PTP1B-IN-35
PTP1B-IN-35 is an orally active protein tyrosine phosphatase 1B (PTP1B) inhibitor, with an IC50 of 32.7 μM, a Kis of 18.8 μM, a Kii of 45.3 μM, and a Kd of 36 μM against human PTP1B. PTP1B-IN-35 promotes glucose uptake, improves glucose tolerance, enhances insulin sensitivity, and reduces blood glucose levels. PTP1B-IN-35 can be used in the research of type 2 diabetes.
For research use only. We do not sell to patients.
- Formula: C33H46FNO5
- Molecular Weight:555.72
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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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PTP1B 32.7 μM (IC50) |
PTP1B 36 μM (Kd) |
PTP1B-IN-35 (Compound 6h) (32-100 μM) potently and selectively inhibits purified PTP1B, with an IC50 of 32.7 μM and a selectivity index of 7.0 against TCPTP[1].
PTP1B-IN-35 (30-60 μM) acts as a reversible mixed-type inhibitor of purified PTP1B, with a Kis of 18.8 μM and a Kii of 45.3 μM[1].
PTP1B-IN-35 (10 min) binds to purified PTP1B with a Kd value of 36.0 μM, and induces the thermal stability of this enzyme[1].
PTP1B-IN-35 (2.6-10.4 μM; 5-10 min) reduces the surface hydrophobicity of purified PTP1B in a dose-dependent manner, with a maximum decrease of 53.4% in ANS fluorescence observed at 10.4 μM[1].
PTP1B-IN-35 (18.12-36.1 μM) alters the secondary structure of purified PTP1B, reducing the α-helix content and increasing the β-sheet content at the highest concentration of 36.1 μM[1].
PTP1B-IN-35 (20 μM) significantly enhances glucose uptake capacity in insulin-resistant HepG2 cells without cytotoxicity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Kunming (KM)[1]
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Dosage:25 mg/kg; 50 mg/kg; 100 mg/kg
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Administration:p.o.; single dose
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Result:Reduced the blood glucose area under the curve (AUC) by 10.6% at 50 mg/kg relative to the model group.
Reduced the blood glucose AUC by 21.6% at 100 mg/kg relative to the model group.
Significantly lowered blood glucose levels at individual time points at 50 mg/kg and 100 mg/kg relative to the model group.
Reduced the blood glucose area under the curve (AUC) by 7.2% at 50 mg/kg relative to the model group.
Reduced the blood glucose AUC by 18.1% at 100 mg/kg relative to the model group.
Significantly lowered blood glucose levels at each time point at 50 mg/kg and 100 mg/kg relative to the model group. Reduced the blood glucose area under the curve (AUC) by 14.7% at 50 mg/kg relative to the model group.
Reduced the blood glucose AUC by 16.5% at 100 mg/kg relative to the model group.
Chemical Information
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Molecular Weight 555.72
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Formula C33H46FNO5
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SMILES
O=C(O)[C@@H](NC(CC[C@H]([C@@]1([H])CC[C@@]2([H])[C@]3([H])C(C[C@]4([H])C[C@H](O)CC[C@]4(C)[C@@]3([H])CC[C@]12C)=O)C)=O)CC5=CC=C(F)C=C5
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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)
PTP1B-IN-35 Related Classifications
HY-184743 Related Classifications
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