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198419-91-9

中文名稱 LY-367385;(R)-(+)-ALPHA-AMINO-4-CARBOXY-2-METHYLBENZENEACETIC ACID
英文名稱 LY 367385
CAS 198419-91-9
分子式 C10H11NO4
分子量 209.2
MOL 文件 198419-91-9.mol
198419-91-9 結(jié)構(gòu)式 198419-91-9 結(jié)構(gòu)式

基本信息

中文別名
化合物 T15818
化合物 LY367385 HYDROCHLORIDE
英文別名
LY 367385
LY-367385 hydrochloride
SGIKDIUCJAUSRD-QMMMGPOBSA-N
(S)-4-[aMino(carboxy)Methyl]-3-Methylbenzoic acid
(S)-(+)-α-Amino-4-carboxy-2-methylbenzeneaceticacid
(S)-(+)-a-amino-4-carboxy-2-methylbenzeneacetic acid
Benzeneacetic acid, α-amino-4-carboxy-2-methyl-, (αS)-
(R)-(+)-alpha-Amino-4-carboxy-2-methylbenzeneacetic acid
(S)-(+)-ALPHA-AMINO-4-CARBOXY-2-METHYLBENZENEACETIC ACID
LY-367385
(R)-(+)-ALPHA-AMINO-4-CARBOXY-2-METHYLBENZENEACETIC ACID

物理化學(xué)性質(zhì)

儲(chǔ)存條件Desiccate at RT
溶解度H2O:>10mg/mL
形態(tài)粉末
顏色白色至灰白色

安全數(shù)據(jù)

WGK Germany3
LY-367385;(R)-(+)-ALPHA-AMINO-4-CARBOXY-2-METHYLBENZENEACETIC ACID價(jià)格(試劑級(jí))
報(bào)價(jià)日期產(chǎn)品編號(hào)產(chǎn)品名稱CAS號(hào)包裝價(jià)格
2024/11/08HY-107515ALY-367385;(R)-(+)-ALPHA-AMINO-4-CARBOXY-2-METHYLBENZENEACETIC ACID
LY367385 hydrochloride
198419-91-95mg850元
2024/11/08HY-107515ALY-367385;(R)-(+)-ALPHA-AMINO-4-CARBOXY-2-METHYLBENZENEACETIC ACID
LY367385 hydrochloride
198419-91-910mM * 1mLin DMSO940元
2024/11/08HY-107515ALY-367385;(R)-(+)-ALPHA-AMINO-4-CARBOXY-2-METHYLBENZENEACETIC ACID
LY367385 hydrochloride
198419-91-910mg1450元

常見問題列表

生物活性
LY367385 是一種高效且選擇性的 mGluR1a 拮抗劑,抑制喹喹啉誘導(dǎo)的磷酸肌醇水解的 IC50 值為 8.8 μM,而對(duì) mGlu5a 的 IC50 值大于 100 μM。LY367385 具有神經(jīng)保護(hù),抗驚厥和抗癲癇作用。
靶點(diǎn)

mGluR1a

8.8 μM (IC 50 )

體外研究

LY367385 combined with N-methyl-D-aspartate (NMDA) during the toxic pulse attenuates neuronal degeneration in a concentration-dependent fashion, with a maximal reduction of NMDA toxicity ranging from 40 to 60%. LY367385 shows greater efficacy than LY367366 and neither of these compounds influenced neuronal viability per se. LY367385 shows potent neuroprotective effects, with causing a 50% reduction in (S)-3,5-Dihydroxyphenylglycine (DHPG) potentiation at a concentration of 10 nM. Under experimental conditions at higher concentrations of antagonist, LY367385 a completely antagonized the amplification of NMDA toxicity by DHPG.

體內(nèi)研究

LY367385 has been administered intracerebroventricularly (i.c.v.) to DBA/2 mice and lethargic mice (lh/lh), and focally into the inferior colliculus of genetically epilepsy prone rats (GEPR). In DBA/2 mice, LY367385 produces a rapid, transient suppression of sound-induced clonic seizures ED50 = 12 nM, i.c.v., 5 min). In lethargic mice, LY367385 significantly reduces the incidence of spontaneous spike and wave discharges on the electroencephalogram, from 30 to >150 min after the administration of LY367385, 250 nM, i.c.v.
In genetically epilepsy prone rats, LY367385 reduces sound-induced clonic seizures. LY367385, 160 nM bilaterally, fully suppresses clonic seizures after 2-4 h.

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