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

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

Product Name: 4-((2S,4S)-4-ethoxy-1-((5-methoxy-7-methyl-1H-indol-4-yl)methyl)piperidin-2-yl)benzoicacidhydrochloride
CAS No.: 1646321-63-2
Chemical Name: 4-((2S,4S)-4-ethoxy-1-((5-methoxy-7-methyl-1H-indol-4-yl)methyl)piperidin-2-yl)benzoicacidhydrochloride
Synonyms: LNP023 hcl;EOS-61917;Iptacopan HCl;Iptacopan(lnp023);LNP023 hydrochloride;Iptacopanhydrochloride;Ipcoopam hydrochloride.;LNP023/Iptacopan hydrochloride;Iptacopan (LNP023) hydrochloride;Iptacopanhydrochloride，LNP023 hcl
CBNumber: CB53142722
Molecular Formula: C25H31ClN2O4
Formula Weight: 458.98
MOL File: 1646321-63-2.mol

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

storage temp.: Store at -20°C
solubility: DMSO : 250 mg/mL (544.69 mM; Need ultrasonic)|
form: A solid
color: White to off-white
Water Solubility: Water : 50 mg/mL (108.94 mM; ultrasonic and warming and heat to 60°C)
InChIKey: SEZXOFFLNHXEJE-QHWHZDSMNA-N
SMILES: C(N1CC[C@H](OCC)C[C@H]1C1C=CC(C(=O)O)=CC=1)C1C(=CC(C)=C2NC=CC=12)OC.Cl |&1:4,9,r|

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

ChemScene

Product number: CS-0131140
Product name: Iptacopan(hydrochloride)
Packaging: 5mg
Price: $400
Updated: 2021/12/16

ChemScene

Product number: CS-0131140
Product name: Iptacopan(hydrochloride)
Packaging: 10mg
Price: $680
Updated: 2021/12/16

ChemScene

Product number: CS-0131140
Product name: Iptacopan(hydrochloride)
Packaging: 50mg
Price: $1900
Updated: 2021/12/16

ChemScene

Product number: CS-0131140
Product name: Iptacopan(hydrochloride)
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)benzoicacidhydrochloride Chemical Properties,Usage,Production

Uses

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].

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 (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)^[3].
LNP023 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)^[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.

References

[1] Dimitrios C Mastellos, et al. Expanding Complement Therapeutics for the Treatment of Paroxysmal Nocturnal Hemoglobinuria. Semin Hematol. 2018 Jul;55(3):167-175. DOI:10.1053/j.seminhematol.2018.02.002
[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. DOI:10.1073/pnas.1820892116
[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. DOI:10.1021/acs.jmedchem.9b01870

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

Raw materials

Preparation Products

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1646321-63-2, 4-((2S,4S)-4-ethoxy-1-((5-methoxy-7-methyl-1H-indol-4-yl)methyl)piperidin-2-yl)benzoicacidhydrochlorideRelated Search:

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

EOS-61917

LNP023 hcl

LNP023 hydrochloride

Iptacopan(lnp023)

Iptacopanhydrochloride

Iptacopanhydrochloride，LNP023 hcl

Iptacopan HCl

Iptacopan (LNP023) hydrochloride

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4-[(2S,4S)-4-Ethoxy-1-[(5-methoxy-7-methyl-1H-indol-4-yl)methyl]-2-piperidinyl]benzoic acid,hydrochloride (1:1)

LNP023/Iptacopan hydrochloride

Ipcoopam hydrochloride.

Iptacopan hydrochloride, 10 mM in DMSO

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

1646321-63-2