规格 | 价格 | 库存 | 数量 |
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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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Other Sizes |
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靶点 |
IRE1α (IC50 = 5.9 nM)
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体外研究 (In Vitro) |
Kira8 effectively suppresses IRE1α RNase activity against XBP1 and Ins2 RNAs and prevents IRE1α oligomerization. Kira8 reverses XBP1 splicing that is stimulated by GNF-2 and more effectively than KIRA6 reduces IRE1α-driven apoptosis in INS-1 cells[1].
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体内研究 (In Vivo) |
Male Ins2+/Akita mice receive intraperitoneal injections of KIRA8 (50 mg/kg) every day for 35 days. Over the course of several weeks, a notable decrease in hyperglycemia is observed[1].
Kira8 (50 mg/kg, i.p., once daily) treatment for one week significantly reduces islet XBP1 splicing and TXNIP mRNAs while preserving Ins1/Ins2, BiP, and MANF mRNAs in pre-diabetic NODs mice[1]. |
动物实验 |
Male Ins2+/Akita mice[1]
50 mg/kg Injected i.p.; daily; for 35 days |
参考文献 |
分子式 |
C₃₁H₂₉CLN₆O₃S
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分子量 |
601.118364095688
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精确质量 |
600.17
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元素分析 |
C, 61.94; H, 4.86; Cl, 5.90; N, 13.98; O, 7.98; S, 5.33
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CAS号 |
1630086-20-2
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相关CAS号 |
Kira8 Hydrochloride;2250019-92-0
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外观&性状 |
Solid powder
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SMILES |
CC1=C(C2=C(C=C1)C(=CC=C2)NS(=O)(=O)C3=CC=CC=C3Cl)OC4=C(C=CC=N4)C5=NC(=NC=C5)N[C@H]6CCCNC6
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InChi Key |
XMWUCMFVDXDRDE-NRFANRHFSA-N
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InChi Code |
InChI=1S/C31H29ClN6O3S/c1-20-13-14-22-23(8-4-11-27(22)38-42(39,40)28-12-3-2-10-25(28)32)29(20)41-30-24(9-6-17-34-30)26-15-18-35-31(37-26)36-21-7-5-16-33-19-21/h2-4,6,8-15,17-18,21,33,38H,5,7,16,19H2,1H3,(H,35,36,37)/t21-/m0/s1
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化学名 |
2-chloro-N-[6-methyl-5-[3-[2-[[(3S)-piperidin-3-yl]amino]pyrimidin-4-yl]pyridin-2-yl]oxynaphthalen-1-yl]benzenesulfonamide
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别名 |
KIRA8; KIRA-8; KIRA 8; AMG-18; AMG 18; AMG18; Amgen IRE1α Inhibitor
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HS Tariff Code |
2934.99.9001
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存储方式 |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
运输条件 |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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溶解度 (体外) |
Ethanol: 76.9~100 mg/mL (128~166.4 mM)
DMSO: ~65 mg/mL (~108.1 mM) H2O: ~30 mg/mL (~49.9 mM) |
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溶解度 (体内) |
Solubility in Formulation 1: 4 mg/mL (6.65 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 40.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 2.31 mg/mL (3.84 mM) (saturation unknown) in 3% ethanol, 7% Tween-80, and 90% normal Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.17 mg/mL (3.61 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: ≥ 2.17 mg/mL (3.61 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 21.7 mg/mL clear DMSO stock solution to 900 μL corn oil and mix evenly. 1、请先配制澄清的储备液(如:用DMSO配置50 或 100 mg/mL母液(储备液)); 2、取适量母液,按从左到右的顺序依次添加助溶剂,澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明,并不一定代表此产品 的实际溶解配方): 10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline); 假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀/澄清;向上述体系中加入50 μL Tween-80,混合均匀/澄清;然后继续加入450 μL ddH2O (或 saline)定容至 1 mL; 3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例; 4、 如产品在配制过程中出现沉淀/析出,可通过加热(≤50℃)或超声的方式助溶; 5、为保证最佳实验结果,工作液请现配现用! 6、如不确定怎么将母液配置成体内动物实验的工作液,请查看说明书或联系我们; 7、 以上所有助溶剂都可在 Invivochem.cn网站购买。 |
制备储备液 | 1 mg | 5 mg | 10 mg | |
1 mM | 1.6636 mL | 8.3178 mL | 16.6356 mL | |
5 mM | 0.3327 mL | 1.6636 mL | 3.3271 mL | |
10 mM | 0.1664 mL | 0.8318 mL | 1.6636 mL |
1、根据实验需要选择合适的溶剂配制储备液 (母液):对于大多数产品,InvivoChem推荐用DMSO配置母液 (比如:5、10、20mM或者10、20、50 mg/mL浓度),个别水溶性高的产品可直接溶于水。产品在DMSO 、水或其他溶剂中的具体溶解度详见上”溶解度 (体外)”部分;
2、如果您找不到您想要的溶解度信息,或者很难将产品溶解在溶液中,请联系我们;
3、建议使用下列计算器进行相关计算(摩尔浓度计算器、稀释计算器、分子量计算器、重组计算器等);
4、母液配好之后,将其分装到常规用量,并储存在-20°C或-80°C,尽量减少反复冻融循环。
计算结果:
工作液浓度: mg/mL;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL)。如该浓度超过该批次药物DMSO溶解度,请首先与我们联系。
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL ddH2O,混匀澄清。
(1) 请确保溶液澄清之后,再加入下一种溶剂 (助溶剂) 。可利用涡旋、超声或水浴加热等方法助溶;
(2) 一定要按顺序加入溶剂 (助溶剂) 。
Mono-selective KIRA8 spares β-cells and reverses established diabetes in NOD mice. Cell Metab . 2017 Apr 4;25(4):883-897.e8. td> |