| Description: |
AGN 194310(VTP-194310) is a potent and selective pan-RARs agonist with Kd values of 3/2/5 nM for RARα/β/γ respectively.
IC50 value: 3/2/5 nM (Kd for RARα/β/γ)
Target: RARs agonist
in vitro: A high affinity pan-RAR antagonist (AGN194310, K(d) for binding to RARs = 2-5 nM) inhibited colony formation (by 50%) by all three lines at 16-34 nM, and led to a transient accumulation of flask-cultured cells in G1 followed by apoptosis. AGN194310 is 12-22 fold more potent than all-trans retinoic acid (ATRA) against cell lines and also more potent in inhibiting the growth of primary prostate carcinoma cells .
in vivo: The administration of all-trans retinoic acid to VAD mice resulted in a transient reduction in NF-kappaB activity and, conversely, a single dose of the RAR-pan-antagonist, AGN 194310, administered to control mice, led to a marked, transient induction of whole-body luminescence . Mice were treated with AGN194310, a synthetic retinoid that antagonises the physiological function of the three RAR isotypes (alpha, beta, gamma) but does not interact with RXRs. Analyses of the granulocytic lineage using Gr-1, c-Kit and CD11b antibodies, demonstrated that granulocyte numbers were strikingly increased across haemopoietic compartments in all AGN194310-treated mice. A significant increase in the frequency of progenitor cells containing granulocytes was observed in the bone marrow of mice following treatment with AGN194310 .. For the detailed information of AGN 194310, the solubility of AGN 194310 in water, the solubility of AGN 194310 in DMSO, the solubility of AGN 194310 in PBS buffer, the animal experiment (test) of AGN 194310, the cell expriment (test) of AGN 194310, the in vivo, in vitro and clinical trial test of AGN 194310, the EC50, IC50,and affinity,of AGN 194310, Please contact DC Chemicals. |
