PD 151746

Name: PD 151746
Brand: MedChemExpress
SKU: HY-19749
Rating: 5.0 (6 reviews)

Cat. No.: HY-19749 Purity: ≥95.0%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

PD151746 is a calpain inhibitor, shows a 20-fold selectivity for u-calpain (Ki = 0.

For research use only. We do not sell to patients.

PD 151746 Chemical Structure

CAS No. : 181765-30-0

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 79	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 79	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 72	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 120	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 240	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 384	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 624	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Based on 6 publication(s) in Google Scholar

Other Forms of PD 151746:

(Rac)-PD 151746 Get quote

6 Publications Citing Use of MCE PD 151746

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Description

PD151746 is a calpain inhibitor, shows a 20-fold selectivity for u-calpain (Ki = 0.26 ± 0.03 μM) over m-calpain (Ki = 5.33 ± 0.77 μM). IC50 value: 0.26 ± 0.03 μM (Ki, for μ-calpain), 5.33 ± 0.77 μM (Ki, for m-calpain) [1] Target: calpain in vitro: The μ-calpain inhibitor PD 151746 decreases oxLDL-induced cytotoxicity. [2]

Molecular Weight

237.25

Formula

C₁₁H₈FNO₂S

CAS No.

181765-30-0

Appearance

Solid

Color

Light yellow to brown

SMILES

O=C(O)/C(S)=C/C1=CNC2=C1C=C(F)C=C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL (210.75 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (8.77 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (8.77 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 95.03%

Select Batch:

Data Sheet (277 KB) SDS (252 KB)

COA (252 KB) HNMR (272 KB) LCMS (297 KB)

Handling Instructions (2659 KB)

References

[1]. Wang KK, 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. [Content Brief]

[2]. P?rn-Ares MI, et al. Oxidized low-density lipoprotein induces calpain-dependent cell death and ubiquitination of caspase 3 in HMEC-1 endothelial cells. Biochem J. 2003 Sep 1;374(Pt 2):403-11. [Content Brief]

Cell Assay

HMEC-1 cells cultured in 60-mm-diameter culture dishes were left untreated or were exposed to 200 μg/ml oxLDL for 20 h or to 200 nM staurosporine (STS) for 4 h. Along with oxLDL, some cells were co-treated with PD 151746 (20 μM) or BAF (50 μM). Thereafter, the cells were harvested and processed for Western blotting as described in the Experimental section. The PVDF membrane was probed with an anti-α-fodrin mAb. The absorbance (A) of the 150 and 120 kDa bands was scanned, and the ratio of the two values (A 150/A 120) is indicated below relevant samples. The illustrated blot is representative of five separate experiments[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

[1]. Wang KK, 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. [Content Brief]

[2]. P?rn-Ares MI, et al. Oxidized low-density lipoprotein induces calpain-dependent cell death and ubiquitination of caspase 3 in HMEC-1 endothelial cells. Biochem J. 2003 Sep 1;374(Pt 2):403-11. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	4.2150 mL	21.0748 mL	42.1496 mL	105.3741 mL
	5 mM	0.8430 mL	4.2150 mL	8.4299 mL	21.0748 mL
	10 mM	0.4215 mL	2.1075 mL	4.2150 mL	10.5374 mL
	15 mM	0.2810 mL	1.4050 mL	2.8100 mL	7.0249 mL
	20 mM	0.2107 mL	1.0537 mL	2.1075 mL	5.2687 mL
	25 mM	0.1686 mL	0.8430 mL	1.6860 mL	4.2150 mL
	30 mM	0.1405 mL	0.7025 mL	1.4050 mL	3.5125 mL
	40 mM	0.1054 mL	0.5269 mL	1.0537 mL	2.6344 mL
	50 mM	0.0843 mL	0.4215 mL	0.8430 mL	2.1075 mL
	60 mM	0.0702 mL	0.3512 mL	0.7025 mL	1.7562 mL
	80 mM	0.0527 mL	0.2634 mL	0.5269 mL	1.3172 mL
	100 mM	0.0421 mL	0.2107 mL	0.4215 mL	1.0537 mL

PD 151746 Related Classifications

Cardiovascular Disease

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PD 151746181765-30-0PD151746PD-151746ProteasomeInhibitorinhibitorinhibit

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PD 151746

Customer Review

Other Forms of PD 151746:

PD 151746 Related Antibodies

6 Publications Citing Use of MCE PD 151746

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

PD 151746 Related Classifications

Keywords:

Your Recently Viewed Products:

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