Zamicastat|BIA 5-1058|CAS 1080028-80-3|DC Chemicals

Cas No.:	1080028-80-3
SMILES:	C1C2C=C(F)C=C(F)C=2OC[C@@H]1N1C(=S)NC=C1CCNCC1C=CC=CC=1
Formula:	C₂₁H₂₁F₂N₃Os
M.Wt:	401.473
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

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.
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.

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