ChemicalBook Product Catalog Biochemical Engineering Biochemical Reagents Agonist Inhibitors AGN 194310

AGN 194310

Product NameAGN 194310
CAS229961-45-9
MFC28H24O2S
MW424.55
EINECS
MOL File229961-45-9.mol

Chemical Properties

Boiling point	598.1±50.0 °C(Predicted)
Density	1.26±0.1 g/cm3(Predicted)
storage temp.	Store at -20°C
solubility	>16.8mg/mL in DMSO
form	Powder
pka	4.02±0.10(Predicted)
color	White to off-white
InChI	1S/C28H24O2S/c1-4-19-7-12-22(13-8-19)25-18-28(2,3)31-26-16-11-21(17-24(25)26)6-5-20-9-14-23(15-10-20)27(29)30/h7-18H,4H2,1-3H3,(H,29,30)
InChIKey	LHUPKWKWYWOMSK-UHFFFAOYSA-N
SMILES	O=C(O)C1=CC=C(C#CC2=CC3=C(SC(C)(C=C3C4=CC=C(CC)C=C4)C)C=C2)C=C1

Safety Information

WGK Germany	WGK 3
Storage Class	11 - Combustible Solids

Usage And Synthesis

Uses

AGN 194310 (VTP-194310) is a high affinity, potent and selective retinioic acid receptors (RARs) pan-antagonist with Kd values of 3 nM, 2 nM, 5 nM for RARα, RARβ, RARγ, respectively[1][2]. AGN 194310 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

Biological Activity

AGN 194310 (VTP-194310) is a high-affinity, potent, and selective pan-antagonist of retinoic acid receptors (RARs) with Kd values of 3 nM and 2 nM for RARα, RARβ, and RARγ, respectively , 5 nM.

in vivo

AGN 194310 (0.5 mg/kg/day; oral gavage; every day; for 10 days; female C57Bl/6J mice) treatment increases the number of granulocytes across haemopoietic compartments. A significant increase in the frequency of granulocyte -progenitor cells are observed in the bone marrow of mice after treatment with AGN194310.

Animal Model:	Female C57Bl/6J mice (Five -week-old (34-37 days))
Dosage:	0.5 mg/kg/ day
Administration:	Oral gavage; every day; for 10 days
Result:	The number of granulocytes was significantly increased across haemopoietic compartments. Progenitor cells containing granulocytes also increased significantly.

target

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References

[1] Johnson AT, et al. Synthesis and biological activity of high-affinity retinoic acid receptor antagonists. Bioorg Med Chem. 1999 Jul;7(7):1321-38. DOI:10.1016/s0968-0896(99)00055-3
[2] Hammond LA, et al. Antagonists of retinoic acid receptors (RARs) are potent growth inhibitors of prostate carcinoma cells. Br J Cancer. 2001 Aug 3;85(3):453-62. DOI:10.1054/bjoc.2001.1939
[3] Walkley CR, et al. Retinoic acid receptor antagonism in vivo expands the numbers of precursor cells during granulopoiesis. Leukemia. 2002 Sep;16(9):1763-72. DOI:10.1038/sj.leu.2402625

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Related Product Information

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RARα

3 nM (Kd)

RARβ

2 nM (Kd)

RARγ

5 nM (Kd)