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ACT-1004-1239 is an orally active, selective, and potent CXCR7 antagonist with immune-modulatory and myelin-promoting effects. It can be used to study inflammatory demyelinating diseases.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $213 | In Stock | |
5 mg | $538 | In Stock | |
10 mg | $868 | In Stock | |
25 mg | $1,780 | In Stock | |
50 mg | $2,860 | In Stock |
Description | ACT-1004-1239 is an orally active, selective, and potent CXCR7 antagonist with immune-modulatory and myelin-promoting effects. It can be used to study inflammatory demyelinating diseases. |
Targets&IC50 | CXCR7 (dog):2.3 nM, CXCR7 (human):3.2 nM |
In vitro | ACT-1004-1239 inhibits CXCR7 in human, dog, rat, mouse, guinea pig and macaque with IC50s of 3.2, 2.3, 3.1, 2.3, 0.6 and 1.5 nM, respectively. [1] ACT-1004-1239 promotes the maturation of OPCs into myelin oligodendrocytes. [2] |
In vivo | In a MOG-induced mouse model of EAE, ACT-1004-1239 treatment (10-100 mg/kg twice daily, orally) showed a significant dose-dependent reduction in the clinical score of the disease, leading to an increase in survival. At the highest dose tested (100 mg/kg twice daily), ACT-1004-1239 delayed disease onset and significantly reduced immune cell infiltration into the CNS and plasma filament light chain concentrations. [2] ACT-1004-1239 reduces pulmonary vascular permeability and reduces inflammatory cell infiltration. [3] |
Molecular Weight | 522.55 |
Formula | C27H28F2N6O3 |
Cas No. | 2178049-58-4 |
Smiles | N(C(=O)[C@@H]1[C@@H](NC(=O)C=2C=C(ON2)C3=C(F)C=C(F)C=C3)CCN(CC4CC4)C1)C5(CC5)C=6N=CC=CN6 |
Storage | keep away from moisture,store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||
Solubility Information | DMSO: 5.00 mg/mL (9.57 mM), Sonication is recommended. | |||||||||||||||
Solution Preparation Table | ||||||||||||||||
DMSO
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