GPR88 agonist 2

• CAT Number: I040675
• CAS Number: 2821859-71-4
• Purity: ≥95%
• Synonyms: N-methyl-1-[(2R)-2-[4-[(2S)-2-methylbutoxy]phenyl]-2-[[(2S)-2-phenylpropanoyl]amino]ethyl]triazole-4-carboxamide
• InChI: InChI=1S/C26H33N5O3/c1-5-18(2)17-34-22-13-11-21(12-14-22)23(15-31-16-24(29-30-31)26(33)27-4)28-25(32)19(3)20-9-7-6-8-10-20/h6-14,16,18-19,23H,5,15,17H2,1-4H3,(H,27,33)(H,28,32)/t18-,19-,23-/m0/s1
• InChIKey: LVUMROGMIIBKQA-YDHSSHFGSA-N
• SMILES: CCC(C)COC1=CC=C(C=C1)C(CN2C=C(N=N2)C(=O)NC)NC(=O)C(C)C3=CC=CC=C3

GPR88 agonist 2 (compound 53) is a potent and brain-penetrantGPR88 agonist with an EC50 value of 14 µM in GPR88 cAMP functional assay[1].
GPR88 agonist 2 significantly enhance [35S]GTPγS binding activity (EC50: 8.9 μM) in WT mouse striatal membranes, but GPR88 agonist 2 is inactive in striatal membranes prepared from GPR88 KO mice.[1].
GPR88 agonist 2 (20mg/ml, ip) has a good plasma exposure (Cmax:1670 ng/mL) and acceptable metabolic stability (T1/2:4.66h, CL:21mL/mg/kg)[1].
GPR88 agonist 2 (20mg/ml, ip) has sufficient brain penetration (Cmax:576 ng/mL)[1].
Pharmacokinetic analysis in mice[1]

20 mg/kg, ip
Cmax (ng/mL)
T1/2 (h)
CL(mL/min/kg)
B/Pratio

plasma
1670
5.6
21
0.34

brain
576
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