6-甲氧基-3-吡啶羧胺

生物活性靶点体外研究体内研究 6-甲氧基-3-吡啶羧胺试剂级价格

6-甲氧基-3-吡啶羧胺

CAS号:7150-23-4
英文名:6-Methoxynicotinamide
中文名:6-甲氧基-3-吡啶羧胺
CBNumber:CB22463564
分子式:C7H8N2O2
分子量:152.15
MOL File:7150-23-4.mol

6-甲氧基-3-吡啶羧胺化学性质

熔点 :178-180°C
沸点 :301.6±22.0 °C(Predicted)
密度 :1.213±0.06 g/cm3(Predicted)
储存条件 :-20°C Freezer
溶解度 :DMSO (Slightly), Methanol (Slightly)
形态 :Solid
酸度系数(pKa) :15.17±0.50(Predicted)
颜色 :Off-White to Pale Beige
InChI :InChI=1S/C7H8N2O2/c1-11-6-3-2-5(4-9-6)7(8)10/h2-4H,1H3,(H2,8,10)
InChIKey :KXDSMFBEVSJYRF-UHFFFAOYSA-N
SMILES :C1=NC(OC)=CC=C1C(N)=O

安全信息

海关编码 :2933399990

6-甲氧基-3-吡啶羧胺性质、用途与生产工艺

生物活性 JBSNF-000088 (6-Methoxynicotinamide)是一种烟酰胺（NA）的类似物，是 Nicotinamide N-methyltransferase (NNMT) 的有效抑制剂，对 human NNMT(hNNMT)、monkey NNMT (mkNNMT) 和 mouse NNMT (mNNMT)的IC50值为1.8 µM、2.8 µM 和 5.0 µM。
靶点
Target Value
hNNMT
(Cell-free assay) 1.8 μM
mkNNM
(Cell-free assay) 2.8 μM
mNNMT
(Cell-free assay) 5.0 μM
体外研究

JBSNF-000088 (6-Methoxynicotinamide) has IC ₅₀ values are 1.6 and 6.3 µM for U2OS or differentiated 3T3L1 cells.

体内研究

JBSNF-000088 (6-Methoxynicotinamide) (50 mg/kg; oral route of administration for four weeks) shows statistically significant reduction in body weight (%) and leads to a statistically significant reduction in fed blood glucose on day 21.
JBSNF-000088 (50 mg/kg; oral gavage administration; twice daily for four weeks) leads to a statistically significant improvement in oral glucose tolerance on day 28 with glucose tolerance being normalized.
JBSNF-000088 (1 mg/kg; intravenous administration; for 4 hours) results in low plasma clearance of 21 mL/min▪kg and the volume of distribution at steady state of 0.7 L/kg, a very short plasma half-life of 0.5 hours upon intravenous administration.
JBSNF-000088 (10 mg/kg; oral gavage; for 4 hours) results in a Cmax of 3568 ng/mL with a T _max value of 0.5 hours, indicating rapid absorption in the intestine, and half-life of 0.4 hours by oral gavage. The oral bioavailability is found to be approximately 40%.

Animal Model:	Mice with high fat diet (HFD)-induced obesity
Dosage:	50 mg/kg
Administration:	Oral route of administration for four weeks; oral gavage administration and twice daily for four weeks
Result:	Showed statistically significant reduction in body weight (%) and led to a statistically significant reduction in fed blood glucose on day 21 by oral route of administration. Led to a statistically significant improvement in oral glucose tolerance on day 28 with glucose tolerance being normalized by oral gavage administration.

Animal Model:	C57BL/6 mice
Dosage:	1 mg/kg (Intravenous administration);10 mg/kg (oral gavage)(Pharmacokinetic Study)
Administration:	Intravenous administration and oral gavage; for 4 hours
Result:	Resulted in low plasma clearance of 21 mL/min▪kg and the volume of distribution at steady state of 0.7 L/kg, a very short plasma half-life of 0.5 h upon intravenous administration. Resulted in a Cmax of 3568 ng/mL with a T _max value of 0.5 hours, indicating rapid absorption in the intestine, and half-life of 0.4 hours by oral gavage.