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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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G647232-10mg | 10mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $90.90 | |
G647232-25mg | 25mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $150.90 | |
G647232-50mg | 50mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $250.90 | |
G647232-100mg | 100mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $400.90 |
Specifications & Purity | ≥99% |
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Biochemical and Physiological Mechanisms | GNE-3511 is an orally active bioavailable and brain-penetrant dual leucine zipper kinase (DLK) inhibitor with a K i of 0.5 nM. GNE-3511 can cross the blood-brain-barrier and can be used for the research of neurodegenerative diseases. |
Storage Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Product Description | GNE-3511 is an orally active bioavailable and brain-penetrant dual leucine zipper kinase (DLK) inhibitor with a K i of 0.5 nM. GNE-3511 can cross the blood-brain-barrier and can be used for the research of neurodegenerative diseases In Vitro GNE-3511 has inhibitory activity for p-JNK and DRG with IC 50 values of 30 nM and 107 nM, respectively. GNE-3511 has kinase selectivity for MKK4, MKK7, JNK1, JNK2, JNK3, MLK1, MLK2 and MLK3 with IC 50 values of >5000 nM, >5000 nM, 129 nM, 514 nM, 364 nM, 67.8 nM, 767 nM and 602 nM, respectively. GNE-3511 displays concentration-dependent protection of neurons from degeneration in vitro. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo GNE-3511 (oral gavage; 75 mg/kg; single) suppresses CYP-induced nociceptive behavior by inhibiting DLK in mice. GNE-3511 (oral gavage; 75 mg/kg; single) suppresses CYP-induced edema and hemorrhage in mouse bladder. GNE-3511 (iv.; 1 mg/kg or po.; 5 mg/kg) exhibits moderate in vivo plasma clearances, moderate volumes of distribution, short half-lives, and brain penetration. Pharmacokinetic Parameters of GNE-3511 (iv.; 1 mg/kg or po.; 5 mg/kg). species CL p (mL/min/kg Vd ss (L/kg t 1/2 (h) F (%) B u /P u CSF/P u mouse 56 2.5 0.6 45 0.24 at 6 h rat 30 3.7 1.8 63 0.7 0.4 dog 41 6.5 4 32 0.4 cynomolgous 16 3.1 2.4 19 0.6 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Cystitis mouse model Dosage: 75 mg/kg Administration: oral gavage;75 mg/kg; single Result: Significantly reduced the number of nociceptive behavior as well as nociceptive score. Had no impact on bladder weight, did not induce bladder edema or hemorrhage and significantly suppressed CYP-induced increase in bladder weight, bladder edema, and hemorrhage. Animal Model: mouse, rat, cynomolgus and dogDosage: 1 mg/k, 5 mg/kg Administration: iv.; 1 mg/kg or po.; 5 mg/kg Result: Exhibited moderate in vivo plasma clearances, moderate volumes of distribution, short half-lives and brain penetration. Form:Solid IC50& Target:Ki: 0.5 nM (DLK),IC50: 30 nM (p-JNK), 107 nM (DRG),>5000 nM (MKK4), >5000 nM (MKK7), 129 nM (JNK1),514 nM (JNK2), 364 nM (JNK3), 67.8 nM (MLK1), 767 nM (MLK2) and 602 nM (MLK3) |
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IUPAC Name | 2-[[6-(3,3-difluoropyrrolidin-1-yl)-4-[1-(oxetan-3-yl)piperidin-4-yl]pyridin-2-yl]amino]pyridine-4-carbonitrile |
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INCHI | InChI=1S/C23H26F2N6O/c24-23(25)4-8-31(15-23)22-11-18(17-2-6-30(7-3-17)19-13-32-14-19)10-21(29-22)28-20-9-16(12-26)1-5-27-20/h1,5,9-11,17,19H,2-4,6-8,13-15H2,(H,27,28,29) |
InChi Key | RHFIAUKMKYHHFA-UHFFFAOYSA-N |
Canonical SMILES | C1CN(CCC1C2=CC(=NC(=C2)N3CCC(C3)(F)F)NC4=NC=CC(=C4)C#N)C5COC5 |
Isomeric SMILES | C1CN(CCC1C2=CC(=NC(=C2)N3CCC(C3)(F)F)NC4=NC=CC(=C4)C#N)C5COC5 |
PubChem CID | 72547959 |
Molecular Weight | 440.49 |
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Solubility | DMSO : 31.25 mg/mL (70.94 mM; Need ultrasonic) |
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