| Bioactivity | (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]. |
| Target | GLP-1R |
| Invitro | (S)-V-0219 ((S)-9) (0.1 nM) hydrochloride 增强稳定表达 hGLP-1R 的 HEK 细胞中的钙通量[1]。(S)-V-0219 (0.1 nM) hydrochloride 在高葡萄糖浓度下增强稳定的人胰腺细胞系 EndoC-βH1 中 GLP-1 刺激的胰岛素分泌[1]。 |
| In Vivo | (S)-V-0219 ((S)-9) (0.04-0.2 mg/kg; i.p.) hydrochloride 在正常雄性 Wistar 大鼠中注射 2 g/kg 葡萄糖后改善葡萄糖处理[1]。(S)-V-0219 (0. 4 mg/kg; i.g.) hydrochloride 在肥胖糖尿病 Zucker 大鼠中具有口服活性[1]。 (S)-V-0219 (0.1-5 μg/kg in 5 μL; i.c.v.) hydrochloride 减少 12 小时禁食雄性 Wistar 大鼠的摄食[1]。 |
| Name | (S)-V-0219 hydrochloride |
| Formula | C20H26ClF3N4O2 |
| Molar Mass | 446.89 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| 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. |
(S)-V-0219 hydrochloride
CAS: F: C20H26ClF3N4O2 W: 446.89
(S)-V-0219 hydrochloride is an enantiomer of V-0219 (HY-143312). V-0219 is an orally active and positive allosteric modu
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