1. Metabolic Enzyme/Protease
  2. RAR/RXR
  3. AGN 194310

AGN 194310 (Synonyms: VTP-194310)

Cat. No.: HY-16681 Purity: 98.02%
Handling Instructions

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.

For research use only. We do not sell to patients.

AGN 194310 Chemical Structure

AGN 194310 Chemical Structure

CAS No. : 229961-45-9

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 616 In-stock
Estimated Time of Arrival: December 31
1 mg USD 180 In-stock
Estimated Time of Arrival: December 31
5 mg USD 660 In-stock
Estimated Time of Arrival: December 31
10 mg USD 1020 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1740 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2700 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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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 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 [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].

Molecular Weight

424.55

Formula

C₂₈H₂₄O₂S

CAS No.

229961-45-9

SMILES

CC(S1)(C)C=C(C2=CC=C(CC)C=C2)C3=C1C=CC(C#CC4=CC=C(C(O)=O)C=C4)=C3

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (117.77 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3554 mL 11.7772 mL 23.5544 mL
5 mM 0.4711 mL 2.3554 mL 4.7109 mL
10 mM 0.2355 mL 1.1777 mL 2.3554 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.89 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.89 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Product Name:
AGN 194310
Cat. No.:
HY-16681
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