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AGN193109 (AGN-193109) is a retinoid analog acting as a novel and potent retinoic acid receptor (RAR) antagonist with Kds of 2 nM, 2 nM, and 3 nM for RARα, RARβ, and RARγ, respectively.
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| ln Vitro |
AGN 193109 is a very potent retinoic acid receptor antagonist, with Kds of 2 nM, 2 nM, and 3 nM for RARα, RARβ, and RARγ, to name a few. Because it does not bind to or transactivate through any RXRs, AGN 193109 is entirely RAR specific[1]. In ECE16-1 cells, AGN 193109 (100 nM) prevents the morphological alteration that is dependent on TTNPB (a retinoic acid receptor agonist). In ECE16-1 cells, AGN193109 totally demonstrates the effect of retinoid-dependent growth suppression at 100 nM, but at 10 nM it partially reverses it. Additionally, TTNPB-induced decreases in K5, K6, K14, K16, and K17 and increases in K7, K8, and K19 levels are eliminated by AGN193109 (100 nM)[2].
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| ln Vivo |
AGN 193109 (1.15 μmol/kg) reduces the increase in spleen weight of mice induced by TTNPB, but does not cause overt toxicity or affect spleen weight in animals. Additionally, AGN 193109 dramatically lessens the cutaneous toxicity that ATRA causes. Topical administration of AGN 193109 (0.30 or 1.20 μmol/kg) effectively lowers cutaneous toxicity and weight loss brought on by oral TTNPB cotreatment[3].
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| References |
[1]. Johnson AT, et al. Synthesis and characterization of a highly potent and effective antagonist of retinoic acid receptors. J Med Chem. 1995 Nov 24;38(24):4764-7.
[2]. Agarwal C, et al. AGN193109 is a highly effective antagonist of retinoid action in human ectocervical epithelial cells. J Biol Chem. 1996 May 24;271(21):12209-12. [3]. Standeven AM, et al. Specific antagonist of retinoid toxicity in mice. Toxicol Appl Pharmacol. 1996 May;138(1):169-75 |
| Molecular Formula |
C28H24O2
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| Molecular Weight |
392.498
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| Exact Mass |
392.1776
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| CAS # |
171746-21-7
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| Related CAS # |
AGN 193109;171746-21-7;AGN 193109-d7;1216429-25-2
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| SMILES |
O=C(O)C1=CC=C(C#CC2=CC=C3C(C)(C)CC=C(C4=CC=C(C)C=C4)C3=C2)C=C1
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| Synonyms |
AGN-193109AGN193109
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~2 mg/mL (~5.10 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 12.5 mg/mL (31.85 mM) in 15% Cremophor EL 85% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 5 mg/mL (12.74 mM) in 0.5% CMC-Na/saline water (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5478 mL | 12.7389 mL | 25.4777 mL | |
| 5 mM | 0.5096 mL | 2.5478 mL | 5.0955 mL | |
| 10 mM | 0.2548 mL | 1.2739 mL | 2.5478 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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