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Pack Size | Price | Availability | Quantity |
---|---|---|---|
5 mg | $643 | 10-14 weeks | |
25 mg | $1,870 | 10-14 weeks | |
50 mg | $2,440 | 10-14 weeks | |
100 mg | $4,090 | 10-14 weeks |
Description | CXCR7 modulator 2 is a 7-type C-X-C chemokine receptor (CXCR7) modulator with a Ki of 13 nM. |
In vitro | CXCR7 modulator 2 showed strong CXCR7 binding affinity (Ki = 13 nM) and β-arrestin activity (EC50 = 11 nM). Compared with 11c, CXCR7 modulator 2 also showed improved selectivity in the GPCR panel and showed a higher therapeutic index in the hERG patch clamp assay. CXCR7 modulator 2 exhibited medium to high in vitro turnover in NADPH- supplemented mouse liver microsomes (MLM, 93 μL / min / mg) and hepatocytes (28 μL / min per million cells), which was shown to be more comparable in MDCK Poor passive absorption permeability type II permeability measurement method, and has good water solubility. CXCR7 regulator 2 is rapidly absorbed, with an average maximum plasma concentration (Cmax) of 682 ng / mL, which appears at 0.25 h (Tmax). The corresponding average area under the plasma concentration-time curve (AUC) is 740 ng / mL / h. |
In vivo | The administration of isoproterenol for 9 days will lead to the development of cardiac fibrosis. This is because the amount of collagen deposition detected by Pixirius red staining has increased by about 4 times relative to that of the control group. proven. Treatment with CXCR7 modulator 2 can lead to a statistically significant reduction in cardiac fibrosis, thus demonstrating that CXCR7 modulator 2 has a protective effect on CXCR7 modulation in isoproterenol-induced cardiac injury. |
Molecular Weight | 522.68 |
Formula | C29H42N6O3 |
Cas No. | 2227426-37-9 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 250 mg/mL (478.30 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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