JBSNF-000088 (Synonyms: 6-Methoxynicotinamide, NSC 70628) |
| カタログ番号GC38012 |
ニコチンアミド (NA) の類似体である JBSNF-000088 (6-メトキシニコチンアミド) は、強力なニコチンアミド N-メチルトランスフェラーゼ (NNMT) 阻害剤であり、ヒト NNMT、サル NNMT、およびマウス NNMT に対して 1.8 μM、2.8 μM、および 5.0 μM の IC50 を示します。それぞれ。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 7150-23-4
Sample solution is provided at 25 µL, 10mM.
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JBSNF-000088 (6-Methoxynicotinamide), a analog of nicotinamide (NA), is a potent Nicotinamide N-methyltransferase (NNMT) inhibitor with IC50s of 1.8 µM, 2.8 µM, and 5.0 µM for human NNMT, monkey NNMT and mouse NNMT, respectively. JBSNF-000088 inhibits NNMT activity, reduces MNA levels and drives insulin sensitization, glucose modulation and body weight reduction in animal models of metabolic disease[1].
JBSNF-000088 (6-Methoxynicotinamide) has IC50 values are 1.6 and 6.3 µM for U2OS or differentiated 3T3L1 cells[1].
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[1]. 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[1]. 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[1]. JBSNF-000088 (10 mg/kg; oral gavage; for 4 hours) results in a Cmax of 3568 ng/mL with a Tmax 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%[1]. Animal Model: Mice with high fat diet (HFD)-induced obesity[1]
[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.
| Cas No. | 7150-23-4 | SDF | |
| 同義語 | 6-Methoxynicotinamide, NSC 70628 | ||
| Canonical SMILES | COc1ccc(cn1)C(=O)N | ||
| Formula | C7H8N2O2 | M.Wt | 152.15 |
| 溶解度 | DMSO: ≥ 100 mg/mL (657.25 mM); Water: 1 mg/mL (6.57 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 18 reference(s) in Google Scholar.)
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