LASSBio-1829 hydrochloride
LASSBio-1829 hydrochloride is an orally active IKK2 inhibitor with an IC50 of 3.8 μM against the human target (Sf21 cells). LASSBio-1829 hydrochloride blocks signal transduction of the inflammation-associated NF-κB activation pathway. LASSBio-1829 hydrochloride reduces leukocyte migration, TNF-α biosynthesis, ROS production and NO production. LASSBio-1829 hydrochloride exhibits anti-inflammatory activity in a carrageenan-induced subcutaneous air pouch mouse model. LASSBio-1829 hydrochloride alleviates licking behavior during the inflammatory phase of the mouse formalin test. LASSBio-1829 hydrochloride can be used in inflammation-related research.
For research use only. We do not sell to patients.
- CAS No.: 1807810-16-7
- Formula: C25H19ClN4O
- Molecular Weight:426.90
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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IKK2 |
TNF-α |
LASSBio-1829 hydrochloride potently inhibits the human recombinant IKK2 enzyme expressed in Sf21 cells, with an IC50 value of 3.8 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
LASSBio-1829 (30 µM/kg; p.o.; single administration) hydrochloride alleviates inflammatory pain in mice in the formalin test, but shows no activity during the neuropathic pain phase[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Swiss Webster (female, 20-25 g)[1]
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Dosage:10 µM/kg; 30 µM/kg; 100 µM/kg
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Administration:p.o.; single dose
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Result:Reduced leukocyte migration to the air pouch by 29% at 30 µmol/kg and 35% at 100 µmol/kg.
Inhibited TNF-α production in exudate by 46% at 30 µmol/kg.
Significantly reduced nitric oxide (NO) production in exudate at 10 µmol/kg; higher doses did not show this effect.
Significantly reduced reactive oxygen species (ROS) production in leukocytes stimulated with phorbol myristate acetate (PMA) at 10 and 30 µmol/kg, with a dose-dependent response.
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Animal Model:Swiss Webster (female, 20-25 g)[1]
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Dosage:30 µM/kg
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Administration:p.o.; single dose
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Result:Showed no significant effect during the neurogenic first phase of the formalin-induced licking response model.
Significantly reduced paw licking time relative to vehicle controls during the inflammatory second phase.
Chemical Information
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CAS No. 1807810-16-7
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Molecular Weight 426.90
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Formula C25H19ClN4O
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SMILES
O=C(C1=CC2=C(C=CC=C2)C=C1)N/N=C/C3=CC=C(C=C3)C4=C5C(NC=C5)=NC=C4.Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
LASSBio-1829 hydrochloride Related Classifications
HY-118973 Related Classifications
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