A1120 | Non-retinoid RBP4 antagonist

CAS:
 1152782-19-8
Catalog Number:
 10-5117
A1120 chemical structure

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A1120 (1152782-19-8) is a high affinity (Ki = 8.3 nM) non-retinoid antagonist for RBP4 (retinol-binding protein 4), which disrupts the interaction between RBP4 and its binding partner transthyretin and lowers serum RBP4 levels in vivo in mice.1 Significantly reduces lipofuscin bisretinoid formation in the retinas of Abca4-/- mice with potential for treatment of atrophic age-related macular degeneration.2,3 Has been employed as a small molecule “On-Switch” for controlling CAR T cells in conjunction with RBP4 and engineered RBP4-binders.4

References/Citations:

  1. Motani et al. (2009), Identification and characterization of a non-retinoid ligand for retinol-binding protein 4 which lowers serum retinol-binding protein 4 levels in vivo; J. Biol. Chem. 284 7673
  2. Cioffi et al. (2014), Design, synthesis, and evaluation of nonretinoid retinol binding protein 4 antagonists for the potential treatment of atrophic age-related macular degeneration and Stargardt disease; J. Med. Chem. 57 7731
  3. Dobri et al. (2013), A1120, a nonretinoid RBP4 antagonist, inhibits formation of cytotoxic bisretinoids in the animal model of enhanced retinal lipofuscinogenesis; Invest. Ophthalmol. Vis. Sci. 54 85
  4. Zajc et al. (2020), A conformation-specific ON-switch for controlling CAR T cells with an orally available drug; Proc. Natl. Acad. Sci. USA 117 14926
1152782-19-8, A-1120, A1120, A1120 supplier, CAR T cell controller, RBP4 antagonist
CAS:
1152782-19-8
Catalog Number:
10-5117
Activity:
Non-retinoid RBP4 antagonist
Chemical Names:
2-(4-(2-(Trifluoromethyl)phenyl)piperidine-1-carboxamido)benzoic acid
Molecular Weight:
392.38
Molecular Formula:

C20H19F3N2O3

Solubility:
Soluble in DMSO (40 mg/ml); Ethanol (10 mg/ml)
Physical Properties:
Off-white solid
Purity:

>98% HPLC
NMR: (Conforms)

Storage Temperature:
-20°C
Stability:
Stable for up to 2 years when stored as supplied @ -20°C. Solutions in DMSO or ethanol may be stored at -20°C for up to 2 months.
Shipping Code:
RT

Safety Data Sheet:

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Product Data Sheet:

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A1120 (1152782-19-8) is a high affinity (Ki = 8.3 nM) non-retinoid antagonist for RBP4 (retinol-binding protein 4), which disrupts the interaction between RBP4 and its binding partner transthyretin and lowers serum RBP4 levels in vivo in mice.1 Significantly reduces lipofuscin bisretinoid formation in the retinas of Abca4-/- mice with potential for treatment of atrophic age-related macular degeneration.2,3 Has been employed as a small molecule “On-Switch” for controlling CAR T cells in conjunction with RBP4 and engineered RBP4-binders.4

References/Citations:

  1. Motani et al. (2009), Identification and characterization of a non-retinoid ligand for retinol-binding protein 4 which lowers serum retinol-binding protein 4 levels in vivo; J. Biol. Chem. 284 7673
  2. Cioffi et al. (2014), Design, synthesis, and evaluation of nonretinoid retinol binding protein 4 antagonists for the potential treatment of atrophic age-related macular degeneration and Stargardt disease; J. Med. Chem. 57 7731
  3. Dobri et al. (2013), A1120, a nonretinoid RBP4 antagonist, inhibits formation of cytotoxic bisretinoids in the animal model of enhanced retinal lipofuscinogenesis; Invest. Ophthalmol. Vis. Sci. 54 85
  4. Zajc et al. (2020), A conformation-specific ON-switch for controlling CAR T cells with an orally available drug; Proc. Natl. Acad. Sci. USA 117 14926

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