| Size | Price | Stock | Qty |
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Purity: ≥98%
JBSNF-000088 (JBSNF 000088; JBSNF000088), a nicotinamide analog, is a potent inhibitor of Nicotinamide N-methyltransferase (NNMT) with the potential to treat metabolic disorders such as obesity. JBSNF-000088 treatment reduced body weight, improved insulin sensitivity, and normalized glucose tolerance to the level of lean control mice in mice with obesity induced by high fat diet (HFD).
| Targets |
human NNMT (IC50 = 1.8 µM); monkey NNMT (IC50 = 2.8 µM); mouse NNMT (IC50 = 5.0 µM)
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| ln Vitro |
JBSNF-000088 (6-carboxamide nicotinamide) has IC50 values of 1.6 μM and 6.3 μM against U2OS or secreted 3T3L1 cells, respectively [1].
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| ln Vivo |
JBSNF-000088 (6-carboxamide nicotinamide) (50 mg/kg; 4 weeks powder efficacy) demonstrated statistically significant % weight loss at day 21 and resulted in significant reductions in diabetic blood glucose [1] JBSNF -000088 (50 mg/kg; borderline gavage; twice daily for 4 weeks) resulted in significant improvements in endpoint tolerance and normalization of endpoint tolerance on day 28 [1]. JBSNF-000088 (1 mg/kg; intravenous topology; duration 4 hours) resulted in a low weave clearance of 21 mL/min·kg and 0.7 L/kg over three repeated cycles, with a very short post-intravenous half-life (0.5 )[1 JBSNF-000088 (10 mg/kg; intragastric gavage; 4 hours duration) resulted in a Cmax of 3568 ng/mL and a Tmax value of 0.5 hours, indicating rapid intraluminal absorption and destruction, with a half-life of 0.4 hours by intragastric gavage .
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| Animal Protocol |
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 |
| References |
[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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| Molecular Formula |
C7H8N2O2
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|---|---|
| Molecular Weight |
152.15
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| Exact Mass |
152.0586
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| Elemental Analysis |
C, 55.26; H, 5.30; N, 18.41; O, 21.03
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| CAS # |
7150-23-4
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| Related CAS # |
7150-23-4
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| Appearance |
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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| Chemical Name |
6-methoxypyridine-3-carboxamide
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| Synonyms |
JBSNF-000088; 6-Methoxynicotinamide; JBSNF 000088; JBSNF000088
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
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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| Solubility (In Vitro) |
DMSO: ~30 mg/mL (~197.2 mM)
Ethanol: ~7 mg/mL (~46 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (13.67 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.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (13.67 mM) (saturation unknown) 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. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 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. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (13.67 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 2.94 mg/mL (19.32 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication (<60°C). |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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