Iptacopan - 10mM in DMSO , Complement factor B inhibitor, CAS No.1644670-37-0, Complement factor B inhibitor

CAS: 1644670-37-0 Cat. No.: I655394 Summenformel: C₂₅H₃₀N₂O₄ Molekulargewicht: 422.52 EG-Nummer: 189-013-1 PubChem CID: 90467622

GRADE & PURITY 10mM in DMSO

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Übersicht

Iptacopan (LNP023) is a first-in-class, orally bioavailable, highly potent and highly selective factor B inhibitor with an IC 50 value of 10 nM. Iptacopan shows direct, reversible, and high-affinity binding to human factor B with a K D of 7.9 nM. Iptacopan targets the underlying cause of complement 3 glomerulopathy (C3G)

In Vitro

Iptacopan (LNP023) demonstrates potent inhibition of alternative complement pathway (AP)-induced membrane attack complex (MAC) formation in 50% human serum (IC 50 value of 130 nM). Iptacopan (LNP023) exhibits excellent selectivity over other proteases affording IC 50 values of >30 μM across a panel of 41 human proteases, including the AP protein factor D (>100 μM). 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. LNP023 exhibits moderate half-lives (T 1/2 ; Wistar Han rats 3.4 h, beagle dogs 5.5 h) and C max (Wistar Han rats 410 nM, beagle dogs 2200 nM) following oral administration (rat 30 and, dog 10 mg/kg). Iptacopan exhibits terminal elimination half-lives (T 1/2 ; 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). MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: C57BL/6 mice with KRN-induced arthritisDosage: 20, 60, and 180 mg/kg Administration: Orally gavaged; twice a day (b.i.d.) for 14 days Result: Blocked KRN-induced arthritis.

IC50& Target:KD: 7.9 nM (factor B),IC50: 10 nM (factor B)

Specifications

Spezifikationen & Reinheit

10mM in DMSO

Biochemische und physiologische Mechanismen

Iptacopan (LNP023) is a first-in-class, orally bioavailable, highly potent and highly selective factor B inhibitor with an IC 50 value of 10 nM. Iptacopan shows direct, reversible, and high-affinity binding to human factor B with a K D of 7.9 nM. Iptacopa

Storage

Store at -80°C

Verschickt in

Dry ice packs + Cold packs

Dieses Produkt erfordert Kühlkettenversand. Grundversand und andere Economy-Optionen sind nicht verfügbar.

Aktionsart

INHIBITOR

Mechanismus der Wirkung

Complement factor B inhibitor

Produkteigenschaften

• ALogP: 1.8

Namen und Kennungen

• Isomere SMILES: CCO[C@H]1CCN([C@@H](C1)C2=CC=C(C=C2)C(=O)O)CC3=C(C=C(C4=C3C=CN4)C)OC
• Alternative CAS-Nummer: 1644670-37-0；1646321-63-2
• PubChem CID: 90467622
• Molekulargewicht: 422.52

Zugehörige Ziele (menschlich)

CFB Tchem Complement factor B (0 Activities)

Discover Target: CFB

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Häufig gestellte Fragen

How should this product be stored?

Store at ?80 °C. Ultra-low temperature storage is required to maintain the specified shelf life.

How is this product shipped?

This product ships frozen with dry ice and cold packs. Unpack on arrival and transfer it to the storage condition stated above; handle dry ice with insulated gloves in a ventilated area.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 1644670-37-0, the molecular formula is C25H30N2O4, and the molecular weight is 422.52 g/mol.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.