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849234-64-6

中文名稱 BRD 6929;COMPOUND-60
英文名稱 4-acetamido-N-(2-amino-5-(thiophen-2-yl)phenyl)benzamide
CAS 849234-64-6
分子式 C19H17N3O2S
分子量 351.42
MOL 文件 849234-64-6.mol
更新日期 2024/12/23 10:32:13
849234-64-6 結(jié)構(gòu)式 849234-64-6 結(jié)構(gòu)式

基本信息

中文別名
化合物BRD-6929
英文別名
151025
Merck60
BRD 6929
Compound-60
BRD 6929
COMPOUND-60
4-acetamido-N-(2-amino-5-(thiophen-2-yl)phenyl)benzamide
Benzamide, 4-(acetylamino)-N-[2-amino-5-(2-thienyl)phenyl]-

物理化學(xué)性質(zhì)

儲(chǔ)存條件-20°C儲(chǔ)存
溶解度可溶于DMSO
形態(tài)固體
顏色Off-white to gray
BRD 6929;COMPOUND-60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-100719BRD 6929;COMPOUND-60
BRD-6929
849234-64-61mg342元
2024/11/08HY-100719BRD 6929;COMPOUND-60
BRD-6929
849234-64-65mg900元
2024/11/08HY-100719BRD 6929;COMPOUND-60
BRD-6929
849234-64-610mM * 1mLin DMSO990元

常見問題列表

生物活性
BRD-6929 是 I 類組蛋白去乙酰化酶 HDAC1 和 HDAC2 的腦滲透性選擇性抑制劑 (IC50=?1 和 8 nM)。BRD-6929 對 HDAC1 和 HDAC2 有高親和力 (Ki?=?0.2 和 1.5 nM)。BRD-6929 可用于情緒相關(guān)行為的研究。
靶點(diǎn)

HDAC1

1 nM (IC 50 )

HDAC2

8 nM (IC 50 )

HDAC3

458 nM (IC 50 )

HIV-1

體外研究

In vitro?IC 50 for HDAC1-9 by BRD-6929 using recombinant human HDAC enzymes and HDAC class-specific substrates. BRD-6929 and substrate are incubated for 180 min (HDAC1-3)?to control for HDAC1-3 inhibition, BRD-6929 is against HDAC1, HDAC2, HDAC3 and HDAC4-9 with IC 50 s of 0.001 μM, 0.008 μM, 0.458 μM and >30 μM, respectively. In vitro?binding affinity (K i ) and kinetics (half-life ‘T 1/2 ′?in minutes) for HDAC 1, 2 and 3 incubated with BRD-6929 (10 μM), the K i values are <0.2 nM, 1.5nM, and 270 nM for HDAC 1, 2 and 3, respectively. The T 1/2 values are >2400 mins, >4800 mins, and 1200 mins for HDAC 1, 2 and 3, respectively. BRD-6929 (1 and 10 uM) does not cause an increase or decrease in overall cell number in brain region specific primary cultures. Additionally, BRD-6929 (10 uM) causes an increase in H4K12 acetylation in brain region specific primary cultures (striatum).BRD-6929 (1-10 uM; 6 hours) causes a significant increase in H2B acetylation in primary neuronal cell cultures. BRD-6929 (1-20 uM; 24 hours) induces a dose-dependent acetylation of H4K12ac with an EC 50 of 7.2 μM in cultured neurons.BRD-6929 potentiates the efficacy of gnidimacrin (a PKC Agonist) against latent HIV-1.

體內(nèi)研究

BRD-6929 (intraperitoneal?injection; 45 mg/kg; single dose) exhibits a C max , T 1/2 and AUC values of 17.7 μM, 7.2 hours, and 25.6 μM/L*hr, respectively in plasma. It shows a C max , T 1/2 and AUC values of 0.83 μM, 6.4 hours, and 3.9 μM/L*hr, respectively in brain.BRD-6929 (intraperitoneal?injection; 45 mg/kg; 10 days) acts as a deacetylase inhibitor in mouse brain. It significantly increases acetylation in each brain region by 1.5- to 2.0-fold compared to vehicle. The western blotting reveals that BRD-6929 significantly increases acetylation of histone H2B (tetra-acetylated), H3K9 and H4K12 in cortex, ventral striatum and hippocampus after the 10th daily treatment in adult male C57BL/6J mice.

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