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Iptacopan

Name: Iptacopan
Brand: TargetMol
SKU: T11864
Price: 51 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T11864Cas No. 1644670-37-0

Alias LNP023

Iptacopan (LNP023) is an inhibitor with high affinity to factor B, with a KD value of 7.9 nM and an IC50 value of 10 nM.

Iptacopan

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Purity: 99.73%

Catalog No. T11864Alias LNP023Cas No. 1644670-37-0

Iptacopan (LNP023) is an inhibitor with high affinity to factor B, with a KD value of 7.9 nM and an IC50 value of 10 nM.

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$51	In Stock	In Stock
5 mg	$123	In Stock	In Stock
10 mg	$205	In Stock	In Stock
25 mg	$370	In Stock	In Stock
50 mg	$619	In Stock	In Stock
100 mg	$1,020	In Stock	In Stock
200 mg	$1,380	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$135	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Purity:99.73%

Appearance:Solid

Color:Yellow

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COA HNMR LCMS

Product Introduction

Iptacopan AI Summary

Iptacopan exhibits bioactivity related to serine protease factor B, demonstrating binding affinity and inhibition across various assays. It shows strong inhibition of human and mouse serine protease factor B at different concentrations and exhibits inhibitory effects on C3d+iC3b formation in plasma and ocular tissues of mouse models of complement activation, suggesting potential anti-inflammatory properties. Additionally, Iptacopan displays moderate protein binding across different species and possesses favorable pharmacokinetic properties, including oral bioavailability and clearance in mice..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	Iptacopan (LNP023) is an inhibitor with high affinity to factor B, with a KD value of 7.9 nM and an IC50 value of 10 nM.
Targets&IC50	Chymase:> 100 μM, CFB:0.012 μM, COX-1 receptor:> 30 μM, COX-2 receptor:> 30 μM, Cathepsin K:> 100 μM, Cathepsin G:> 100 μM, Chymotrypsin:> 100 μM, CFB:0.01 μM, Cathepsin L:48 μM, Cathepsin H:> 100 μM, Cathepsin S:> 30 μM, DPP4:> 100 μM, Apopain:> 100 μM, Blood-coagulation factor Xa:> 100 μM, DPP2:> 100 μM
In vitro	METHODS: Blood from three patients was analyzed in 2-14 replicates and Iptacopan was used at 1 μM. Hemolysis of PNH erythrocytes was determined by FACS analysis. RESULTS LNP023 can block C3 deposition on the surface of CD59-negative red blood cells. [2]
In vivo	METHODS: Iptacopan (LNP023) was tested in KRN-induced arthritis at doses of 20, 60 and 180 mg/kg by injection twice daily. RESULTS Comprehensive disease protection was observed at 60 and 180 mg/kg, and LNP023 significantly inhibited complement activation in joints at all doses, with significant reductions in Ba, C3d, and C5a levels. [1] METHODS: Sixty-eight patients with biopsy-proven C3G, decreased C3 (<77 mg/dl), proteinuria ≥1.0 g/g), and estimated glomerular filtration rate (eGFR) ≥30 ml/min per 1.73 m2 were recruited. Patients will be randomized 1:1 to receive iptacopan 200 mg twice daily or placebo for 6 months, followed by open-label treatment of all patients with iptacopan 200 mg twice daily for 6 months. RESULTS Iptacopan slows disease progression by inhibiting FB and preventing excessive activation of AP and may become one of the first targeted therapies available for C3G patients. [3]
Synonyms	LNP023

Chemical Properties

Molecular Weight	422.52
Formula	C₂₅H₃₀N₂O₄
Cas No.	1644670-37-0
Smiles	CCO[C@H]1CCN(Cc2c(OC)cc(C)c3[nH]ccc23)[C@@H](C1)c1ccc(cc1)C(O)=O
Relative Density.	1.25 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 255 mg/mL (603.52 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5 mg/mL (11.83 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.3668 mL	11.8338 mL	23.6675 mL	118.3376 mL
5 mM	0.4734 mL	2.3668 mL	4.7335 mL	23.6675 mL
10 mM	0.2367 mL	1.1834 mL	2.3668 mL	11.8338 mL
20 mM	0.1183 mL	0.5917 mL	1.1834 mL	5.9169 mL
50 mM	0.0473 mL	0.2367 mL	0.4734 mL	2.3668 mL
100 mM	0.0237 mL	0.1183 mL	0.2367 mL	1.1834 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc