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Purity: ≥98%
KL1333, a novel NAD+ modulator, is a potent, orally bioavailable and small organic molecule with the potential to treat Mitochondrial encephalomyopathy, lactic acidosis, and stroke-like episodes (MELAS). It reacts with NAD(P)H : quinone oxidoreductase 1 (NQO1) as a substrate, resulting in increases in intracellular NAD+ levels via NADH oxidation. KL-1333 Improves Energy Metabolism and Mitochondrial Dysfunction in MELAS Fibroblasts. Elevated NAD+ levels induced by KL1333 triggered the activation of SIRT1 and AMPK, and subsequently activated PGC-1α in these cells. In MELAS fibroblasts, KL1333 increased ATP levels and decreased lactate and ROS levels, which are often dysregulated in this disease. In addition, mitochondrial functional analyses revealed that KL1333 increased mitochondrial mass, membrane potential, and oxidative capacity. These results indicate that KL1333 improves mitochondrial biogenesis and function, and thus represents a promising therapeutic agent for the treatment of MELAS. Mitochondrial encephalomyopathy, lactic acidosis, and stroke-like episodes (MELAS), one of the most common maternally inherited mitochondrial diseases, is caused by mitochondrial DNA mutations that lead to mitochondrial dysfunction. Several treatment options exist, including supplementation with CoQ10, vitamins, and nutrients, but no treatment with proven efficacy is currently available.
| ln Vitro |
KL1333 is NAD A powerful regulator within cells, NAD It is essential for the cellular energy awakening coenzyme. PGC-1α is activated by SIRT1 and AMPK, which are activated by elevated NAD+ levels[1].
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| References |
[1]. Seo KS, et al. KL1333, a Novel NAD+ Modulator, Improves Energy Metabolism and Mitochondrial Dysfunction in MELAS Fibroblasts. Front Neurol. 2018;9:552. Published 2018 Jul 5.
[2]. Lee HS, et al. KL1333, a derivative of β-lapachone, protects against cisplatin-induced ototoxicity in mouse cochlear cultures. Biomed Pharmacother. 2020;126:110068. |
| Molecular Formula |
C14H12N2O2
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| Molecular Weight |
240.257283210754
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| CAS # |
1800405-30-4
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| SMILES |
O=C(C1=C2N=C(C(C)C)N1)C(C3=C2C=CC=C3)=O
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| Chemical Name |
2-(1-Methylethyl)-3H-naphth(1,2-d)imidazole-4,5-dione
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| Synonyms |
KL-1333; KL 1333; KL1333;
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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 : ~100 mg/mL (~416.22 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (10.41 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 25.0 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: ≥ 2.5 mg/mL (10.41 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), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.1622 mL | 20.8108 mL | 41.6216 mL | |
| 5 mM | 0.8324 mL | 4.1622 mL | 8.3243 mL | |
| 10 mM | 0.4162 mL | 2.0811 mL | 4.1622 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.
 KL1333 increases the intracellular NAD+/NADH ratio.
KL1333 induces PGC-1α activation.Front Neurol. 2018; 9: 552. |
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 KL1333 activates SIRT1 and AMPK.
KL1333 regulates intracellular ATP, lactate, and ROS levels in MELAS fibroblasts.Front Neurol. 2018; 9: 552. |
 KL1333 activates AMPK in a NQO1-dependent manner.
KL1333 increases the NAD+/NADH ratio and activates SIRT1, AMPK, and PGC-1α in MELAS fibroblasts.Front Neurol. 2018; 9: |
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