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Zamicastat

Names

[ CAS No. ]:
1080028-80-3

[ Name ]:
Zamicastat

[Synonym ]:
Zamitat
UNII-YLU32D0DNV

Biological Activity

[Description]:

Zamicastat is a concentration-dependent dual P-gp and BCRP inhibitor with IC50 values of 73.8±7.2 μM and 17.0±2.7 μM, respectively.

[Related Catalog]:

Signaling Pathways >> Membrane Transporter/Ion Channel >> BCRP
Signaling Pathways >> Membrane Transporter/Ion Channel >> P-glycoprotein
Research Areas >> Cancer

[Target]

IC50: 73.8±7.2 μM (P-gp), 17.0±2.7 μM (BCRP)[1]


[In Vitro]

Zamicastat is a concentration-dependent dual P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP) inhibitor with IC50 values of 73.8±7.2 μM and 17.0±2.7 μM. Zamicastat also reversibly inhibits dopamine β-hydroxylase (DBH) without effect in brain tissue[1].

[References]

[1]. Bicker J, et al. In vitro assessment of the interactions of dopamine β-hydroxylase inhibitors with human P-glycoprotein and Breast Cancer Resistance Protein. Eur J Pharm Sci. 2018 May 30;117:35-40.


[Related Small Molecules]

Ko 143 | elacridar | Valspodar | Tariquidar | Zosuquidar trihydrochloride | Risperidone | Sinapine thiocyanate | Fumitremorgin C | Piperine | HM30181 | (20S)-Protopanaxdiol | Dofequidar (fumarate) | KS 176 | YHO-13177 | NSC23925

Chemical & Physical Properties

[ Molecular Formula ]:
C21H21F2N3OS

[ Molecular Weight ]:
401.47300

[ Exact Mass ]:
401.13700

[ PSA ]:
77.88000

[ LogP ]:
4.34940

[ Storage condition ]:
2-8℃

Related Compounds

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