KIRA8 (AMG-18)
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- CAS号:
- 1630086-20-2
- 英文名:
- Amgen IRE1α Inhibitor
- 英文别名:
- Kira8;KIRA8 (AMG-18);IRE-1 INHIBITOR;Amgen IRE1α Inhibitor;Amgen IRE1a Inhibitor;Inositol requiring enzyme 1,inhibit,AMG18,AMG 18,Kira 8,Kira8,Inhibitor,IRE1,Kira-8;(S)-2-Chloro-N-[6-methyl-5-[[3-[2-(3-piperidylamino)-4-pyrimidinyl]-2-pyridyl]oxy]-1-naphthyl]benzenesulfonamide;(S)-2-Chloro-N-(6-methyl-5-((3-(2-(piperidin-3-ylamino)pyrimidin-4-yl)pyridin-2-yl)oxy)naphthalen-1-yl)benzenesulfonamide;Benzenesulfonamide, 2-chloro-N-[6-methyl-5-[[3-[2-[(3S)-3-piperidinylamino]-4-pyrimidinyl]-2-pyridinyl]oxy]-1-naphthalenyl]-
- 中文名:
- KIRA8 (AMG-18)
- 中文别名:
- 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;(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
- CBNumber:
- CB73123772
- 分子式:
- C31H29ClN6O3S
- 分子量:
- 601.12
- MOL File:
- 1630086-20-2.mol
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KIRA8 (AMG-18)化学性质
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沸点:
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812.6±75.0 °C(Predicted)
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密度:
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1.383±0.06 g/cm3(Predicted)
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储存条件:
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Store at -20°C
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溶解度:
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Water:30.0(Max Conc. mg/mL);49.91(Max Conc. mM)
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酸度系数(pKa):
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7.66±0.30(Predicted)
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KIRA8 (AMG-18)性质、用途与生产工艺
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.
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Animal Model:
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Male
Ins2
+/Akita
mice
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Dosage:
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50 mg/kg
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Administration:
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Injected i.p.; daily; for 35 days
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Result:
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Significant reduction of hyperglycemia became apparent over several weeks.
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KIRA8 (AMG-18)
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
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| 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 |
1630086-20-2, KIRA8 (AMG-18) 相关搜索:
- C31H29ClN6O3S
- (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
- 化合物KIRA8
- (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
- 1630086-20-2
- (S)-2-Chloro-N-[6-methyl-5-[[3-[2-(3-piperidylamino)-4-pyrimidinyl]-2-pyridyl]oxy]-1-naphthyl]benzenesulfonamide
- Inositol requiring enzyme 1,inhibit,AMG18,AMG 18,Kira 8,Kira8,Inhibitor,IRE1,Kira-8
- Amgen IRE1a Inhibitor
- (S)-2-Chloro-N-(6-methyl-5-((3-(2-(piperidin-3-ylamino)pyrimidin-4-yl)pyridin-2-yl)oxy)naphthalen-1-yl)benzenesulfonamide
- Benzenesulfonamide, 2-chloro-N-[6-methyl-5-[[3-[2-[(3S)-3-piperidinylamino]-4-pyrimidinyl]-2-pyridinyl]oxy]-1-naphthalenyl]-
- KIRA8 (AMG-18)
- IRE-1 INHIBITOR
- Kira8
- Amgen IRE1α Inhibitor