1. Immunology/Inflammation
  2. Complement System
  3. LNP023 hydrochloride

LNP023 hydrochloride 

Cat. No.: HY-127105A Purity: 98.10% ee.: 99.58%
Handling Instructions

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

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LNP023 hydrochloride Chemical Structure

LNP023 hydrochloride Chemical Structure

CAS No. : 1646321-63-2

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Description

LNP023 hydrochloride is an orally bioavailable, highly potent and highly selective factor B inhibitor. LNP023 shows direct, reversible, and high-affinity binding to human factor B with a KD of 7.9 nM. LNP023 inhibits factor B with an IC50 value of 10 nM[1][2].

IC50 & Target

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

In Vitro

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].
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].

In Vivo

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].
LNP023 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].

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.
Molecular Weight

458.98

Formula

C₂₅H₃₁ClN₂O₄

CAS No.

1646321-63-2

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.[H]Cl

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 : 200 mg/mL (435.75 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1787 mL 10.8937 mL 21.7874 mL
5 mM 0.4357 mL 2.1787 mL 4.3575 mL
10 mM 0.2179 mL 1.0894 mL 2.1787 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 (10.89 mM); Clear solution

  • 2.

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

    Solubility: ≥ 5 mg/mL (10.89 mM); Clear solution

  • 3.

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

    Solubility: ≥ 5 mg/mL (10.89 mM); Clear solution

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

LNP023LNP 023LNP-023Complement Systemfactor BalternativepathwayAPcomplementsystempathogenesisparoxysmalnocturnalhemoglobinuriaPNHatypicalhemolyticuremicsyndromeInhibitorinhibitorinhibit

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LNP023 hydrochloride
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HY-127105A
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