3-Pyridinecarboxamide, N-[3-[(1S)-1-[[6-(3,4-dimethoxyphenyl)-2-pyrazinyl]amino]ethyl]phenyl]-5-methyl-
- Product Name
- 3-Pyridinecarboxamide, N-[3-[(1S)-1-[[6-(3,4-dimethoxyphenyl)-2-pyrazinyl]amino]ethyl]phenyl]-5-methyl-
- CAS No.
- 1619931-27-9
- Chemical Name
- 3-Pyridinecarboxamide, N-[3-[(1S)-1-[[6-(3,4-dimethoxyphenyl)-2-pyrazinyl]amino]ethyl]phenyl]-5-methyl-
- Synonyms
- GB002;PK-10571;Seralutinib;Valine Impurity 98;Seralutinib (GB002);Seralutinib (PK-10571;Seralutinib, 10 mM in DMSO;(S)-N-(3-(1-((6-(3,4-Dimethoxyphenyl)pyrazin-2-yl)amino)ethyl)phenyl)-5-methylnicotinamide;N-3-(1S)-1-6-(3,4-Dimethoxy-phenyl)-pyrazin-2-ylamino-ethylphenyl-5-methylpyridin-3-carboxamide;3-Pyridinecarboxamide, N-[3-[(1S)-1-[[6-(3,4-dimethoxyphenyl)-2-pyrazinyl]amino]ethyl]phenyl]-5-methyl-
- CBNumber
- CB58352036
- Molecular Formula
- C27H27N5O3
- Formula Weight
- 469.54
- MOL File
- 1619931-27-9.mol
3-Pyridinecarboxamide, N-[3-[(1S)-1-[[6-(3,4-dimethoxyphenyl)-2-pyrazinyl]amino]ethyl]phenyl]-5-methyl- Property
- Boiling point:
- 601.4±55.0 °C(Predicted)
- Density
- 1.252±0.06 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO : 100 mg/mL (212.98 mM; Need ultrasonic)
- form
- Solid
- pka
- 12.16±0.70(Predicted)
- color
- White to light yellow
- InChIKey
- JHJNPOSPVGRIAN-SFHVURJKSA-N
- SMILES
- C1=NC=C(C)C=C1C(NC1=CC=CC([C@@H](NC2=NC(C3=CC=C(OC)C(OC)=C3)=CN=C2)C)=C1)=O
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.
P302+P352IF ON SKIN: wash with plenty of soap and water.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- CS-0116463
- Product name
- Seralutinib
- Packaging
- 5mg
- Price
- $400
- Updated
- 2021/12/16
- Product number
- CS-0116463
- Product name
- Seralutinib
- Packaging
- 10mg
- Price
- $680
- Updated
- 2021/12/16
- Product number
- CS-0116463
- Product name
- Seralutinib
- Packaging
- 25mg
- Price
- $1350
- Updated
- 2021/12/16
- Product number
- CS-0116463
- Product name
- Seralutinib
- Packaging
- 50mg
- Price
- $2200
- Updated
- 2021/12/16
- Product number
- CS-0116463
- Product name
- Seralutinib
- Packaging
- 100mg
- Price
- $3400
- Updated
- 2021/12/16
3-Pyridinecarboxamide, N-[3-[(1S)-1-[[6-(3,4-dimethoxyphenyl)-2-pyrazinyl]amino]ethyl]phenyl]-5-methyl- Chemical Properties,Usage,Production
Uses
Seralutinib (GB002) is an inhaled PDGFRα and PDGFRβ inhibitor. Seralutinib also targets to CSF1R and c-KIT with IC50s of 8 nM and 14 nM, respectively. Seralutinib (GB002) is used in the study for pulmonary arterial hypertension[1][2].
in vivo
Seralutinib (GB002) (two-week treatment, delivered by inhalation) significantly reduces right ventricular systolic pressure and mean pulmonary artery pressure. Hemodynamic changes are accompanied by reduced pulmonary arteriole muscularization and restoration of BMPR2 protein expression in the lung lobes in Seralutinib (GB002)-treated animals. Seralutinib (GB002) is well tolerated[1].
Seralutinib-mediated inhibition of lung PDGFRα/β phosphorylation in healthy Sprague Dawley rats immediately post inhalation[2].
Seralutinib dose- and time-dependently induces lung BMPR2 protein expression[2].
IC 50
PDGFRα; PDGFRβ; CSF1R: 8 nM (IC50); c-KIT: 14 nM (IC50)
References
[1] Robert P. Frantz1, et.al. Phase 2 Clinical Study to Evaluate the Efficacy and Safety of Inhaled GB002 (Seralutinib) for the Treatment of World Health Organization Group 1 Pulmonary Arterial Hypertension
[2] Anna Galkin, et al. Abstract 11102: Gb002, A Novel Inhaled Pdgfr Kinase Inhibitor, Demonstrates Efficacy in the Su5416 Hypoxia Rat Model of Pulmonary Arterial Hypertension (pah). Circulation. 2019;140:A11102.
[3] Anna Galkin, et al. Pharmacologic Characterization of GB002, a Novel Inhaled PDGFR Kinase Inhibitor in Development for Pulmonary Arterial Hypertension (PAH).
3-Pyridinecarboxamide, N-[3-[(1S)-1-[[6-(3,4-dimethoxyphenyl)-2-pyrazinyl]amino]ethyl]phenyl]-5-methyl- Preparation Products And Raw materials
Raw materials
Preparation Products
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View Lastest Price from 3-Pyridinecarboxamide, N-[3-[(1S)-1-[[6-(3,4-dimethoxyphenyl)-2-pyrazinyl]amino]ethyl]phenyl]-5-methyl- manufacturers
- Product
- 3-Pyridinecarboxamide, N-[3-[(1S)-1-[[6-(3,4-dimethoxyphenyl)-2-pyrazinyl]amino]ethyl]phenyl]-5-methyl- 1619931-27-9
- Price
- US $8.00-1.00/kg
- Min. Order
- 1kg
- Purity
- 99%
- Supply Ability
- g-kg-tons, free sample is available
- Release date
- 2024-03-28