AFN-1252

AFN-1252 구조식 이미지
카스 번호:
620175-39-5
상품명:
AFN-1252
동의어(영문):
CS-2098;AFN-1252;Debio-1452;AFN-1252, API-1252;Debio-1452(AFN1252);AFN-1252(Debio 1452);API1252; DEBIO1452;API 1252; DEBIO-1452;API1252; DEBIO1452;Antibiotic,AFN 1252,AFN1252,inhibit,API1252,Bacterial,Debio-1452,AFN-1252,Debio1452,Inhibitor,API 1252;(E)-3-(1,2,3,4-tetrahydro-2-oxo-1,8-naphthyridin-6-yl)-N-methyl-N-((3-methylbenzofuran-2-yl)methyl)acrylamide;(E)-N-Methyl-N-((3-methylbenzofuran-2-yl)methyl)-3-(7-oxo-5,6,7,8-tetrahydro-1,8-naphthyridin-3-yl)acrylamide
CBNumber:
CB23041381
분자식:
C22H21N3O3
포뮬러 무게:
375.42
MOL 파일:
620175-39-5.mol

AFN-1252 속성

끓는 점
601.2±65.0 °C(Predicted)
밀도
1.28±0.1 g/cm3(Predicted)
저장 조건
2-8°C
용해도
DMSO:5.8(Max Conc. mg/mL);15.45(Max Conc. mM)
물리적 상태
결정성 고체
산도 계수 (pKa)
3.60±0.20(Predicted)
안전
  • 위험 및 안전 성명
  • 위험 및 사전주의 사항 (GHS)
그림문자(GHS): GHS hazard pictograms
신호 어: Warning
유해·위험 문구:
암호 유해·위험 문구 위험 등급 범주 신호 어 그림 문자 P- 코드
H302 삼키면 유해함 급성 독성 물질 - 경구 구분 4 경고 GHS hazard pictograms P264, P270, P301+P312, P330, P501
H315 피부에 자극을 일으킴 피부부식성 또는 자극성물질 구분 2 경고 GHS hazard pictograms P264, P280, P302+P352, P321,P332+P313, P362
H319 눈에 심한 자극을 일으킴 심한 눈 손상 또는 자극성 물질 구분 2A 경고 GHS hazard pictograms P264, P280, P305+P351+P338,P337+P313P
H335 호흡 자극성을 일으킬 수 있음 특정 표적장기 독성 - 1회 노출;호흡기계 자극 구분 3 경고 GHS hazard pictograms
예방조치문구:
P261 분진·흄·가스·미스트·증기·...·스프레이의 흡입을 피하시오.
P305+P351+P338 눈에 묻으면 몇 분간 물로 조심해서 씻으시오. 가능하면 콘택트렌즈를 제거하시오. 계속 씻으시오.

AFN-1252 C화학적 특성, 용도, 생산

개요

AFN-1252 is an inhibitor of staphylococcal enoyl-acyl carrier protein reductase (FabI; Ki = 12.8 nM), an enzyme that activates bacterial fatty acid biosynthesis. It is selective for isolates of methicillin-susceptible and methicillin-resistant S. aureus (MIC90s = ≤0.008 μg/ml) over isolates of S. pneumoniae, β-hemolytic streptococci, Enterococcus, Enterobacteriaceae, non-fermentative Gram-negative bacilli, and M. catarrhalis (MIC90s = >4 μg/ml). In vivo, AFN-1252 increases survival in a murine acute lethal septicemia model, showing 100% survival when administered at a single oral dose of 1 mg/kg.

효소 저해제

This selective, orally available, first-in-class antibiotic (FW = 375.43 g/mol; CAS 620175-39-5; Formulated in 1% Poloxamer 407) is a potent inhibitor of Staphylococcus aureus enoyl-acyl carrier protein reductase (FabI), thereby preventing fatty acyl chain elongation and disrupting biosynthesis of both saturated and unsaturated fatty acids needed for bacterial growth. It demonstrates exceptional potency and specificity against staphylococcal isolates, with typical S. aureus MIC ranges of 0.002–0.12 μg/mL and MIC90s of ≤ 0.015 μg/mL. Mode of Action: FabI is the only enoyl-ACP reductase in S. aureus, S. epidermidis, and related staphylococci, with no alternative enzyme or rescue pathway, including processing of exogenously supplied fatty acids. Such metabolic features suggest FabI may be essential to cell viability in Staphylococcus spp. The inhibitor’s target was convincingly confirmed (a) by using direct enzyme assays (IC50 = 14 nM, with no inhibition of the human enzyme, even at 67 μM); (b) by employing radiolabeled acetate to demonstrate that AFN-1252 greatly reduced incorporation into lipids; (c) by co-crystallizing AFN-1252 and FabI in the presence of the unnatural substrate 3′-NADPH, and (d) by genetically determining AFN-1252’s spontaneous resistance frequency and characterizing AFN-1252-resistant FabI mutants. In socalled time-kill assays, AFN-1252 caused a time-dependent reduction in the viability of S. aureus ATCC 29213 (MSSA) and S. aureus ATCC 43300 (MRSA), with similar magnitudes and rates of killing were obtained at 4 and 128 times the MIC (i.e., 2.0- and 2.9-log10 reductions).

AFN-1252 준비 용품 및 원자재

원자재

준비 용품


AFN-1252 공급 업체

글로벌( 50)공급 업체
공급자 전화 이메일 국가 제품 수 이점
ATK CHEMICAL COMPANY LIMITED
+undefined-21-51877795
ivan@atkchemical.com China 32480 60
Shenzhen Shengda Pharma Limited
755-85269922 +8613424394241
sales@shengdapharm.com CHINA 310 58
InvivoChem
+1-708-310-1919 +1-13798911105
sales@invivochem.cn United States 6393 58
Henan Aochuang Chemical Co.,Ltd.
+86-0371-63689365 +8618638391208
sales@aochuangchem.com China 9425 58
TargetMol Chemicals Inc.
+1-781-999-5354
support@targetmol.com United States 19973 58
Amadis Chemical Company Limited
571-89925085
sales@amadischem.com China 132020 58
Shanghai Rechem science Co., Ltd. 21-31433387 15618786686
sales@rechemscience.com China 2970 58
Shanghai Boyle Chemical Co., Ltd.
sales@boylechem.com China 2923 55
Dalian Meilun Biotech Co., Ltd. 0411-62910999 13889544652
sales@meilune.com China 4648 58
Haoyuan Chemexpress Co., Ltd. 021-58950125
info@chemexpress.com China 7553 61

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