(S)-V-0219 hydrochloride

• CAT Number: I041375
• Molecular Formula: C20H26ClF3N4O2
• Molecular Weight: 446.89
• Purity: ≥95%
• Synonyms: 4-[[(3S)-1-[[3-[4-(trifluoromethyl)phenyl]-1,2,4-oxadiazol-5-yl]methyl]piperidin-3-yl]methyl]morpholine;hydrochloride
• InChI: InChI=1S/C20H25F3N4O2.ClH/c21-20(22,23)17-5-3-16(4-6-17)19-24-18(29-25-19)14-27-7-1-2-15(13-27)12-26-8-10-28-11-9-26;/h3-6,15H,1-2,7-14H2;1H/t15-;/m0./s1
• InChIKey: PTRIYHLSBQMDQM-RSAXXLAASA-N
• SMILES: C1CC(CN(C1)CC2=NC(=NO2)C3=CC=C(C=C3)C(F)(F)F)CN4CCOCC4.Cl

(S)-V-0219 hydrochloride is an enantiomer of V-0219 (HY-143312). V-0219 is an orally active and positive allosteric modulator (PAM) of the GLP Receptor-1 (GLP-1R). (S)-V-0219 hydrochloride activates calcium fluxes in HEK cells stably expressing hGLP-1R. (S)-V-0219 hydrochloride is orally active and ameliorates high glucose levels in mice and inhibits feeding behavior in fasted mice[1].
(S)-V-0219 ((S)-9) (0.1 nM) hydrochloride potentiates calcium fluxes in HEK cells stably expressing hGLP-1R[1].
(S)-V-0219 (0.1 nM) hydrochloride potentiates insulin secretion stimulated by GLP-1 in the stable human pancreatic cell line EndoC-βH1 under high glucose concentration[1].
(S)-V-0219 ((S)-9) (0.04-0.2 mg/kg; i.p.) hydrochloride improves glucose handling after injection of 2 g/kg glucose in normal male Wistar rats[1].
(S)-V-0219 (0. 4 mg/kg; i.g.) hydrochloride is orally active in fatty diabetic Zucker rats[1].
(S)-V-0219 (0.1-5 μg/kg in 5 μL; i.c.v.) hydrochloride decreases feeding in 12-h fasted male Wistar rats[1].

Reference

[1]. Decara JM, et, al. Discovery of V-0219: A Small-Molecule Positive Allosteric Modulator of the Glucagon-Like Peptide-1 Receptor toward Oral Treatment for “Diabesity”. J Med Chem. 2022 Apr 14;65(7):5449-5461.
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