AGN 194310

Modify Date: 2024-01-11 09:49:34

AGN 194310 Structure
AGN 194310 structure
Common Name AGN 194310
CAS Number 229961-45-9 Molecular Weight 424.554
Density 1.3±0.1 g/cm3 Boiling Point 598.1±50.0 °C at 760 mmHg
Molecular Formula C28H24O2S Melting Point N/A
MSDS N/A Flash Point 315.5±30.1 °C

 Use of AGN 194310


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) [1][2]Target: RARs agonistin 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 [2].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 [3]. 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 [4].

 Names

Name AGN 194310
Synonym More Synonyms

 AGN 194310 Biological Activity

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) [1][2]Target: RARs agonistin 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 [2].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 [3]. 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 [4].
Related Catalog
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.

[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.

[3]. Austenaa LM, et al. Vitamin A status significantly alters nuclear factor-kappaB activity assessed by in vivo imaging. FASEB J. 2004 Aug;18(11):1255-7.

[4]. 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.

 Chemical & Physical Properties

Density 1.3±0.1 g/cm3
Boiling Point 598.1±50.0 °C at 760 mmHg
Molecular Formula C28H24O2S
Molecular Weight 424.554
Flash Point 315.5±30.1 °C
Exact Mass 424.149689
LogP 9.56
Vapour Pressure 0.0±1.8 mmHg at 25°C
Index of Refraction 1.683
Storage condition 2-8℃

 Synonyms

4-{[4-(4-Ethylphenyl)-2,2-dimethyl-2H-thiochromen-6-yl]ethynyl}benzoic acid
Benzoic acid, 4-[2-[4-(4-ethylphenyl)-2,2-dimethyl-2H-1-benzothiopyran-6-yl]ethynyl]-
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