| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
micro-Calpain (Ki = 0.26 +/- 0.03 microM) and m-calpain (Ki = 5.33 +/- 0.77 microM), with approximately 20-fold selectivity for micro-calpain. PD 151746 is a cell-permeable, competitive calpain inhibitor.
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|---|---|
| ln Vitro |
PD 151746 inhibits micro-calpain with a Ki of 0.26 microM, showing about 20-fold selectivity over m-calpain (Ki = 5.33 microM). It decreases oxLDL-induced cytotoxicity in cell culture models and inhibits calpain-dependent cleavage of substrates such as alpha-spectrin, making it a standard tool for studying calpain function in vitro.
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| ln Vivo |
In vivo activity data for PD 151746 are limited; it is primarily used as an in vitro and cell-based research tool. Some studies have investigated its effects in models of cardiovascular disorders and hypertension. Further research is ongoing to explore its potential therapeutic applications.
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| Enzyme Assay |
For enzyme inhibition assays, micro-calpain and m-calpain are activated by calcium in the presence of a fluorogenic substrate (e.g., Suc-LLVY-AMC or casein). PD 151746 is added at concentrations ranging from 0.01-100 microM. Proteolytic activity is measured by fluorescence (excitation 380 nm, emission 460 nm) or absorbance, and Ki values are calculated from dose-response curves.
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| Cell Assay |
For cellular assays, HMEC-1 or other cells are cultured in dishes and exposed to oxLDL (200 microg/mL) or staurosporine (200 nM) for up to 20 hours. PD 151746 is co-treated at 20 microM. Cells are harvested for analysis of calpain activity, substrate cleavage (e.g., alpha-spectrin), and cell viability (e.g., MTT or LDH release assays).
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| Animal Protocol |
For animal studies, PD 151746 is administered via intraperitoneal (i.p.) injection or oral gavage (typically 1-30 mg/kg). Formulations commonly use DMSO/PEG300/Tween-80/saline. Tissues are collected for measurement of calpain activity, assessment of protein cleavage, and evaluation of tissue damage or functional outcomes.
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| ADME/Pharmacokinetics |
PD 151746 is cell-permeable with moderate solubility in DMSO (≥50 mg/mL). For in vivo administration, it can be formulated using 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline. Detailed pharmacokinetic parameters (half-life, bioavailability) have not been extensively reported; it is primarily used as an in vitro tool.
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| Toxicity/Toxicokinetics |
Comprehensive toxicological studies for PD 151746 have not been published. As a research chemical with sub-micromolar calpain inhibitory activity, it should be handled with standard laboratory precautions. It is not intended for human therapeutic use.
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| References |
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| Additional Infomation |
PD 151746 (CAS: 181765-30-0) has molecular formula C11H8FNO2S and molecular weight 237.25. It is a highly useful tool for dissecting the distinct roles of micro-calpain versus m-calpain in cellular processes, particularly in apoptosis, neurodegeneration, and oxidative stress. It is not an approved drug.
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| Molecular Formula |
C11H8FNO2S
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|---|---|
| Molecular Weight |
237.25
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| Exact Mass |
237.025
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| CAS # |
181765-30-0
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| PubChem CID |
5353866
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| Appearance |
Light yellow to brown solid powder
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| Density |
1.5±0.1 g/cm3
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| Boiling Point |
481.4±45.0 °C at 760 mmHg
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| Flash Point |
245.0±28.7 °C
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| Vapour Pressure |
0.0±1.3 mmHg at 25°C
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| Index of Refraction |
1.756
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| LogP |
3.28
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
16
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| Complexity |
321
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC2=C(C=C1F)C(=CN2)/C=C(/C(=O)O)\S
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| InChi Key |
HWMQHECFXSVZGN-KMKOMSMNSA-N
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| InChi Code |
InChI=1S/C11H8FNO2S/c12-7-1-2-9-8(4-7)6(5-13-9)3-10(16)11(14)15/h1-5,13,16H,(H,14,15)/b10-3-
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| Chemical Name |
(Z)-3-(5-fluoro-1H-indol-3-yl)-2-sulfanylprop-2-enoic acid
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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: 50 mg/mL (210.75 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (8.77 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 (8.77 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 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.2150 mL | 21.0748 mL | 42.1496 mL | |
| 5 mM | 0.8430 mL | 4.2150 mL | 8.4299 mL | |
| 10 mM | 0.4215 mL | 2.1075 mL | 4.2150 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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