10mM in DMSO 최소한의 기준선 간섭이 필요한 민감한 크로마토그래피 및 분석 워크플로우용.
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보관 및 배송
Argon charged,Store at -80°C Dry ice packs + Cold packs 출고. 정확한 사양은 로트별 COA를 확인하세요.
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품질 문서
SDS, COA, 데이터시트, 사양서를 다운로드할 수 있습니다. 로트별 COA는 로트 번호 조회를 통해 확인할 수 있습니다.
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문헌적 근거
크로마토그래피, 유기 합성 및 교차 커플링 반응 분야의 동료 심사 논문 0편에서 인용되었습니다.
개요
Etamicastat hydrochloride (BIA 5-453 hydrochloride) is a potent and reversible dopamine-β-hydroxylase ( DBH ) inhibitor with an IC 50 value of 107 nM Etamicastat can be used in the research of cardiovascular diseases .
In Vitro
Etamicastat blocks the hERG current amplitude with an IC 50 value of 44 μg/mL (141 μM). MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Etamicastat (100 mg/kg; administered intraperitoneally) leads to a significant reduction of noradrenaline levels in heart with concomitant increasing in dopamine levels . Etamicastat (50 mg/kg; a single oral administration) exhibits moderate oral bioavailability (64%), C max (4.9 nM), and terminal elimination half-lives (T 1/2 =3.7 h) in male Wistar rats . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: NMRi mice Dosage: 100 mg/kg Administration: Administered intraperitoneally Result: Led to a significant reduction of noradrenaline levels (36% control) in heart with concomitant increasing in dopamine levels (850% of control). Animal Model: Male Wistar rats Dosage: 50 mg/kg (Pharmacokinetic Analysis) Administration: Orally administered with at a dose volume of 10 mL/kg Result: Oral bioavailability (64%), C max (4.9 nM), and (T 1/2 =3.7 h).
IC50& Target:IC50: 107 nM (DBH)
사양
사양 및 순도
10mM in DMSO
생화학 및 생리적 메커니즘
Etamicastat hydrochloride (BIA 5-453 hydrochloride) is a potent and reversible dopamine-β-hydroxylase ( DBH ) inhibitor with an IC 50 value of 107 nM. Etamicastat can be used in the research of cardiovascular diseases.
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