Bioactivity | Chymase-IN-1 is a potent, selective, orally active, nonpeptide inhibitor of human mast cell chymase with an IC50 of 29 nM. |
Target | IC50: 29 nM (chymase) |
Invitro | Chymase-IN-1 (compound 5f) is a potent, selective, orally active, nonpeptide inhibitor of human mast cell chymase with an IC50 of 29 nM. Results demonstrate that Chymase-IN-1 has a chymase Ki value of 36 nM and a Cat G Ki value of 9500 nM[1]. |
In Vivo | Chymase-IN-1 exhibits low oral bioavailability in rats (F=3%; oral t1/2=1.8 h)[1]. |
Name | Chymase-IN-1 |
CAS | 862090-74-2 |
Formula | C20H15ClNO4PS |
Molar Mass | 431.83 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Greco MN, et al. Discovery of potent, selective, orally active, nonpeptide inhibitors of human mast cell chymase. J Med Chem. 2007 Apr 19;50(8):1727-30. |