추천 제품
Quality Level
분석
≥98% (HPLC)
양식
powder
색상
faint red to dark brown
solubility
DMSO: 2 mg/mL, clear
저장 온도
−20°C
SMILES string
C[N+]1=CC=CC2=C(C=CC=C12)N.[I-]
InChI
1S/C10H10N2.HI/c1-12-7-3-4-8-9(11)5-2-6-10(8)12;/h2-7,11H,1H3;1H
InChI key
JPEZFBFIRRAFNR-UHFFFAOYSA-N
생화학적/생리학적 작용
5-Amino-1-methylquinolinium (5-amino-1MQ) is a substrate site-targeting, selective nicotinamide N-methyltransferase (NNMT) inhibitor (IC50 = 1.2 μM; 50 μM SAM, 100 μM NCA) that reduces 3T3-L1 lipogenesis (EC50 = 30μM) and adipocytes 1-methylnicotinamide level (EC50 = 2.3 μM) without affecting related methyltransferases & enzymes in the NAD+ salvage pathway. 5-amino-1MQ shows in vivo therapeutic efficacy in murine models of DIO (20 mg/kg/d sc.), muscle injury (5 or 10 mg/kg bid. sc.), and intraperitoneal HeyA8 ovarian cancer metastasis (20 mg/kg/d ip.) with no adverse effects to the animals (up to 60 mg/kg/d). Note:1.89 mg iodide salt contains 1 mg eq of 5-amino-1MQ.
Substrate site-targeting, selective nicotinamide N-methyltransferase (NNMT) inhibitor with in vitro and in vivo efficay.
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point (°F)
Not applicable
Flash Point (°C)
Not applicable
가장 최신 버전 중 하나를 선택하세요:
Harshini Neelakantan et al.
Journal of medicinal chemistry, 60(12), 5015-5028 (2017-05-27)
Nicotinamide N-methyltransferase (NNMT) is a fundamental cytosolic biotransforming enzyme that catalyzes the N-methylation of endogenous and exogenous xenobiotics. We have identified small molecule inhibitors of NNMT with >1000-fold range of activity and developed comprehensive structure-activity relationships (SARs) for NNMT inhibitors.
Mark A Eckert et al.
Nature, 569(7758), 723-728 (2019-05-03)
High-grade serous carcinoma has a poor prognosis, owing primarily to its early dissemination throughout the abdominal cavity. Genomic and proteomic approaches have provided snapshots of the proteogenomics of ovarian cancer1,2, but a systematic examination of both the tumour and stromal
Harshini Neelakantan et al.
Biochemical pharmacology, 147, 141-152 (2017-11-21)
There is a critical need for new mechanism-of-action drugs that reduce the burden of obesity and associated chronic metabolic comorbidities. A potentially novel target to treat obesity and type 2 diabetes is nicotinamide-N-methyltransferase (NNMT), a cytosolic enzyme with newly identified
Harshini Neelakantan et al.
Biochemical pharmacology, 163, 481-492 (2019-02-13)
Aging is accompanied by progressive declines in skeletal muscle mass and strength and impaired regenerative capacity, predisposing older adults to debilitating age-related muscle deteriorations and severe morbidity. Muscle stem cells (muSCs) that proliferate, differentiate to fusion-competent myoblasts, and facilitate muscle
자사의 과학자팀은 생명 과학, 재료 과학, 화학 합성, 크로마토그래피, 분석 및 기타 많은 영역을 포함한 모든 과학 분야에 경험이 있습니다..
고객지원팀으로 연락바랍니다.