PD 145305 |
Catalog No.GC13450
One-Click Copy Product Info
|
selective inhibitor of calpains
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 90536-15-5
Sample solution is provided at 25 µL, 10mM.
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PD 145305 is an inactive analog of PD 150606, a potent and selective calpains inhibitor [1].
Calpain is a class of cytosolic cysteine protease that is activated by elevated intracellular calcium. Overactivation of calpain has been implicated in the pathophysiology of several degenerative conditions, including stroke, myocardial ischemia, neuromuscular degeneration, and cataract formation [1].
PD 145305 is an inactive analog of PD 150606, a potent and selective calpains inhibitor. PD 150606, an alpha-mercaptoacrylate derivative, inhibited μ-calpain and m-calpain with Ki values of 0.21 and 0.37 μM, respectively. PD 145305 was inactive at concentrations up to 500 μM. In human leukemic Molt-4 cells, PD150606 inhibited a-spectrin proteolysis in a dose-dependent way and virtually eliminated the formation of the 145-kDa fragment at 10 μM, whereas PD145305 did not attenuate a-spectrin breakdown product formation. In fetal rat cerebrocortical cultures subjected to a combination of hypoxia and hypoglycemia, PD150606 significantly inhibited the release of lactate dehydrogenase, whereas PD145305 was ineffective. PD150606, but not PD145305, was found to make cerebral glutamatergic neurons more resistant to hypoxic/hypoglycemic challenge [1].
Reference:
[1]. Wang KK, Nath R, Posner A, et al. An alpha-mercaptoacrylic acid derivative is a selective nonpeptide cell-permeable calpain inhibitor and is neuroprotective. Proc Natl Acad Sci U S A. 1996 Jun 25;93(13):6687-92.
| Cas No. | 90536-15-5 | SDF | |
| Chemical Name | α-mercapto-benzenepropanoic acid | ||
| Canonical SMILES | OC(C(S)CC1=CC=CC=C1)=O | ||
| Formula | C9H10O2S | M.Wt | 182.2 |
| Solubility | ≤20mg/ml in ethanol;20mg/ml in DMSO;20mg/ml in dimethyl formamide | 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 | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 5.4885 mL | 27.4424 mL | 54.8847 mL |
| 5 mM | 1.0977 mL | 5.4885 mL | 10.9769 mL |
| 10 mM | 548.8 μL | 2.7442 mL | 5.4885 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
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 saline, 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
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 29 reference(s) in Google Scholar.)