Pralnacasan (Synonyms: VX-740; HMR 3480)

Name: Pralnacasan
Brand: MedChemExpress
SKU: HY-19676
Rating: 4.5 (1 reviews)

Cat. No.: HY-19676 Purity: 99.83%: FAQs
Data Sheet SDS COA Handling Instructions

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Pralnacasan (VX-740) is a potent, selective, non-peptide and orally active interleukin-1β converting enzyme (ICE, caspase 1) inhibitor with a K_i of 1.4 nM. Pralnacasan inhibits proinflammatory cytokines IL-18, IL-1β , and IFN-γ. Pralnacasan has the potential for osteoarthritis and rheumatoid arthritis treatment.

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

Pralnacasan Chemical Structure

CAS No. : 192755-52-5

Size	Price	Stock	Quantity
1 mg	USD 520	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 1650	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 2700	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 5600	In-stock	Estimated Time of Arrival: December 31
50 mg		Get quote
100 mg		Get quote

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Based on 1 publication(s) in Google Scholar

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Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

Interleukin-1β converting enzyme

1.4 nM (Ki)

Cellular Effect

Cell Line	Type	Value	Description	References
THP-1	IC₅₀	120 nM Compound: 3	Inhibition of 1 ug/mL LPS-induced IL1-beta production in human monocytic cells after 4 hrs Inhibition of 1 ug/mL LPS-induced IL1-beta production in human monocytic cells after 4 hrs	[PMID: 16046125]

In Vivo

Pralnacasan (0 -50 mg/kg; oral gavage; twice a day; for 6 weeks; female Balb/c mice) treatment reduces joint damage. Pralnacasan treatment does not appear to affect the weight of the animals^[1].

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

Animal Model:	Female Balb/c mice induced with collagenase^[1]
Dosage:	0 mg/kg, 12.5 mg/kg, 25 mg/kg and 50 mg/kg
Administration:	Oral gavage; twice a day; for 6 weeks
Result:	Significantly ameliorated the histopathological damage of the medial knee joint compartments.

Molecular Weight

523.54

Formula

C₂₆H₂₉N₅O₇

CAS No.

192755-52-5

Appearance

Solid

Color

White to off-white

SMILES

O=C([C@@H]1CCCN2N1C([C@@H](NC(C3=NC=CC4=C3C=CC=C4)=O)CCC2=O)=O)N[C@@H](C5)[C@H](OCC)OC5=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 220 mg/mL (420.22 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	1.9101 mL	9.5504 mL	19.1007 mL
5 mM	0.3820 mL	1.9101 mL	3.8201 mL
10 mM	0.1910 mL	0.9550 mL	1.9101 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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: ≥ 5.5 mg/mL (10.51 mM); Clear solution

This protocol yields a clear solution of ≥ 5.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (55.0 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: ≥ 5.5 mg/mL (10.51 mM); Clear solution

This protocol yields a clear solution of ≥ 5.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (55.0 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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 5.5 mg/mL (10.51 mM); Clear solution

This protocol yields a clear solution of ≥ 5.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (55.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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: 99.83%

Select Batch:

Data Sheet (281 KB) SDS (252 KB)

COA (261 KB) LCMS (89 KB)

Handling Instructions (2659 KB)

References

[1]. Rudolphi K, et al. Pralnacasan, an inhibitor of interleukin-1beta converting enzyme, reduces joint damage in two murine models of osteoarthritis. Osteoarthritis Cartilage. 2003 Oct;11(10):738-46. [Content Brief]

[2]. Loher F, et al. The interleukin-1 beta-converting enzyme inhibitor pralnacasan reduces dextran sulfate sodium-induced murine colitis and T helper 1 T-cell activation. J Pharmacol Exp Ther. 2004 Feb;308(2):583-90. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	1.9101 mL	9.5504 mL	19.1007 mL	47.7518 mL
	5 mM	0.3820 mL	1.9101 mL	3.8201 mL	9.5504 mL
	10 mM	0.1910 mL	0.9550 mL	1.9101 mL	4.7752 mL
	15 mM	0.1273 mL	0.6367 mL	1.2734 mL	3.1835 mL
	20 mM	0.0955 mL	0.4775 mL	0.9550 mL	2.3876 mL
	25 mM	0.0764 mL	0.3820 mL	0.7640 mL	1.9101 mL
	30 mM	0.0637 mL	0.3183 mL	0.6367 mL	1.5917 mL
	40 mM	0.0478 mL	0.2388 mL	0.4775 mL	1.1938 mL
	50 mM	0.0382 mL	0.1910 mL	0.3820 mL	0.9550 mL
	60 mM	0.0318 mL	0.1592 mL	0.3183 mL	0.7959 mL
	80 mM	0.0239 mL	0.1194 mL	0.2388 mL	0.5969 mL
	100 mM	0.0191 mL	0.0955 mL	0.1910 mL	0.4775 mL

Pralnacasan Related Classifications

Inflammation/Immunology

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.

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Pralnacasan (Synonyms: VX-740; HMR 3480)

Customer Review

Pralnacasan Related Antibodies

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View All Caspase Isoform Specific Products:

Biological Activity

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References

Customer Review

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Complete Stock Solution Preparation Table

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