YXX0248
YXX0248 is an orally active anti-hypoxic agent. YXX0248 upregulates mRNA expression of FGF21 and GDF15 via activation of the ISR/ATF4 transcriptional axis. YXX0248 exhibits low cytotoxicity. YXX0248 enhances hypoxic survival in mice. YXX0248 can be used for the research of acute mountain sickness and hypoxia-related diseases.
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- 화학식: C13H13N3S
- 분자량:243.33
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
제품 설명
IC50 & Target
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GDF15 |
In Vitro
YXX0248 (10 μM;) upregulates FGF21 and GDF15 mRNA expression in primary hepatocytes, with EC50 values of 8.082 μM and 8.338 μM, respectively[1].
YXX0248 has low in vitro cytotoxicity, with CC50 values of >160 μM in HEPG2 cells and 74.23 μM in primary hepatocytes[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
| Species | Dose | Route | Cmax | AUClast | Tmax | T1/2 | Vz/F | CL/F | MRTlast |
|---|---|---|---|---|---|---|---|---|---|
| Mice[1] | 100 mg/kg | p.o. | 1847.36 ng/mL | 1996.23 ng·h/mL | 0.25 h | 2.48 h | 172898.93 mL/kg | 48298.26 mL/h/kg | 2.56 h |
In Vivo
YXX0248 (25, 50 and 100 mg/kg; p.o.; daily for 3 days) exhibits anti-hypoxia effect in mice[1].
YXX0248 (125, 250 and 500 mg/kg; p.o.; single dose) exhibits low in vivo toxicity in mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mice[1]
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Dosage:50 and 100 mg/kg
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Administration:p.o.; sigle dose
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Result:Upregulated FGF21 and GDF15 expression at both mRNA and protein levels in mouse livers.
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Animal Model:Mice[1]
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Dosage:25, 50 and 100 mg/kg
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Administration:p.o.; daily for 3 days
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Result:Significantly prolonged the survival time of mice under hypoxic conditions.
Exhibited anti-hypoxia effect in a dose-dependent manner.
Chemical Information
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분자량 243.33
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화학식 C13H13N3S
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SMILES
S=C(NC1=NC=CC=C1)C2=NC=C(CC)C=C2
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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)