1H-Pyrazol-5-ol, 3-phenyl-4-propyl-1-(2-pyridinyl)-

1H-Pyrazol-5-ol, 3-phenyl-4-propyl-1-(2-pyridinyl)-

3-Phenyl-4-propyl-1-(pyridin-2-yl)-1H-pyrazol-5-ol

CAS: 1270084-92-8

Molecular Formula: C17H17N3O

1H-Pyrazol-5-ol, 3-phenyl-4-propyl-1-(2-pyridinyl)- - Names and Identifiers

Name	3-Phenyl-4-propyl-1-(pyridin-2-yl)-1H-pyrazol-5-ol
Synonyms	APX-115 freebase Ewha-18278 free base 3-Phenyl-4-propyl-1-(pyridin-2-yl)-1H-pyrazol-5-ol 1H-Pyrazol-5-ol, 3-phenyl-4-propyl-1-(2-pyridinyl)-
CAS	1270084-92-8

1H-Pyrazol-5-ol, 3-phenyl-4-propyl-1-(2-pyridinyl)- - Physico-chemical Properties

Molecular Formula	C17H17N3O
Molar Mass	279.34
Density	1.17±0.1 g/cm3(Predicted)
Boling Point	493.3±45.0 °C(Predicted)
pKa	7?+-.0.50(Predicted)
Storage Condition	2-8°C
In vitro study	APX-115 free base (5 μm; 60 μm min) almost completely inhibited the expression of pro-inflammatory and fibrotic molecules in the mouse podocyte cell line induced by high glucose. In the kidney, APX-115 free base reduces Nox gene up-regulation and protein expression while improving inflammatory and fibrotic processes.
In vivo study	APX-115 free base (oral gavage; 60 μg/kg/day; For 12 consecutive weeks) can significantly improve insulin resistance in diabetic mice. Treatment with APX-115 free base reduced urinary protein excretion and plasma creatinine levels. Animal Model: Six-week-old male diabetic db/db mice (C57BLKS/J- lepr db /lepr db ) Dosage: 60 mg/kg Administration: Oral gavage; per day; for 12 weeks Result: Significantly improved insulin resistance in diabetic mice.

1H-Pyrazol-5-ol, 3-phenyl-4-propyl-1-(2-pyridinyl)- - Reference Information

biological activity	APX-115 free base (Ewha-18278 free base) is an effective and orally active inhibitor of pan NADPH oxidase (pan-Nox). the Ki values for nox1, nox2 and nox4 are 1.08 μM, 0.57 μM and 0.63 μM respectively. APX-115 free base (Ewha-18278 free base) can significantly inhibit MCP-1/CCL2, IL-6 and TNFα in diabetic kidney.
target	TargetValue MCP-1/CCL2 () IL-6 () TNFα () NOX2 (Cell-free say) 0.57 μM(Ki) NOX4 (Cell-free say) 0.63 μM(Ki)
Target	Value
MCP-1/CCL2 ()
IL-6 ()
TNFα ()
NOX2 (Cell-free assay)	0.57 μM(Ki)
NOX4 (Cell-free assay)	0.63 μM(Ki)
in vitro study	APX-115 free base (5 μM; 60 min) almost completely inhibited the expression of pro-inflammatory and fibrotic molecules in mouse podocyte cell lines induced by high glucose. In the kidney, APX-115 free base attenuates Nox gene up-regulation and protein expression while improving inflammatory and fibrotic processes.
in vivo studies	APX-115 free base (oral gavage; 60 mg/kg/day; 12 weeks) significantly improved insulin resistance in diabetic mice. APX-115 free base treatment decreased urinary protein excretion and plasma creatinine levels. Animal Model: Six-week-old male diabetic db/db mice (C57BLKS/J- lepr db /lepr db ) Dosage: 60 mg/kg Administration: Oral gavage; per day; for 12 weeks Result: Significantly improved insulin resistance in diabetic mice.
Animal Model:	Six-week-old male diabetic db/db mice (C57BLKS/J- lepr db /lepr db )
Dosage:	60 mg/kg
Administration:	Oral gavage; per day; for 12 weeks
Result:	Significantly improved insulin resistance in diabetic mice.

Last Update：2024-04-09 20:52:54

1H-Pyrazol-5-ol, 3-phenyl-4-propyl-1-(2-pyridinyl)-

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1H-Pyrazol-5-ol, 3-phenyl-4-propyl-1-(2-pyridinyl)-

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