GLP-1R Antagonist 1
CAS No. : 488097-06-9
| Size | Price | Stock |
|---|---|---|
| 5mg | $110 | In-stock |
| 10mg | $180 | In-stock |
| 25mg | $350 | In-stock |
| 50mg | $550 | In-stock |
| 100mg | $850 | In-stock |
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| Cat. No. : | HY-101116 |
| M.Wt: | 440.73 |
| Formula: | C16H11ClF6N4O2 |
| Purity: | >98 % |
| Solubility: | DMSO : 100 mg/mL (ultrasonic) |
GLP-1R Antagonist 1 (compound 5d) is an orally active, CNS penetrant and non-competitive antagonist of glucagon-like peptide 1 receptor (GLP-1R), with an IC50 of 650 nM[1].
IC50 & Target:IC50: 650 nM (GLP-1R)[1].
In Vitro:GLP-1R Antagonist 1 (compound 5d) (0.3-10 μM) inhibits the activity of glucagon-like peptide 1 (GLP-1) (7-36) amide in a dose-dependent manner in human TREx293 HEK cells[1].
In Vivo:GLP-1R Antagonist 1 (compound 5d) (10 mg/kg, p.o.) increases the levels of blood glucose and decreases the levels of blood insulin in male Sprague-Dawley rats[1].
Pharmacokinetic Analysis in MC38 Syngeneic Model[1]
| Route | Dose (mg/kg) | CLp (mL/min/kg) | t1/2 (min) | Vss (L/kg) | %F |
| i.v., p.o. | 1, 3 | 4.79 | 587 | 3.57 | 50 |
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