2. Metabolic Enzyme/Protease Membrane Transporter/Ion Channel
  3. Creatine Kinase Amino acid Transporter
  4. 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.

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

INSP-0154

INSP-0154 Chemical Structure

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INSP-0154 Related Antibodies

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Description

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[1].

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.

INSP-0154 Related Antibodies
Parmacokinetics
Species Dose Route Cmax Tmax AUClast T1/2 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.
Molecular Weight

170.17

Formula

C6H10N4O2
SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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INSP-0154 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

INSP-0154INSP0154INSP 0154Creatine KinaseAmino acid TransporterCK氨基酸转运蛋白creatineC57BL/6 micecancerC144HCT-116 cellsGAT-3TAUTBGT-1GAT-2SLC6A8Inhibitorinhibitorinhibit

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