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
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|
N-Bromosuccinimide Price
- Product number
- CS-0131140
- Product name
- Iptacopan(hydrochloride)
- Packaging
- 5mg
- Price
- $400
- Updated
- 2021/12/16
- Product number
- CS-0131140
- Product name
- Iptacopan(hydrochloride)
- Packaging
- 10mg
- Price
- $680
- Updated
- 2021/12/16
- Product number
- CS-0131140
- Product name
- Iptacopan(hydrochloride)
- Packaging
- 50mg
- Price
- $1900
- Updated
- 2021/12/16
- Product number
- CS-0131140
- Product name
- Iptacopan(hydrochloride)
- 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)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 (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. |
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
4-((2S,4S)-4-ethoxy-1-((5-methoxy-7-methyl-1H-indol-4-yl)methyl)piperidin-2-yl)benzoicacidhydrochloride Suppliers
- Tel
- +1-781-999-5354; +17819995354
- marketing@targetmol.com
- Country
- United States
- ProdList
- 32435
- Advantage
- 58
- Tel
- +1-708-310-1919 +1-13798911105
- Fax
- 708-557-7486
- sales@invivochem.cn
- Country
- United States
- ProdList
- 6391
- Advantage
- 58
- Tel
- tp@aladdinsci.com
- Country
- United States
- ProdList
- 52923
- Advantage
- 58
- Tel
- +1-781-999-5354;
- support@targetmol.com
- Country
- United States
- ProdList
- 39035
- Advantage
- 58
- Tel
- --
- Fax
- --
- cayman@caymanchem.com
- Country
- United States
- ProdList
- 6213
- Advantage
- 81