Zamicastat

Product Name: Zamicastat
CAS No.: 1080028-80-3
Chemical Name: Zamicastat
Synonyms: BIA 5-1058;Zamicastat;Zamicastat USP/EP/BP;Zamicastat (BIA 5-1058);Zamicastat, 10 mM in DMSO;1-[6-[[(1S,3S)-3-aminocyclopentyl]amino]-3-pyridyl]pyridin-2-one dihydrochloride;2H-Imidazole-2-thione, 1-[(3R)-6,8-difluoro-3,4-dihydro-2H-1-benzopyran-3-yl]-1,3-dihydro-5-[2-[(phenylmethyl)amino]ethyl]-;ABCB1,Dopamine β-monooxygenase,Inhibitor,Cluster of differentiation 243,ABCG2,inhibit,P-glycoprotein,Multidrug resistance protein 1,BCRP,MDR1,CD243,Breast cancer resistance protein,P-gp,Pgp,Zamicastat,Dopamine β-hydroxylase,Dopamine beta-hydroxylase,Dopamine beta-monooxygenase
CBNumber: CB03168664
Molecular Formula: C21H21F2N3OS
Formula Weight: 401.47
MOL File: 1080028-80-3.mol

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Zamicastat Property

Boiling point:: 525.8±60.0 °C(Predicted)
Density: 1.36±0.1 g/cm3(Predicted)
storage temp.: Store at -20°C
solubility: DMSO : 150 mg/mL (373.63 mM);Water : < 0.1 mg/mL (insoluble)
form: Solid
pka: 11.74±0.70(Predicted)
color: White to yellow
InChIKey: ZSSLCFLHEFXANG-GOSISDBHSA-N
SMILES: C1(=S)N([C@@H]2CC3=CC(F)=CC(F)=C3OC2)C(CCNCC2=CC=CC=C2)=CN1

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

ChemScene

Product number: CS-0024612
Product name: Zamicastat
Purity: 99.85%
Packaging: 5mg
Price: $250
Updated: 2021/12/16

ChemScene

Product number: CS-0024612
Product name: Zamicastat
Purity: 99.85%
Packaging: 10mg
Price: $450
Updated: 2021/12/16

ChemScene

Product number: CS-0024612
Product name: Zamicastat
Purity: 99.85%
Packaging: 50mg
Price: $1350
Updated: 2021/12/16

ChemScene

Product number: CS-0024612
Product name: Zamicastat
Purity: 99.85%
Packaging: 100mg
Price: $2100
Updated: 2021/12/16

DC Chemicals

Product number: 020457
Product name: Zamicastat
Packaging: 003
Price: $1900
Updated: 2021/12/16

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Zamicastat Chemical Properties,Usage,Production

Uses

Zamicastat (BIA 5-1058) is a dopamine β-hydroxylase (DBH) inhibitor and can cross the blood-brain barrier (BBB) to cause central as well as peripheral effects. Zamicastat is also a concentration-dependent dual P-gp and BCRP inhibitor with IC50 values of 73.8 μM and 17.0 μM, respectively[1]. Zamicastat reduces high blood pressure[2].

in vivo

Zamicastat (10, 30 and 100 mg/kg/day; oral bolus, 7 days) is tested acutely against salt-induced hypertension in the Dahl SS rat. Zamicastat produces a dose-dependent decrease in blood pressure. 24 h after Zamicastat administration mean systolic blood pressure (SBP) decrease is -12.6±4.1 mm Hg (P=0.0284), -15.2±2.7 mm Hg (P=0.0026) and -19.0±3.7 mm Hg (P=0.0036) for the 10, 30, and 100 mg/kg body weight dose, respectively. Zamicastat administration also produces a significant 24-h average decrease in diastolic blood pressure (DBP) of - 14.6±3.4 mm Hg (P=0.0073) with 10 mg/kg body weight dose, -13.0±4.5 mm Hg (P=0.0347) with 30 mg/kg body weight dose and -15.0±3.1 mm Hg (P=0.0046) with 100 mg/kg body weight dose. Zamicastat administration leads to a decrease in the 24h post-dose mean arterial pressure (MAP) of -13.4±3.8 mm Hg (P=0.0162), -14.0±3.5 mm Hg (P=0.0101) and -20.6±3.7 mm Hg (P=0.0026) for the 10, 30, and 100 mg/kg body weight dose, respectively. There is a small, but significant, effect of Zamicastat on the 24-h mean heart rate (HR) post-dose for all tested doses (10 mg/kg: -19.1±3.2 beats/min, P=0.0019; 30 mg/kg: -13.0±4.5 beats/min, P=0.0347; 100 mg/kg: -21.6±6.6 beats/min, P=0.0235)^[2].

Animal Model:	Six-week-old male inbred male Dahl SS rats^[2]
Dosage:	10, 30, or 100 mg/kg; 4 mL/kg
Administration:	Oral bolus, daily, seven days
Result:	Treatment produced a dose-dependent decrease in blood pressure. Twenty four hours after administration mean SBP decrease was -12.6±4.1 mm Hg (P=0.0284), -15.2±2.7 mm Hg (P=0.0026) and -19.0±3.7 mm Hg (P=0.0036) for the 10, 30, and 100 mg/kg body weight dose, respectively.

Animal Model:	ten-week-old male Wistar Han rats^[2]
Dosage:	30 mg/kg/day
Administration:	in animal feedings (mixed in meal rodent food) everyday
Result:	lead to a significant 51% decrease in noradrenaline levels excreted in urine

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. DOI:10.1016/j.ejps.2018.02.006
[2] Igreja B, et al. Effects of Zamicastat treatment in a genetic model of salt-sensitive hypertension and heart failure. Eur J Pharmacol. 2019 Jan 5;842:125-132. DOI:10.1016/j.ejphar.2018.10.030

Zamicastat Preparation Products And Raw materials

Raw materials

Preparation Products

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Zamicastat Suppliers

China 32 United States 4 Global 36

DC Chemicals

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Shanghai Lollane Biological Technology Co.,Ltd.

Tel: 021-52996696，15000506266 15000506266
Fax: +86-21-52996696
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Chengdu Saint - Kay Biotechnology Co., Ltd.

Tel: 028-85157043 15882256948
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Country: China
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Fan De(Beijing) Biotechnology Co., Ltd.

Tel: 15911056312
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Country: China
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TargetMol Chemicals Inc.

Tel: +1-781-999-5354; +17819995354
Email: marketing@targetmol.com
Country: United States
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InvivoChem

Tel: +1-708-310-1919 +1-13798911105
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Dideu Industries Group Limited

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career henan chemical co

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Absin Bioscience Inc.

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Shanghai hongqu biomedical technology co. LTD

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View Lastest Price from Zamicastat manufacturers

Dideu Industries Group Limited

Product: Zamicastat 1080028-80-3
Price: US $1.10/g
Min. Order: 1g
Purity: 99.9%
Supply Ability: 100 Tons min
Release date: 2021-08-17

Career Henan Chemical Co

Product: Zamicastat 1080028-80-3
Price: US $1.00/g
Min. Order: 1g
Purity: 99.99%
Supply Ability: 200kg
Release date: 2019-12-23

1080028-80-3, ZamicastatRelated Search:

ZANAMIVIR HYDRATE

Zamicastat

BIA 5-1058

Zamicastat (BIA 5-1058)

2H-Imidazole-2-thione, 1-[(3R)-6,8-difluoro-3,4-dihydro-2H-1-benzopyran-3-yl]-1,3-dihydro-5-[2-[(phenylmethyl)amino]ethyl]-

Zamicastat USP/EP/BP

ABCB1,Dopamine β-monooxygenase,Inhibitor,Cluster of differentiation 243,ABCG2,inhibit,P-glycoprotein,Multidrug resistance protein 1,BCRP,MDR1,CD243,Breast cancer resistance protein,P-gp,Pgp,Zamicastat,Dopamine β-hydroxylase,Dopamine beta-hydroxylase,Dopamine beta-monooxygenase

Zamicastat, 10 mM in DMSO

1-[6-[[(1S,3S)-3-aminocyclopentyl]amino]-3-pyridyl]pyridin-2-one dihydrochloride

1080028-80-3