ADX71743

ADX71743 구조식 이미지
카스 번호:
1431641-29-0
상품명:
ADX71743
동의어(영문):
ADX71743;ADX-71743,ADX71743;ADX71743 >=98% (HPLC);4(5H)-Benzoxazolone, 6-(2,4-dimethylphenyl)-2-ethyl-6,7-dihydro-, (+)-
CBNumber:
CB53364104
분자식:
C17H19NO2
포뮬러 무게:
269.34
MOL 파일:
1431641-29-0.mol
MSDS 파일:
SDS

ADX71743 속성

끓는 점
405.1±24.0 °C(Predicted)
밀도
1.130±0.06 g/cm3(Predicted)
산도 계수 (pKa)
-0.05±0.40(Predicted)

안전

ADX71743 C화학적 특성, 용도, 생산

효소 저해제

This brain-penetrant mGlu7 allosteric negative modulator (FW = 269.34 g/mol; CAS 1431641-29-0; Solubility: 100 mM in DMSO), also named 6- (2,4-dimethylphenyl)-2-ethyl-6,7-dihydro-4(5H)-benzoxazolone, potently and selectively targets the metabotropic glutamate receptor-7, itself a promising novel target for treatment of anxiety, post-traumatic stress disorder, depression, drug abuse, and schizophrenia. When tested in vitro, Schild plot analysis and reversibility tests at the target confirmed the NAM properties of the compound and attenuation of L-(+)-2-amino-4- phosphonobutyric acid (or L-AP4) -induced synaptic depression confirmed activity at the native receptor. When tested in vitro, ADX-71743 gives a IC50 value versus EC80 of glutamate = 22 nM at human mGlu7 in a 3’,5’- cyclic-AMP assay, with IC50 values versus EC80 of L-AP4 are 63 and 125 nM at human mGlu7 in Ca2+ and cAMP assays respectively; IC50 value versus EC80 of L-AP4 = 88 nM at rmGlu7 in a Ca2+assay). Selective for mGlu7 over all other mGlu receptor subtypes and a panel of relevant GPCRs. Exhibits an anxiolytic-like profile in vivo. The Schild plot experiments clearly indicate the noncompetitive nature of ADX71743 inhibition, whereas simple wash experiments seem to indicate that its binding to the receptor is readily reversible. Other Targets: When tested for its action at other mGlu-expressing cells in series of FLIPR experiments, ADX71743 showed no detectable activity (either agonist or allosteric effects) in cell lines expressing hmGlu3, hmGlu4, rmGlu5, hmGlu6, and hmGlu8. A negligible inhibition of rmGlu1 (32% at 30 μM) and a weak positive allosteric modulator effect on hmGlu2 (EC50 = 11 μM) was measured. When further tested in a functional GPCR screen against 27 targets in agonist and antagonist modes, ADX71743 exhibited no stimulation or inhibition above 27% was observed.

ADX71743 준비 용품 및 원자재

원자재

준비 용품


ADX71743 공급 업체

글로벌( 9)공급 업체
공급자 전화 이메일 국가 제품 수 이점
TargetMol Chemicals Inc.
+1-781-999-5354 +1-00000000000
marketing@targetmol.com United States 19892 58
Shanghai Hongye Biotechnology Co. Ltd 400-9205774
sales@glpbio.cn China 6870 58
BOC Sciences --
info@bocsci.com USA 0 65
Energy Chemical 021-58432009 400-005-6266
marketing@energy-chemical.com China 44941 58
Changzhou Furuisi Biotechnology Co., Ltd 0519-85524369
3477467573@qq.com China 8618 58
Beijing Jin Ming Biotechnology Co., Ltd. 010-60605840 15801484223;
psaitong@jm-bio.com China 29778 58
TargetMol Chemicals Inc. 4008200310
marketing@tsbiochem.com China 23963 58
Nantong QuanYi Biotechnology Co., Ltd 0513-66337626 18051384581
sales@chemhifuture.com China 4578 58

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