An RXR agonist
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V-125

Item No. 37532

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
6-[ethyl(5,6,7,8-tetrahydro-3,5,5,8,8-pentamethyl-2-naphthalenyl)amino]-3-pyridinecarboxylic acid
CAS Number
1807740-94-8
Molecular Formula
C23H30N2O2
Formula Weight
366.5
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMF: 2 mg/mlDMSO: Slightly solubleEthanol: Slightly solublePBS (pH 7.2): 0.3 mg/ml
λmax
291 nm
SMILES
CC1(C)C2=C(C=C(C)C(N(CC)C3=CC=C(C(O)=O)C=N3)=C2)C(C)(C)CC1
InChi Code
InChI=1S/C23H30N2O2/c1-7-25(20-9-8-16(14-24-20)21(26)27)19-13-18-17(12-15(19)2)22(3,4)10-11-23(18,5)6/h8-9,12-14H,7,10-11H2,1-6H3,(H,26,27)
InChi Key
HYDUUPGGUIYHGP-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    5 mg

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    100 mg

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    Cayman Chemical
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    Product Description

    V-125 is an agonist of retinoid X receptors (RXRs).1 It induces homodimerization of RXR in HCT116 cells in a two-hybrid assay (EC50 = 13.8 nM). V-125 selectively induces transactivation of RXRα in human RXRα-overexpressing HCT116 cells over transactivation of RARα in human RARα-overexpressing HEK293 cells when used at concentrations of 25 and 100 nM, respectively. In vivo, V-125 (80 mg/kg in the diet) inhibits vinyl carbamate-induced lung tumor growth in mice.2 Unlike the RXR agonist bexarotene (Item No. 11571), V-125 does not increase plasma triglyceride or cholesterol levels in mice.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Heck, M.C., C.E., W., Shahani, P.H., et al. Modeling, synthesis, and biological evaluation of potential retinoid X receptor (RXR)-selective agonists: Analogues of 4‑[1-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydro-2-naphthyl)ethynyl]benzoic acid (bexarotene) and 6‑(ethyl(5,5,8,8-tetrahydronaphthalen-2-yl)amino)nicotinic acid (NEt-TMN). J. Med. Chem. 59(19), 8924-8940 (2016).

    2. Reich, L.A., Moerland, J.A., Leal, A.S., et al. The rexinoid V‑125 reduces tumor growth in preclinical models of breast and lung cancer. Sci. Rep. 12(1), 293 (2022).