规格 | 价格 | 库存 | 数量 |
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10 mM * 1 mL in DMSO |
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50mg |
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100mg |
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250mg |
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500mg |
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Other Sizes |
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靶点 |
human NNMT (IC50 = 1.8 µM); monkey NNMT (IC50 = 2.8 µM); mouse NNMT (IC50 = 5.0 µM)
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体外研究 (In Vitro) |
JBSNF-000088(6-甲酰胺烟酰胺)针对 U2OS 或分泌型 3T3L1 细胞的 IC50 值分别为 1.6 μM 和 6.3 μM [1]。
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体内研究 (In Vivo) |
JBSNF-000088(6-甲酰胺烟酰胺)(50 毫克/公斤;4 周粉末功效)在第 21 天表现出统计显着的体重减轻百分比,并导致糖尿病血糖显着降低 [1] JBSNF -000088(50 毫克/公斤;4 周粉末功效)临界强饲法;每天两次,持续 4 周)导致终点耐受性显着改善,并在第 28 天使终点耐受性正常化 [1]。 JBSNF-000088(1 mg/kg;静脉拓扑;持续时间 4 小时)在三个重复周期中产生 21 mL/min·kg 和 0.7 L/kg 的低组织清除率,静脉注射后半衰期非常短( 0.5 )[1 JBSNF-000088(10 mg/kg;灌胃;4 小时持续时间)导致 Cmax 为 3568 ng/mL,Tmax 值为 0.5 小时,表明快速腔内吸收和破坏,半衰期为0.4小时灌胃。
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动物实验 |
Animal/Disease Models: High-fat diet (HFD)-induced obese mice [1]
Doses: 50 mg/kg Route of Administration: Oral route for 4 weeks; the blocking bioavailability was found to be approximately 40% [1]. po (oral gavage) administration twice (two times) daily for four weeks Experimental Results: Demonstrated significant weight loss (%) and resulted in a significant reduction in postprandial blood glucose by the oral route on day 21. On day 28, there was a statistically significant improvement in oral glucose tolerance, which was normalized by po (oral gavage). Animal/Disease Models: C57BL/6 mice[1] Doses: 1 mg/kg (intravenous (iv) (iv)administration); 10 mg/kg (po (oral gavage)) (pharmacokinetic/PK/PK study) Route of Administration: intravenous (iv) (iv)administration and po (oral gavage) ; 4 hour Experimental Results: resulting in a low plasma clearance of 21 mL/min·kg, a steady-state volume of distribution of 0.7 L/kg, and a very short plasma half-life of 0.5 hrs (hrs (hours)) after intravenous (iv) (iv)injection. The results demonstrated that the Cmax was 3568 ng/mL, and the Tmax value was 0.5 hrs (hrs (hours)), indicating ra |
参考文献 |
[1]. Kannt A, et al. A small molecule inhibitor of Nicotinamide N-methyltransferase for the treatment of metabolic disorders. Sci Rep. 2018 Feb 26;8(1):3660.
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分子式 |
C7H8N2O2
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分子量 |
152.15
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精确质量 |
152.0586
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元素分析 |
C, 55.26; H, 5.30; N, 18.41; O, 21.03
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CAS号 |
7150-23-4
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外观&性状 |
Solid powder
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SMILES |
COC1=NC=C(C=C1)C(=O)N
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InChi Key |
KXDSMFBEVSJYRF-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C7H8N2O2/c1-11-6-3-2-5(4-9-6)7(8)10/h2-4H,1H3,(H2,8,10)
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化学名 |
6-methoxypyridine-3-carboxamide
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别名 |
JBSNF-000088; 6-Methoxynicotinamide; JBSNF 000088; JBSNF000088
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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) |
DMSO: ~30 mg/mL (~197.2 mM)
Ethanol: ~7 mg/mL (~46 mM) |
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制备储备液 | 1 mg | 5 mg | 10 mg | |
1 mM | 6.5725 mL | 32.8623 mL | 65.7246 mL | |
5 mM | 1.3145 mL | 6.5725 mL | 13.1449 mL | |
10 mM | 0.6572 mL | 3.2862 mL | 6.5725 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) 。
Profile of compound 1 (JBSNF-000088) in enzymatic and cell based assays. Sci Rep . 2018 Feb 26;8(1):3660. td> |
Structures of human and mouse NNMT in complex with SAH and N-methylated JBSNF-00088. Sci Rep . 2018 Feb 26;8(1):3660. td> |
JBSNF-000088: Pharmacokinetics profile and target engagement. Sci Rep . 2018 Feb 26;8(1):3660. td> |
Effect of 4-w treatment with JBSNF-000088 (50 mg kg−1 bid) in db/db mice. Sci Rep . 2018 Feb 26;8(1):3660. td> |