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Art. -Nr.: HY-182379

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SBI-0802767

SBI-0802767 is an orally active, uncompetitive and highly selective inhibitor of protein tyrosine phosphatase (LMPTP) with an IC₅₀ of 0.239 μM. SBI-0802767 exhibits >1000-fold selectivity over other protein tyrosine phosphatases and enhances insulin signaling in hepatocytes. SBI-0802767 is used in studies of obesity-related type 2 diabetes and insulin resistance.

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CAS. Nr.: 68220-27-9
Formel: C₁₂H₉Cl₂N₅
Molecular Weight:294.14

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

SBI-0802767 Chemical Structure

CAS. Nr.: 68220-27-9

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Biologische Aktivität
- Beschreibung
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

In Vitro

SBI-0802767 (Compound 3) inhibits human LMPTP-A with an IC₅₀ of 0.239 μM and displays >1000-fold selectivity for LMPTP over other PTPs^[1].
SBI-0802767 acts as an uncompetitive inhibitor of LMPTP^[1].
SBI-0802767 shows moderate plasma protein binding and good microsomal stability in in vitro metabolic studies^[1].

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

Parmacokinetics

Species	Dose	Route	C_max	AUC	T_1/2	F	CL_plasma	V_d
Mice^[1]	2 mg/kg	i.v.	/	/	/	/	5.8 mL/min/kg	3.01 L/kg
Mice^[1]	10 mg/kg	p.o.	5018 ng/mL	18544 ng·h/mL	4.71 h	66 %	/	/

In Vivo

SBI-0802767 (Compound 3) shows good oral bioavailability (F% = 66) and favorable pharmacokinetic properties in mice^[1].

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

Chemical Information

CAS. Nr. 68220-27-9
Molecular Weight 294.14
Formel C₁₂H₉Cl₂N₅
SMILES

ClC1=CC=CC(Cl)=C1CN2C=NC(N)=C3N=CN=C32
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Stanford SM, et al. Discovery of Orally Bioavailable Purine-Based Inhibitors of the Low-Molecular-Weight Protein Tyrosine Phosphatase. J Med Chem. 2021;64(9):5645-5653. [Content Brief]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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