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  3. Iptacopan

Iptacopan (Synonyms: LNP023)

Cat. No.: HY-127105 Purity: 99.86%
Handling Instructions

Iptacopan (LNP023) is a first-in-class, orally bioavailable, highly potent and highly selective factor B inhibitor with an IC50 value of 10 nM. Iptacopan shows direct, reversible, and high-affinity binding to human factor B with a KD of 7.9 nM. Iptacopan targets the underlying cause of complement 3 glomerulopathy (C3G).

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

Iptacopan Chemical Structure

Iptacopan Chemical Structure

CAS No. : 1644670-37-0

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 440 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 440 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 400 In-stock
Estimated Time of Arrival: December 31
10 mg USD 680 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1900 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2900 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

Iptacopan (LNP023) is a first-in-class, orally bioavailable, highly potent and highly selective factor B inhibitor with an IC50 value of 10 nM. Iptacopan shows direct, reversible, and high-affinity binding to human factor B with a KD of 7.9 nM. Iptacopan targets the underlying cause of complement 3 glomerulopathy (C3G)[1][2].

IC50 & Target

KD: 7.9 nM (factor B)[2]
IC50: 10 nM (factor B)[2]

In Vitro

Iptacopan (LNP023) demonstrates potent inhibition of alternative complement pathway (AP)-induced membrane attack complex (MAC) formation in 50% human serum (IC50 value of 130 nM)[2].
Iptacopan (LNP023) exhibits 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].

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

In Vivo

Iptacopan (LNP023; 20-180 mg/kg; oral administration) prevents KRN (150 μL)-induced arthritis in mice and is effective upon prophylactic and therapeutic dosing in an experimental model of membranous nephropathy in rats[2].
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) following oral administration (rat 30 and, dog 10 mg/kg)[3].
Iptacopan exhibits terminal elimination half-lives (T1/2; Wistar Han rats 7 h, beagle dogs 5.6 h) due to high plasma clearance (8, and 2 mL/min/kg respectively combined with large volumes of distribution (2.3, and 0.6 L/kg respectively) following intravenous administration (rat 1.0 and, dog 0.1 mg/kg)[3].

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

Animal Model: C57BL/6 mice with KRN-induced arthritis[2]
Dosage: 20, 60, and 180 mg/kg
Administration: Orally gavaged; twice a day (b.i.d.) for 14 days
Result: Blocked KRN-induced arthritis.
Clinical Trial
Molecular Weight

422.52

Formula

C₂₅H₃₀N₂O₄

CAS No.
SMILES

O=C(O)C1=CC=C([[email protected]]2N(CC3=C(OC)C=C(C)C4=C3C=CN4)CC[[email protected]](OCC)C2)C=C1

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 : 50 mg/mL (118.34 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3668 mL 11.8338 mL 23.6675 mL
5 mM 0.4734 mL 2.3668 mL 4.7335 mL
10 mM 0.2367 mL 1.1834 mL 2.3668 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 5 mg/mL (11.83 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 5 mg/mL (11.83 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 5 mg/mL (11.83 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.86%

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Keywords:

IptacopanLNP023LNP 023LNP-023Complement Systemfactor BalternativepathwayAPcomplementsystempathogenesisparoxysmalnocturnalhemoglobinuriaPNHatypicalhemolyticuremicsyndromeunderlyingcausecomplement 3glomerulopathyC3GInhibitorinhibitorinhibit

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