GLPBio

BIA 10-2474

Catalog No.: GC18174Purity:>98.00%
BIA 10-2474는 다양한 쥐의 뇌 영역에서 IC50 값이 50~70mg/kg인 지방산 아미드 가수분해효소(FAAH) 억제제입니다.

제품은 연구용으로만 사용됩니다. 인체에 사용할 수 없으며 환자에게 판매하지 않습니다.


BIA 10-2474
Cas No.: 1233855-46-3
5mgIn Stock
$151.00
1
10mgIn Stock
$273.00
1
50mgIn Stock
$312.00
1
100mgIn Stock
$495.00
1

인용 문헌 (Citations)

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제품 설명 (Description)

BIA 10-2474 is an inhibitor of fatty acid amide hydrolase (FAAH; IC50 = 4.9 nM in HEK293T cells expressing the human recombinant enzyme). It also inhibits FAAH2, α/β-hydrolase domain-containing protein 6 (ABHD6), carboxylesterase 2 (CES2), and patatin-like phospholipase domain 6 (PNPLA6) with IC50 values of 0.4, 0.081, 2, and 11 μM, respectively. BIA 10-2474 alters expression of 161 lipid species, including FAAH substrates as well as other lipid classes, in human cortical neuron cultures indicating compound promiscuity. Formulations containing BIA 10-2474 were previously investigated clinically for the management of chronic pain but use was halted due to development of significant neurotoxicity.

실험 프로토콜 (Protocol)

Animal experiment:

Rats: Groups of rats (n=4) are pre-treated with BIA 10-2474 (2 mL/kg in 5% Tween 80 in saline i.p.) or with vehicle 40 min prior to radiotracer injection. Rats, in a restraining box, receives 3–4 MBq of high-specific activity [18F]-DOPP in 0.3mL of 10% ethanol in citrate buffer (pH 6) via the tail vein which has been vasodilated in a warm water bath. They are sacrificed by decapitation at 40 min after radiotracer administration, the brain is surgically removed from the skull and stored on ice. Brain regions are excised, blotted, and weighed while blood is collected. Radioactivity in tissues is assayed[1].

References:

[1]. Tong J, et al. Inhibition of fatty acid amide hydrolase by BIA 10-2474 in rat brain. J Cereb Blood Flow Metab. 2016 Sep 20.
[2]. Kaur R, et al. What failed BIA 10-2474 Phase I clinical trial Global speculations and recommendations for future Phase I trials. J Pharmacol Pharmacother. 2016 Jul-Sep;7(3):120-6

제품 문서 (Product Documents)

Purity:>98.00%Appearance:A solid

화학적 특성 (Chemical Properties)

CAS 번호
1233855-46-3
화학명
N-cyclohexyl-N-methyl-4-(1-oxido-3-pyridinyl)-1H-imidazole-1-carboxamide
SMILES
CN(C(N1C=NC(C2=C[N+]([O-])=CC=C2)=C1)=O)C3CCCCC3
분자식
C16H20N4O2
분자량
300.4
용해도
DMSO : 2.2 mg/mL (7.32 mM; Need ultrasonic)
보관
Store at -20°C
일반 주의사항
제품의 용해도 데이터에 따라 적절한 용매를 선택하십시오. 조제 후에는 반복적인 동결·해동을 피할 수 있도록 저장 용액을 소분하십시오.
저장 용액은 -80°C 보관 시 6개월 이내, -20°C 보관 시 1개월 이내에 사용하십시오.
용해도를 높이려면 튜브를 37°C로 데운 뒤 적절한 시간 동안 초음파 처리하십시오.
배송 조건
평가용 샘플은 아이스팩과 함께 배송됩니다. 그 외 용량은 실온 배송되며, 요청 시 아이스팩과 함께 배송할 수 있습니다.

계산 도구 (Calculators)몰 농도 / 희석 / 분자량 / 단위 변환 / 생체 내 제형 / 용해도

g/mol

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