规格 | 价格 | 库存 | 数量 |
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1mg |
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5mg |
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10mg |
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Other Sizes |
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靶点 |
DYRK1 DYRK1A 0.0062 μM (IC50) GSK3β >50 μM (IC50)
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体内研究 (In Vivo) |
GNF2133(30 mg/kg;口服)的口服生物利用度为 22.3%,口服吸收良好。[1]。 GNF2133(30 mg/kg;口服;每天一次,持续五天)表现出体内 β 细胞增殖[1]。在 RIP-DTA 小鼠中,GNF2133(3、10、30 mg/kg)显着增加胰岛素分泌和葡萄糖处理能力[1]。 GNF2133在CD-1小鼠中的药代动力学参数[1]。血浆 (iv) 胰腺 (po) 和血浆 (po) CL,单位为毫升/分钟/千克 23.5 // Vss (L/kg) AUC (h·nM) 3268 10974 144420 Clast(nM) 36.6 19 1324 t1/2<( h) Cmax(nM) 1977 1675 13319 tmax<(h) 0.03 3.0 3.0 30 mg/kg;宝[1]; 6.6 3.4 6.6 F (%) / 22.3 / CD-1 小鼠。
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动物实验 |
Animal/Disease Models: CD-1 mice[1]
Doses: 30 mg/kg Route of Administration: Po Experimental Results: demonstrated good oral absorption and moderate plasma exposure with oral bioavailability of 22.3%. Animal/Disease Models: Wistar Han rat[1] Doses: 30 mg/kg (0.5% methylcellulose + Tween-80) Route of Administration: Po; one time/day for 5 days Experimental Results: Increased cyclin D1 levels and overall cell density, and increased in cell proliferation marker Ki67 and insulin. Animal/Disease Models: Diphtheria toxin A (RIP-DTA) mice[1] Doses: 3, 10, 30 mg/kg (20 mg/kg doxycycline (Dox) for 5 days) Route of Administration: Po, one time/day for 35 days Experimental Results: Dramatically improves glucose disposal capacity and increased insulin secretion. |
参考文献 |
[1]. Liu YA, et al. Selective DYRK1A Inhibitor for the Treatment of Type 1 Diabetes: Discovery of 6-Azaindole Derivative GNF2133. J Med Chem. 2020 Mar 26;63(6):2958-2973.
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分子式 |
C24H30N6O2
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分子量 |
434.53
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CAS号 |
2561414-56-8
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相关CAS号 |
GNF2133 hydrochloride;2561414-57-9
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SMILES |
N(C1N=CC=C(C2=CN(C3CCOCC3)C3=CN=CC=C23)C=1)C(N1CCN(CC)CC1)=O
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溶解度 (体外) |
DMSO: 4 mg/mL (9.21 mM)
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溶解度 (体内) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 请根据您的实验动物和给药方式选择适当的溶解配方/方案: 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 | 2.3013 mL | 11.5067 mL | 23.0134 mL | |
5 mM | 0.4603 mL | 2.3013 mL | 4.6027 mL | |
10 mM | 0.2301 mL | 1.1507 mL | 2.3013 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) 。