KIRA8 (AMG-18)
| 中文名称 | KIRA8 (AMG-18) |
|---|---|
| 中文同义词 | (S)-2-氯-N-(6-甲基-5-((3-(2-(哌啶-3-基氨基)嘧啶-4-基)吡啶-2-基)氧基)萘-1-基)苯磺酰胺;化合物KIRA8;(S)-2-氯-N-[6-甲基-5-[[3-[2-(3-哌啶基氨基)-4-嘧啶基]-2-吡啶基]氧基]-1-萘基]苯磺酰胺 |
| 英文名称 | Amgen IRE1α Inhibitor |
| 英文同义词 | Amgen IRE1α Inhibitor;Kira8;IRE-1 INHIBITOR;KIRA8 (AMG-18);Benzenesulfonamide, 2-chloro-N-[6-methyl-5-[[3-[2-[(3S)-3-piperidinylamino]-4-pyrimidinyl]-2-pyridinyl]oxy]-1-naphthalenyl]-;(S)-2-Chloro-N-(6-methyl-5-((3-(2-(piperidin-3-ylamino)pyrimidin-4-yl)pyridin-2-yl)oxy)naphthalen-1-yl)benzenesulfonamide;Amgen IRE1a Inhibitor;Inositol requiring enzyme 1,inhibit,AMG18,AMG 18,Kira 8,Kira8,Inhibitor,IRE1,Kira-8 |
| CAS号 | 1630086-20-2 |
| 分子式 | C31H29ClN6O3S |
| 分子量 | 601.12 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 1630086-20-2.mol |
| 结构式 |  |
KIRA8 (AMG-18) 性质
| 沸点 | 812.6±75.0 °C(Predicted) |
|---|---|
| 密度 | 1.383±0.06 g/cm3(Predicted) |
| 储存条件 | Store at -20°C |
| 溶解度 | 水：30.0（最大浓度 mg/mL）；49.91（最大浓度 mM） |
| 形态 | 固体 |
| 酸度系数(pKa) | 7.66±0.30(Predicted) |
| 颜色 | 浅黄至黄色 |
Kira8 (AMG-18) 是一种单选择性 IRE1α 抑制剂，可以变构减弱 IRE1α RNase 活性，IC50 为 5.9 nM。
IRE1α
IC50: 5.9 nM (IRE1α RNase)
Kira8 blocks IRE1α oligomerization, and potently inhibits IRE1α RNase activity against XBP1 and Ins2 RNAs. Kira8 more potently reduces IRE1α-driven apoptosis in INS-1 cells than KIRA6 and also reverses XBP1 splicing promoted by GNF-2.
Male
Ins2
+/Akita
mice are injected i.p. with KIRA8 (50 mg/kg; daily; for 35 days), significant reduction of hyperglycemia become apparent over several weeks.
One week treatment of pre-diabetic NODs mice with Kira8 (50 mg/kg; i.p.; once a day) leads to significant reductions in islet XBP1 splicing and TXNIP mRNAs, and preserves Ins1/Ins2, BiP and MANF mRNAs.
| Animal Model: | Male Ins2 +/Akita mice |
| Dosage: | 50 mg/kg |
| Administration: | Injected i.p.; daily; for 35 days |
| Result: | Significant reduction of hyperglycemia became apparent over several weeks. |
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/01/25 | HY-114368 | Kira8 | 1 mg | 1050元 | |
| 2024/01/25 | HY-114368 | KIRA8 (AMG-18) Kira8 | 1630086-20-2 | 5 mg | 2300元 |