexes)[1]
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Dosage:10, 20, 30 mg/kg
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Administration:s.c.; single dose
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Result:Reversed mechanical allodynia with an ED50 of 12.17 mg/kg.
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Animal Model:Strychnine reversal experiment in ICR mice (20-32 g, both sexes)[1]
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Dosage:25 mg/kg
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Administration:s.c.; single dose
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Result:Produced 61% inhibition rate.
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Animal Model:Open-field test in ICR mice (20-32 g, both sexes)[1]
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Dosage:36 mg/kg
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Administration:s.c.; single dose
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Result:Showed no significant alteration in locomotor activity.
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Animal Model:Rotarod test in ICR mice (20-32 g, both sexes)[1]
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Dosage:36 mg/kg
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Administration:s.c.; single dose
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Result:Showed no significant effect on latency to fall.
Chemical Information
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CAS. Nr. 2789716-24-9
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Molecular Weight 413.51
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Formel C23H31N3O4
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SMILES
O=C(NC1CCN(C2=CC=NC=C2)CC1)C3=CC(OC)=C(OCCCC)C(OC)=C3
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
GLyT2-IN-3 Related Classifications
HY-184901 Related Classifications
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