4-((2S,4S)-4-ethoxy-1-((5-methoxy-7-methyl-1H-indol-4-yl)methyl)piperidin-2-yl)benzoicacid

ChemicalBook > CAS DataBase List > 4-((2S,4S)-4-ethoxy-1-((5-methoxy-7-methyl-1H-indol-4-yl)methyl)piperidin-2-yl)benzoicacid

4-((2S,4S)-4-ethoxy-1-((5-methoxy-7-methyl-1H-indol-4-yl)methyl)piperidin-2-yl)benzoicacid

Product Name: 4-((2S,4S)-4-ethoxy-1-((5-methoxy-7-methyl-1H-indol-4-yl)methyl)piperidin-2-yl)benzoicacid
CAS No.: 1644670-37-0
Chemical Name: 4-((2S,4S)-4-ethoxy-1-((5-methoxy-7-methyl-1H-indol-4-yl)methyl)piperidin-2-yl)benzoicacid
Synonyms: LNP023;LNP0233;EOS-62416;LNP023(LNP-023;4-((2S,4S)-4-ethoxy-1-((5-methoxy-7-methyl-1H-indol-4-yl)methyl)piperidin-2-yl)benzoicacid;Benzoic acid, 4-[(2S,4S)-4-ethoxy-1-[(5-methoxy-7-methyl-1H-indol-4-yl)methyl]-2-piperidinyl]-
CBNumber: CB23142721
Molecular Formula: C25H30N2O4
Formula Weight: 422.52
MOL File: 1644670-37-0.mol

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4-((2S,4S)-4-ethoxy-1-((5-methoxy-7-methyl-1H-indol-4-yl)methyl)piperidin-2-yl)benzoicacid Property

Boiling point:: 599.1±50.0 °C(Predicted)
Density: 1.25±0.1 g/cm3(Predicted)
storage temp.: Store at -20°C
solubility: DMSO:50.0(Max Conc. mg/mL);118.34(Max Conc. mM)
pka: 4.07±0.10(Predicted)
form: Solid
color: Off-white to gray

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

ChemScene

Product number: CS-0093107
Product name: Iptacopan
Purity: 98.66%
Packaging: 5mg
Price: $400
Updated: 2021/12/16

ChemScene

Product number: CS-0093107
Product name: Iptacopan
Purity: 98.66%
Packaging: 10mg
Price: $680
Updated: 2021/12/16

ChemScene

Product number: CS-0093107
Product name: Iptacopan
Purity: 98.66%
Packaging: 50mg
Price: $1900
Updated: 2021/12/16

ChemScene

Product number: CS-0093107
Product name: Iptacopan
Purity: 98.66%
Packaging: 100mg
Price: $2900
Updated: 2021/12/16

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4-((2S,4S)-4-ethoxy-1-((5-methoxy-7-methyl-1H-indol-4-yl)methyl)piperidin-2-yl)benzoicacid Chemical Properties,Usage,Production

Biological Activity

Iptacopan (LNP023) is a first-in-class, potent, and orally active and highly selective factor B inhibitor with IC50 of 10 nM. Iptacopan binds factor B directly and reversibly with high affinity with a KD of 7.9 nM. Iptacopan targets the underlying cause of C3 glomerulopathy.

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).
It 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) .

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. < br/> It 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 respectively) ).

Animal Model:	C57BL/6 mice with KRN-induced arthritis
Dosage:	20, 60, and 180 mg/kg
Administration:	Orally gavaged; twice a day (bid) for 14 days
Result:	Blocked KRN-induced arthritis.

target

KD: 7.9 nM (factor B)
IC50: 10 nM (factor B)

4-((2S,4S)-4-ethoxy-1-((5-methoxy-7-methyl-1H-indol-4-yl)methyl)piperidin-2-yl)benzoicacid Preparation Products And Raw materials

Raw materials

Preparation Products

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1644670-37-0, 4-((2S,4S)-4-ethoxy-1-((5-methoxy-7-methyl-1H-indol-4-yl)methyl)piperidin-2-yl)benzoicacidRelated Search:

4-((2S,4S)-4-ethoxy-1-((5-methoxy-7-methyl-1H-indol-4-yl)methyl)piperidin-2-yl)benzoicacid

EOS-62416

LNP023

Benzoic acid, 4-[(2S,4S)-4-ethoxy-1-[(5-methoxy-7-methyl-1H-indol-4-yl)methyl]-2-piperidinyl]-

LNP023(LNP-023

LNP0233

1644670-37-0