Apinocaltamide - 10mM in DMSO , Voltage-gated T-type calcium channel blocker, CAS No.1838651-58-3, Voltage-gated T-type calcium channel blocker

CAS: 1838651-58-3 Cat. No.: A655794 분자식: C22H18F3N5O 분자량: 425.41 PubChem CID: 118560618
주문 가능
등급 & 순도 10mM in DMSO
Storage
Store at -80°C
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1ml
A655794-1ml
주문제작 · 8~12주

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이 등급을 선택하는 이유

10mM in DMSO 최소한의 기준선 간섭이 필요한 민감한 크로마토그래피 및 분석 워크플로우용.

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보관 및 배송

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

Apinocaltamide (ACT-709478) is a potent, selective, orally active, and brain penetrating T-type calcium channel blocker. ACT-709478 is used in the research of generalized epilepsies

In Vitro

Apinocaltamide (Compound 66b) blocks Ca v 3.1, Ca v 3.2, Ca v 3.3, Ca v 1.2 with IC 50 s of 6.4, 18, 7.5 and 2410 nM, respectively. Apinocaltamide blocks recombinant channel hCa v 3.3 potently with marked voltage-dependency (K r ≈1500 nM and K i ≈20 nM). Apinocaltamide blocks currents through hK v 11.1-hERG channels with an IC 50 of 5.5 μM. Apinocaltamide also inhibits P450 enzymes with IC 50 s of 14, 15, 22, 25, 51 and 52 μM for CYP2C8,CYP2D6 CYP2C9, CYP2C19, CYP3A4, and CYP2B6, respectively. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Apinocaltamide (Compound 66b, 100, 300 mg/kg, p.o., measured 12 hours later) potently decreases the cumulative duration of absence-like seizures in mice . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male juvenile DBA/2J mice (22-24 days old) Dosage: 100, 300 mg/kg, 1 hour or 3 hours before exposure to the stimulus. Administration: P.O., for 12 hours Result: Decreased the cumulative duration of absence-like seizures over the next 12 h period by 93%.

IC50& Target:Ca v 1.2 2410 nM (IC 50 ) Ca V 3.1 6.4 nM (IC 50 ) Ca v 3.2 18 nM (IC 50 ) Ca V 3.3 7.5 nM (IC 50 )

사양

사양 및 순도
10mM in DMSO
생화학 및 생리적 메커니즘
Apinocaltamide (ACT-709478) is a potent, selective, orally active, and brain penetrating T-type calcium channel blocker. ACT-709478 is used in the research of generalized epilepsies.
보관 조건
Store at -80°C
배송
Dry ice packs + Cold packs
이 제품은 콜드 체인 배송이 필요합니다.지상 및 기타 경제 서비스는 사용할 수 없습니다.
작업 유형
BLOCKER
작동 메커니즘
Voltage-gated T-type calcium channel blocker
제품 특성
ALogP
3.3
이름과 식별자
이성체 SMILES
C1CC1(C2=CC=C(C=C2)CC(=O)NC3=NN(C=C3)CC4=NC=C(C=C4)C#N)C(F)(F)F
대체 CAS
1838651-58-3
PubChem CID
118560618
MeSH 용어
ACT-709478;N-(1-((5-cyanopyridin-2-yl)methyl)pyrazol-3-yl)-2-(4-(1-(trifluoromethyl)cyclopropyl)phenyl)acetamide
분자량
425.41

문서

📋 안전 데이터 시트(SDS)

위험성, 취급, 보관 및 규제 준수를 포괄하는 종합 문서.

<<<<<<< HEAD SDS 다운로드 → ======= SDS 다운로드 → >>>>>>> release248-p3

✅ 분석 성적서(COA)

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🔬 사양서

이 등급의 전체 품질 특성 및 합격 기준.

사양서 보기 →

고급 데이터

관련 대상(인간)
CACNA1H Tclin Voltage-dependent T-type calcium channel subunit alpha-1H (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
CACNA1G Tclin Voltage-dependent T-type calcium channel subunit alpha-1G (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
CACNA1I Tclin Voltage-dependent T-type calcium channel subunit alpha-1I (2 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
CACNA1C Tclin Voltage-dependent L-type calcium channel subunit alpha-1C (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
KCNH2 Tclin Potassium voltage-gated channel subfamily H member 2 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
인증서(CoA, COO, BSE/TSE 및 분석 차트)
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1 results found

Lot NumberCertificate Type날짜항목
J2613710J2613710Certificate of AnalysisOct 16, 2026 A655794
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