GIBH-130

SKU: orb1226675

Description

A novel inhibitor of neuroinflammation, suppresses the proinflammatory cytokine production in LPS-stimulated N9 microglial cells (IC50=3.4 nM); modulates the release of detrimental proinflammatory cytokines; exhibits in vivo efficacy of cognitive impairment in both β amyloid-induced and APP/PS1 double transgenic Alzheimer's murine models.Alzheimer's Disease Phase 1 Clinical.

Images & Validation

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Key Properties

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CAS Number	1252608-59-5
MW	360.421
Purity	>98% (HPLC)
Formula	C₂₀H₂₀N₆O
SMILES	O=C(C1=NN=C(C2=CC=CC=C2)C=C1C)N3CCN(C4=NC=CC=N4)CC3
Target	IL-1β
Solubility	< 1 mg/ml refers to the product slightly soluble or insoluble

Bioactivity

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In Vivo

GIBH-130 exhibits comparable In vivo efficacy of cognitive impairment relief to donepezil and memantine respectively in both β amyloid-induced and APP/PS1 double transgenic Alzheimer’s murine models at a substantially lower dose (0.25 mg/kg). The pharmacokinetic properties of GIBH-130 are assessed in Sprague-Dawley rats. As a potential drug candidate targeting in CNS, GIBH-130 is found to be orally bioavailable in rats, with 74.91% bioavailability and 4.32 h half-life. In addition, GIBH-130 displays good penetration ability across blood-brain barrier (AUCBrain/Plasma = 0.21).

In Vitro

GIBH-130 is a novel antineuroinflammatory agent that is identified through microglia-based phenotypic screenings. GIBH-130 (IC50 3.4 nM) is identified in screenings as one of the most effective inhibitors with an acceptable half-life. Pretreatment of microglia with GIBH-130 significantly reduces the production of these factors in response to Lipopolysaccharides (LPS) stimulation, and the extent of the reduction is dependent on the concentrations of GIBH-130. The IC50 values of GIBH-130 for NO and TNF-α inhibition are 46.24 and 40.82 μM, respectively. Notably, pretreatment with GIBH-130 significantly suppresses the IL-1β secretion by activated microglia (IC50 = 3.4 nM). The inhibitory efficiency of GIBH-130 at 20 nM is comparable to 20 μM minocycline against IL-1β release. IL-1β is one of the major cytokines during neuroinflammatory progression of AD. So, it is meaningful to explain the selectivity of GIBH-130 against IL-1β (IC50 value 3.4 nM) over NO and TNF-α (IC50 value 46.24 and 40.82 μM, respectively).

Storage & Handling

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Storage	Storage temperature: -20°C. Stability: ≥ 2 years
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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GIBH 130 | GIBH130

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IL-1β

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GIBH-130 (orb1226675)

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Purity:	99.86%
CAS Number:	1252608-59-5
MW:	360.41
Formula:	C₂₀H₂₀N₆O

GIBH-130

Description

Images & Validation

Key Properties

Bioactivity

Storage & Handling

Alternative Names

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