1. Metabolic Enzyme/Protease
  2. Phosphatase
  3. PTP1B-IN-3 diammonium

PTP1B-IN-3 diammonium 

Cat. No.: HY-15133A
Handling Instructions

PTP1B-IN-3 diammonium is a potent and orally active PTP1B inhibitor with IC50s of 120 nM for both PTP1B and TCPTP. PTP1B-IN-3 diammonium has antidiabetic and anticancer effects.

For research use only. We do not sell to patients.

PTP1B-IN-3 diammonium Chemical Structure

PTP1B-IN-3 diammonium Chemical Structure

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Description

PTP1B-IN-3 diammonium is a potent and orally active PTP1B inhibitor with IC50s of 120 nM for both PTP1B and TCPTP. PTP1B-IN-3 diammonium has antidiabetic and anticancer effects[1][2].

IC50 & Target

IC50: 120 nM (PTP1B), 120 nM (TCPTP)[2]

In Vivo

In diet-induced obese (DIO) mice, PTP1B-IN-3 (compounds 3g) exhibits dose dependent inhibition (60%, 80% and 100% inhibition at 1, 3 and 10 mg/kg, respectively) of glucose excursion when given orally 2 h before oral glucose challenge with an estimated ED50 of 0.8 mg/kg[1].
In the NDL2 Ptpn1 transgenic mice, PTP1B-IN-3 (compounds 3g; orally; 30 mg/kg for 21 days) shows a significant delay in the onset of tumor development in NDL2 Ptpn1+/+ mice, extending the median tumor free days (T50) from 28 days to 75 days[1].
In diet-induced obese (DIO) mice, PTP1B-IN-3 (compounds 3g) exhibits good oral bioavailability (F of 24%), slow clearance (CL of 0.71 mL/kg/min), and good elimination half live (t1/2 of 6 h). The oral bioavailability in higher species such as rats (F of 4%) and squirrel monkeys (F of 2%) are substantially lower but excellent exposures are achieved with oral dosing[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

396.12

Formula

C₁₂H₁₃BrF₂N₃O₃P

SMILES

BrC1=C(C(F)(P(O)(O)=O)F)C=C2C(C=CC(C#N)=C2)=C1.N.N

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

References
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Keywords:

PTP1B-IN-3 diammoniumPhosphatasePTP1BTCPTPantidiabeticanticancerInhibitorinhibitorinhibit

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Product Name:
PTP1B-IN-3 diammonium
Cat. No.:
HY-15133A
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