Kira8|1630086-20-2|(AMG-18)-陌孚医药/Medlife

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Kira8 (Synonyms: AMG-18)

目录号: PL02208 纯度: ≥99%

CAS No. :1630086-20-2

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中文名称	Kira8
英文名称	Kira8
英文别名	Kira8;Ire-1 inhibitor;Amgen IRE1alpha Inhibitor;BDBM50043766;(S)-2-Chloro-N-(6-methyl-5-((3-(2-(piperidin-3-ylamino)pyrimidin-4-yl)pyridin-2-yl)oxy)naphthalen-1-yl)benzenesulfonamide;2-chloro-N-(6-methyl-5-{[3-(2-{[(3S)-piperidin-3-yl]amino}pyrimidin-4-yl)pyridin-2-yl]oxy}naphthalen-1-yl)benzene-1-sulfonamide;QFV;2-chloro-N-[6-methyl-5-[3-[2-[[(3S)-piperidin-3-yl]amino]pyrimidin-4-yl]pyridi;AMG-18
Cas No.	1630086-20-2
分子式	C₃₁H₂₉ClN₆O₃S
分子量	601.12
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情	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。
生物活性	Kira8 (AMG-18) is a mono-selective IRE1α inhibitor that allosterically attenuates IRE1α RNase activity with an IC 50 of 5.9 nM.
性状	Solid
IC50 & Target[1][2]	IRE1α IC50: 5.9 nM (IRE1α RNase)
体外研究(In Vitro)	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. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	Male Ins2 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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Powder -20°C 3 years；4°C 2 years
参考文献	[1]. Morita S, et al. Targeting ABL-IRE1α Signaling Spares ER-Stressed Pancreatic β Cells to Reverse Autoimmune Diabetes. Cell Metab. 2017 Apr 4;25(4):883-897.e8.

溶解度数据	In Vitro: Ethanol : 76.92 mg/mL (127.96 mM; ultrasonic and adjust pH to 5 with HCl)DMSO : 65 mg/mL (108.13 mM; Need ultrasonic)H₂O : 30 mg/mL (49.91 mM; ultrasonic and warming and adjust pH to 2 with HCl and heat to 60°C)

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1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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