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
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
N-Bromosuccinimide Price
- Product number
- CS-0024612
- Product name
- Zamicastat
- Purity
- 99.85%
- Packaging
- 5mg
- Price
- $250
- Updated
- 2021/12/16
- Product number
- CS-0024612
- Product name
- Zamicastat
- Purity
- 99.85%
- Packaging
- 10mg
- Price
- $450
- Updated
- 2021/12/16
- Product number
- CS-0024612
- Product name
- Zamicastat
- Purity
- 99.85%
- Packaging
- 50mg
- Price
- $1350
- Updated
- 2021/12/16
- Product number
- CS-0024612
- Product name
- Zamicastat
- Purity
- 99.85%
- Packaging
- 100mg
- Price
- $2100
- Updated
- 2021/12/16
- Product number
- 020457
- Product name
- Zamicastat
- Packaging
- 001
- Price
- $600
- Updated
- 2021/12/16
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
Zamicastat Suppliers
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- Country
- United States
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- United States
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- United States
- ProdList
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View Lastest Price from Zamicastat manufacturers
- 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
- Product
- Zamicastat 1080028-80-3
- Price
- US $1.00/g
- Min. Order
- 1g
- Purity
- 99.99%
- Supply Ability
- 200kg
- Release date
- 2019-12-23