CS-003 Free base Struktur

CS-003 Free base

Bezeichnung:CS-003 Free base

Englisch Name:CS-003 Free base

CBNumberCB95821351

SummenformelC34H38Cl2N2O6S

Molgewicht673.65

CS-003 Free base physikalisch-chemischer Eigenschaften

CS-003 Free base Chemische Eigenschaften,Einsatz,Produktion Methoden

Biologische Aktivität
CS-003 Free base (CS-003) is a tritachykinin receptor antagonist with high affinity for human neurokinin NK1, NK2 and NK3 receptors with Ki values of 2.3 nM and 0.54 nM, respectively and 0.74 nM.It can be used in the study of neurokinin-related respiratory diseases.
in vitro

CS-003 (0.01-10 μM; 24 hours) inhibits NK1, NK2 or NK3 induced inositol phosphate formation in a concentration-dependent manner with pA2 values of 8.7, 9.4 and 9.5 μM, respectively.
in vivo

CS-003 (intravenous injection; 0.01-3.0 mg/kg; 5 min before neurokinin A/B/C injection) inhibits substance P-induced tracheal vascular hyperpermeability, neurokinin A- and neurokinin B-induced bronchoconstriction with ID ₅₀ values of 0.13, 0.040 and 0.063 mg/kg, respectively.

target

< /table>

NK1

2.3 nM (Ki)

NK2

0.54 nM (Ki)

NK3

0.74 nM (Ki)