| Company Name: |
cjbscvictory
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| Tel: |
13348960310 |
| Email: |
3003867561@qq.com |
| Products Intro: |
Product Name:GRK2-IN-1
CAS:2055990-90-2
Purity:98% Package:5mg；10mg；20mg；50mg；100mg；200mg
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| Company Name: |
TargetMol Chemicals Inc.
|
| Tel: |
15002134094 |
| Email: |
marketing@targetmol.cn |
| Products Intro: |
Product Name:CCG258208
CAS:2055990-90-2
Package:25mg/RMB 17200;50mg/RMB 22800;100mg/RMB 29500
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| | GRK2-IN-1 Basic information |
| Product Name: | GRK2-IN-1 | | Synonyms: | GRK2-IN-1;Benzamide, 5-[(3S,4R)-3-[(1,3-benzodioxol-5-yloxy)methyl]-4-piperidinyl]-2-fluoro-N-(1H-pyrazol-3-ylmethyl)-;CCG258208;CCG258208,CCG-258208;CCG258208 hydrochloride (GRK2-IN-1) | | CAS: | 2055990-90-2 | | MF: | C24H25FN4O4 | | MW: | 452.48 | | EINECS: | | | Product Categories: | | | Mol File: | 2055990-90-2.mol |  |
| | GRK2-IN-1 Chemical Properties |
| Boiling point | 660.9±55.0 °C(Predicted) | | density | 1.314±0.06 g/cm3(Predicted) | | pka | 13.12±0.46(Predicted) |
| | GRK2-IN-1 Usage And Synthesis |
| Uses | CCG258208 (GRK2-IN-1) is a potent and selective GRK2 (G protein-coupled receptor kinase 2) inhibitor (IC50=30 nM) while maintaining 230-fold selectivity over GRK5 (IC50=7.09 μM) and more than 2500-fold selectivity over GRK1 (IC50=87.3 μM), PKA, and ROCK1. CCG258208 can be used in heart failure research[1]. | | in vivo | CCG258208 (Compound 14as) (intraperitoneal injection; 10 mg/kg; once) treatment shows superior half-life in vivo[1]. | Animal Model: | CD-1 mice[1] | | Dosage: | 10 mg/kg | | Administration: | Intraperitoneal injection; 10 mg/kg; once | | Result: | Showed total plasma drug levels after single IP administration that exceed the GRK2 IC50 for seven hours. |
| | IC 50 | GRK2: 30 nM (IC50); GRK5: 7.1 μM (IC50) | | References | [1] Waldschmidt HV, et al. Structure-Based Design of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2Inhibitors Based on Paroxetine. J Med Chem. 2017 Apr 13;60(7):3052-3069. DOI:10.1021/acs.jmedchem.7b00112 |
| | GRK2-IN-1 Preparation Products And Raw materials |
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