1. Metabolic Enzyme/Protease
  2. Endogenous Metabolite
  3. JBSNF-000088

JBSNF-000088 (Synonyms: 6-Methoxynicotinamide)

Cat. No.: HY-112584 Purity: >97.0%
Handling Instructions

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.

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JBSNF-000088 Chemical Structure

JBSNF-000088 Chemical Structure

CAS No. : 7150-23-4

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 55 In-stock
Estimated Time of Arrival: December 31
100 mg USD 50 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

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].

IC50 & Target

IC50: 1.8 µM (human NNMT), 2.8 µM (monkey NNMT) and 5.0 µM (mouse NNMT)[1]

In Vitro

JBSNF-000088 (6-Methoxynicotinamide) has IC50 values are 1.6 and 6.3 µM for U2OS or differentiated 3T3L1 cells[1].

In Vivo

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]
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[1]
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 Tmax value of 0.5 hours, indicating rapid absorption in the intestine, and half-life of 0.4 hours by oral gavage.
Molecular Weight

152.15

Formula

C₇H₈N₂O₂

CAS No.

7150-23-4

SMILES

COc1ccc(cn1)C(=O)N

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (657.25 mM)

H2O : 1 mg/mL (6.57 mM; Need ultrasonic)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (16.43 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (16.43 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (16.43 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: >97.0%

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Product name:
JBSNF-000088
Cat. No.:
HY-112584
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