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| 1mg |
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Purity: =99.46%
| Targets |
SLU-PP-332 targets the estrogen-related receptors ERRα, ERRβ, and ERRγ. It is a pan-agonist with EC50 values of 98 nM, 230 nM, and 430 nM for ERRα, ERRβ, and ERRγ, respectively. Activation of these receptors regulates mitochondrial function and energy metabolism.
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| ln Vitro |
In vitro, SLU-PP-332 activates ERRα, ERRβ, and ERRγ with EC50 values of 98, 230, and 430 nM, respectively. It enhances mitochondrial function and cellular respiration in skeletal muscle cell lines. It also increases the proportion of type IIa oxidative skeletal muscle fibers.
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| ln Vivo |
In vivo, SLU-PP-332 enhances skeletal muscle oxidative capacity by increasing mitochondrial content and oxidative muscle fibers, resulting in improved stamina and fatigue resistance. It mimics aerobic exercise effects in metabolic tissues. The compound activates an acute aerobic exercise genetic response via inducing the expression of DDIT4.
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| Enzyme Assay |
The binding affinity and agonist activity of SLU-PP-332 are measured using cell-based reporter assays. EC50 values are determined from dose-response curves.
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| Cell Assay |
Cellular activity of SLU-PP-332 is evaluated in skeletal muscle cell lines. Mitochondrial function and cellular respiration are measured, and expression of oxidative genes is assessed.
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| Animal Protocol |
In vivo efficacy of SLU-PP-332 is evaluated in animal models of metabolic disease. Exercise endurance and muscle function are assessed, and mitochondrial content in muscle tissues is measured.
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| ADME/Pharmacokinetics |
SLU-PP-332 has a molecular formula of C18H14N2O2 and a molecular weight of 290.32. Its chemical name is (E)-4-Hydroxy-N'-(naphthalen-2-ylmethylene)benzohydrazide. It is a potent synthetic agonist of all ERR isoforms.
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| Toxicity/Toxicokinetics |
Toxicological data for SLU-PP-332 are limited. The compound is intended for research use only. Standard laboratory safety precautions should be followed when handling this compound.
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| References |
1. Billon C, Sitaula S, Banerjee S, Welch R, Elgendy B, Hegazy L, Oh TG, Kazantzis M, Chatterjee A, Chrivia J, Hayes ME, Xu W, Hamilton A, Huss JM, Zhang L, Walker JK, Downes M, Evans RM, Burris TP. Synthetic ERRα/β/γ Agonist Induces an ERRα-Dependent Acute Aerobic Exercise Response and Enhances Exercise Capacity. ACS Chem Biol. 2023 Apr 21;18(4):756-771. doi: 10.1021/acschembio.2c00720. Epub 2023 Mar 29. PMID: 36988910. 2. https://www.ahajournals.org/doi/10.1161/circ.144.suppl_1.9682 3. https://www.ncbi.nlm.nih.gov/geo/query/acc.cgi?acc=GSM4663186
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| Additional Infomation |
SLU-PP-332 is a pan-ERR agonist that mimics the effects of aerobic exercise. It enhances muscle function and has potential for studying metabolic diseases. It is a valuable tool for studying ERR biology and energy metabolism and offers opportunities for researching metabolic ailments and enhancing muscle functionality.
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| Molecular Formula |
C18H14N2O2
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|---|---|
| Molecular Weight |
290.315964221954
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| Exact Mass |
290.11
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| Elemental Analysis |
Elemental Analysis:Exact Mass:Elemental Analysis: C, 74.47; H, 4.86; N, 9.65; O, 11.02
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| CAS # |
303760-60-3
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| PubChem CID |
5338394
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| Appearance |
White to off-white solid powder
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| LogP |
3.7
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
22
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| Complexity |
402
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C(NN=CC1=CC=C2C(=C1)C=CC=C2)(=O)C1=CC=C(O)C=C1
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| InChi Key |
RNZIMBFHRXYRLL-XDHOZWIPSA-N
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| InChi Code |
InChI=1S/C18H14N2O2/c21-17-9-7-15(8-10-17)18(22)20-19-12-13-5-6-14-3-1-2-4-16(14)11-13/h1-12,21H,(H,20,22)/b19-12+
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| Chemical Name |
(E)-4-hydroxy-N'-(naphthalen-2-ylmethylene)benzohydrazide
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| Synonyms |
SLU-PP-332; SLU PP 332
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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 : ~125 mg/mL (~430.56 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.4445 mL | 17.2224 mL | 34.4448 mL | |
| 5 mM | 0.6889 mL | 3.4445 mL | 6.8890 mL | |
| 10 mM | 0.3444 mL | 1.7222 mL | 3.4445 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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