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ACT-1004-1239

Chemical Structure : ACT-1004-1239

CAS No.: 2178049-58-4

ACT-1004-1239 (ACT1004-1239)

Catalog No.: PC-72634Not For Human Use, Lab Use Only.

ACT-1004-1239 is a potent, selective, orally available CXCR7 antagonist with IC50 of 3.2 nM (hCXCR7).

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

ACT-1004-1239 is a potent, selective, orally available CXCR7 antagonist with IC50 of 3.2 nM (hCXCR7).
ACT-1004-1239 also shows similar potency against rat, mouse and dog CXCR (IC50=2-3 nM), shows high selectivity in a panel of 87 enzymatic and radioligand binding assays (CXCR4, IC50>10 uM).
ACT-1004-1239 is a potent insurmountable CXCR7 antagonist against both CXCL11 and CXCL12, shows a dose-dependent increase of CXCL12 plasma concentration in mice.

Physicochemical Properties

M.Wt 522.557
Formula C27H28F2N6O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

3-Piperidinecarboxamide, 1-(cyclopropylmethyl)-4-[[[5-(2,4-difluorophenyl)-3-isoxazolyl]carbonyl]amino]-N-[1-(2-pyrimidinyl)cyclopropyl]-, (3S,4S)-

References

1. Sylvia Richard-Bildstein, et al. J Med Chem. 2020 Dec 24;63(24):15864-15882.

2. Huynh C, et al. Clin Pharmacol Ther. 2021 Jun;109(6):1648-1659.

3. Huynh C, et al. Biomed Pharmacother. 2021 Dec;144:112363.

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