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Art. -Nr.: HY-181753

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INSP-0154

INSP-0154 is a potent creatine kinase B (CKB)/creatine transporter (SLC6A8) inhibitor. INSP-0154 binds to the SLC6A8 occluded pocket, prevents creatine transport into cells, and protects SLC6A8 cysteine residue C144 from irreversible inactivation. INSP-0154 inhibits creatine uptake in mouse heart tissue. INSP-0154 can be used for the research of cancer.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Formel: C₆H₁₀N₄O₂
Molecular Weight:170.17

Speicherung:

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

Data Sheet (272 KB)

INSP-0154 Chemical Structure

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Preis

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

^[1]

SLC6A8

In Vitro

INSP-0154 (Compound 46) (0.46-1000 μM; 1 h) potently inhibits SLC6A8-mediated creatine uptake in HCT-116 cells with an IC₅₀ of 8.2 μM^[1].
INSP-0154 (0.46-1000 μM) inhibits GAT-2, GAT-3, BGT-1, and TAUT-mediated creatine uptake with IC₅₀ of 22.7, 150, 116 and 11.9 μM, while showing no activity against GAT-1 at concentrations up to 1000 μM^[1].
INSP-0154 shows strong in vitro plasma and metabolic stability, low Caco-2 permeability, and is not a P-gp efflux substrate^[1].

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

Parmacokinetics

Species	Dose	Route	C_max	T_max	AUC_last	T_1/2	F	C₀
Mice^[1]	3 mg/kg	i.v.	/	/	2151 ng·h/mL	0.9 h	/	7698 ng/mL
Mice^[1]	100 mg/kg	p.o.	13517 ng/mL	0.5 h	30616 ng·h/mL	2.7 h	42.7 %	/
Mice^[1]	100 mg/kg	i.p.	42700 ng/mL	0.5 h	27742 ng·h/mL	3.3 h	59.6 %	/

In Vivo

INSP-0154 (Compound 46) (100 mg/kg; i.p.; single dose) inhibits creatine transport in mouse heart tissue^[1].

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

Animal Model:

C57BL/6 (male, 6−9 weeks old)^[1]
Dosage:

100 mg/kg
Administration:

i.p.; single dose
Result:

Achieved inhibition of creatine-d₃ uptake in heart tissue, with greater potency than β-GPA under the tested conditions.

Chemical Information

Molecular Weight 170.17
Formel C₆H₁₀N₄O₂
SMILES

[H][C@]12CN(C[C@]1(C(NO2)=O)[H])C(N)=N
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

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (272 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Martinez EJ, et al. Carboxylic Acid Bioisosteres of Creatine as Novel and Selective Substrate Competitive Inhibitors of the Creatine Transporter SLC6A8. J Med Chem. 2026;69(4):3915-3931. [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.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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