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;Iptacopan, 10 mM in DMSO;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
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
- InChIKey
- RENRQMCACQEWFC-UGKGYDQZSA-N
- SMILES
- C(O)(=O)C1=CC=C([C@@H]2C[C@@H](OCC)CCN2CC2=C(OC)C=C(C)C3=C2C=CN3)C=C1
N-Bromosuccinimide Price
- Product number
- CS-0093107
- Product name
- Iptacopan
- Purity
- 98.66%
- Packaging
- 5mg
- Price
- $400
- Updated
- 2021/12/16
- Product number
- CS-0093107
- Product name
- Iptacopan
- Purity
- 98.66%
- Packaging
- 10mg
- Price
- $680
- Updated
- 2021/12/16
- Product number
- CS-0093107
- Product name
- Iptacopan
- Purity
- 98.66%
- Packaging
- 50mg
- Price
- $1900
- Updated
- 2021/12/16
- Product number
- CS-0093107
- Product name
- Iptacopan
- Purity
- 98.66%
- Packaging
- 100mg
- Price
- $2900
- Updated
- 2021/12/16
4-((2S,4S)-4-ethoxy-1-((5-methoxy-7-methyl-1H-indol-4-yl)methyl)piperidin-2-yl)benzoicacid Chemical Properties,Usage,Production
Uses
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].
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)
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)benzoicacid Preparation Products And Raw materials
Raw materials
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