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Iptacopan hydrochloride

Catalog No. T9189 CAS 1646321-63-2

Synonyms: Iptacopan HCl, LNP023 hydrochloride

Iptacopan hydrochloride (LNP023 hydrochloride) is an orally bioavailable, highly potent and highly selective factor B inhibitor with an IC50 of 10 nM. Iptacopan hydrochloride shows direct, reversible, and high-affinity binding to human factor B with a KD of 7.9 nM.

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Iptacopan hydrochloride Chemical Structure

Iptacopan hydrochloride, CAS 1646321-63-2

Pack Size	Availability	Price/USD
1 mg	In stock	$ 155.00
5 mg	In stock	$ 328.00
10 mg	In stock	$ 563.00
25 mg	In stock	$ 879.00
50 mg	In stock	$ 1,190.00
100 mg	In stock	$ 1,620.00
1 mL * 10 mM (in DMSO)	In stock	$ 333.00

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Purity: 99.84%

Purity: 98.83%

Purity: 98.32%

ee: 99.12%

Purity: 97.31%

Purity: 97.03%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Iptacopan hydrochloride (LNP023 hydrochloride) is an orally bioavailable, highly potent and highly selective factor B inhibitor with an IC50 of 10 nM. Iptacopan hydrochloride shows direct, reversible, and high-affinity binding to human factor B with a KD of 7.9 nM.
Targets&IC50	FB:10 nM, FB:7.9 nM(KD)
In vitro	LNP023 demonstrates excellent selectivity over other proteases affording IC50 values of >30 μM across a panel of 41 human proteases, including the AP protein factor D (>100 μM)[3].
In vivo	LNP023 (20-180 mg/kg; oral administration) is effective upon prophylactic and therapeutic dosing in an experimental model of membranous nephropathy in rats and prevents KRN (150 μL)-induced arthritis in mice[2]. After oral administration (rat 30 and, dog 10 mg/kg), LNP023 exhibits moderate half-lives (T1/2; Wistar Han rats 3.4 h, beagle dogs 5.5 h) and Cmax (Wistar Han rats 410 nM, beagle dogs 2200 nM)[3].

Synonyms	Iptacopan HCl, LNP023 hydrochloride
Molecular Weight	458.98
Formula	C25H31ClN2O4
CAS No.	1646321-63-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: 50 mg/mL (108.94 mM), Sonification and heating are recommended.

DMSO: 250 mg/mL (544.69 mM), Sonification is recommended.

References and Literature

1. Dimitrios C Mastellos, et al. Expanding Complement Therapeutics for the Treatment of Paroxysmal Nocturnal Hemoglobinuria. Semin Hematol. 2018 Jul;55(3):167-175. 2. Anna Schubart, et al. Small-molecule Factor B Inhibitor for the Treatment of Complement-Mediated Diseases. Proc Natl Acad Sci U S A. 2019 Apr 16;116(16):7926-7931. 3. Nello Mainolfi, et al. Discovery of 4-((2 S,4 S)-4-Ethoxy-1-((5-methoxy-7-methyl-1 H-indol-4-yl)methyl)piperidin-2-yl)benzoic Acid (LNP023), a Factor B Inhibitor Specifically Designed To Be Applicable to Treating a Diverse Array of Complement Mediated Diseases. J Med Chem. 2020 Jun 11;63(11):5697-5722.

Related compound libraries

This product is contained In the following compound libraries：

Highly Selective Inhibitor Library Inhibitor Library Drug Repurposing Compound Library Bioactive Compound Library NO PAINS Compound Library Immunology/Inflammation Compound Library Clinical Compound Library Orally Active Compound Library Bioactive Compounds Library Max

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Related compounds with same targets

W-54011 CP-289 Compstatin 3-Phenoxybenzaldehyde Danicopan Eculizumab PMX 53 acetate(219639-75-5 free base) EG01377 2HCl

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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 add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Keywords

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