QX-31
QX-31 is an orally active selective NLRP3 inhibitor with a Kd value of 2.8 μM for hNLRP3. QX-31 inhibits PI3K/AKT and HIF-1α signaling. QX-31 shows anti-fibrotic effects in mouse models of unilateral ureteral obstruction and ischemia-reperfusion injury. QX-31 can be used for research on renal fibrosis.
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- CAS No.: 3065380-90-4
- 화학식: C24H20FN3OS
- 분자량:417.50
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocol
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
IC50 & Target
[1]|
NLRP3 2.8 μM (Kd) |
HIF-1α |
In Vitro
QX-31 selectively binds the NLRP3 LRR domain with a KD of 1.25 μM by ITC[1].
QX-31 (1-10 μM) disrupts NEK7 recruitment and ASC oligomerization in THP-M cells[1].
QX-31 (1-10 μM) inhibits COL-I expression in kidney organoids[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
| Species | Dose | Route | AUC0-t | AUC0-∞ | MRT0-t | MRT0-∞ | CLz | Vz | F | Tmax | Cmax | CLz/F | Vz/F |
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Mice[1] | 50 mg/kg | p.o. | 28,282.10 min·ng/mL | 29,231.60 min·ng/mL | 204.2 min | 226.6 min | / | / | / | 8.3 min | 157.1 ng/mL | 1,835.8 mL/min/kg | 381,065.3 mL/kg |
| Mice[1] | 1 mg/kg | i.v. | 19,763.50 min·ng/mL | 20,614.70 min·ng/mL | 64.9 min | 126.6 min | 61.2 mL/min/kg | 4,850.47 mL/kg | 2.84 % | / | / | / | / |
In Vivo
QX-31 (12.5-50 mg/kg/day; p.o. (oral gavage); daily; 28 consecutive days following the initial ischemic insult) dose-dependently attenuates renal fibrosis in the IRI mouse model, reducing tubular injury, collagen deposition, myofibroblast activation, and profibrotic/inflammatory gene expression[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J[1]
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Dosage:12.5 mg/kg/day; 25 mg/kg/day; 50 mg/kg/day
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Administration:p.o. (intragastric gavage); daily; 14 consecutive days starting day 1 postsurgery
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Result:Dose-dependently mitigated UUO-induced tubular injury and architectural damage.
It markedly reduced interstitial fibrotic burden by H&E and Masson staining and produced dose-responsive reductions in COL-I deposition and α-SMA-positive myofibroblast activation.
Suppressed FN and vimentin protein expression and downregulated proinflammatory/profibrotic genes Il6, Il1b, Tnfa, Col1a1, Col3a1, and Acta2.
QX-31 administration significantly blunted UUO-induced activation of the PI3K/AKT/HIF-1α axis and reduced protein levels of GLS1 and LDHA.
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Animal Model:C57BL/6J[1]
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Dosage:12.5 mg/kg/day; 25 mg/kg/day; 50 mg/kg/day
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Administration:p.o. (oral gavage); daily; 28 consecutive days following the initial ischemic insult
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Result:Dose-dependently ameliorated IRI-induced renal damage and structural distortion, with reduced tubular injury scores and diminished interstitial collagen deposition.
It produced dose-responsive reductions in COL-I accumulation and α-SMA myofibroblast activation.
Downregulated FN, vimentin, and α-SMA protein expression and suppressed transcription of Il6, Il1b, Tnfa, Col1a1, Col3a1, and Acta2.
In IRI kidneys, QX-31 blunted the PI3K/AKT/HIF-1α axis and reduced GLS1 and LDHA protein levels.
Chemical Information
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CAS No. 3065380-90-4
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분자량 417.50
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화학식 C24H20FN3OS
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SMILES
FC(C=C1)=CC=C1CSC2=NC3=CC=CC=C3N2CC4=CC=C(NC(C=C)=O)C=C4
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
QX-31 Related Classifications
HY-189659 Related Classifications
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Keywords
- QX-31
- 3065380-90-4
- QX31
- QX 31
- NOD-like Receptor (NLR)
- PI3K
- Akt
- HIF/HIF Prolyl-Hydroxylase
- AIM2
- ASC oligomerization
- IL-1β
- LRR domain
- NEK7
- NLRC4
- NLRP1
- NLRP3
- PI3K/AKT
- TGF-β
- collagen I
- glutaminolysis
- glycolysis
- human kidney organoids
- hypoxia-inducible factor alpha
- inflammasome
- ischemia-reperfusion injury
- mitochondrial membrane potential
- renal fibrosis
- unilateral ureteral obstruction
- Inhibitor
- inhibitor
- inhibit