A1480LS
DAGLA and DAGLB were both inhibited with similar potency across species with an average IC50 15 nM. Covalent, irreversible mechanism of inhibition. A1480LS effectively inhibited conversion of isotopically labeled DAG substrate (DAG(18:0/AA-d8)) to 2-AG-d8, with an IC50 of 8.6 nM; Specificity: Only AHBD6 and carboxylesterase 2 (CES2) were inhibited >50% among 43 enzymes detected
General
Type : Trifluoro, Piperazine, Indazole, Urea derivative
Chemical_Nomenclature : 2-[(2S)-2-benzyl-4-[6-(trifluoromethyl)pyrazin-2-yl]piperazine-1-carbonyl]-5-phenylindazole
Canonical SMILES : C([N]1N=C2C(=C1)C=C(C=C2)C3=CC=CC=C3)(=O)N4[C@H](CN(CC4)C5=NC(=CN=C5)C(F)(F)F)CC6=CC=CC=C6
InChI : InChI=1S\/C30H25F3N6O\/c31-30(32,33)27-17-34-18-28(35-27)37-13-14-38(25(20-37)15-21-7-3-1-4-8-21)29(40)39-19-24-16-23(11-12-26(24)36-39)22-9-5-2-6-10-22\/h1-12,16-19,25H,13-15,20H2\/t25-\/m0\/s1
InChIKey : LULPTIBVONZWPH-VWLOTQADSA-N
Other name(s) :
Target
Families : A1480LS ligand of proteins in family
Lipase_3
Protein :
human-DAGLA
human-DAGLB
References (2)
| Title : Suppression of pain transmission and behavior by inhibition of peripheral diacylglycerol metabolism - Tufail_2026_Cell.Chem.Biol_33_74 |
| Author(s) : Tufail YZ , Guijas C , Kummer DA , Henry CL , Moody JV , Andalis T , Boyd B , Gil J , Ha J , Herbst DM , Herbst-Graham RA , Hutton C , Kozina EM , Niphakis MJ , Ngo N , O'Neill GP , Reardon HT , Shaghafi M , Ulanovskaya OA , Raffaele N , Viader A , Weber OD , Jones TK , Grice CA , Wiener JJM , Simonsen KB , Blankman JL , Clapper JR |
| Ref : Cell Chemical Biology , 33 :74 , 2026 |
| Abstract : |
| PubMedSearch : Tufail_2026_Cell.Chem.Biol_33_74 |
| PubMedID: 41544618 |
| Gene_locus related to this paper: human-DAGLA , human-DAGLB |
| Title : Suppression of pain transmission and behavior by inhibition of peripheral diacylglycerol metabolism - Tufail_2026_Cell.Chem.Biol_33_74 |
| Author(s) : Tufail YZ , Guijas C , Kummer DA , Henry CL , Moody JV , Andalis T , Boyd B , Gil J , Ha J , Herbst DM , Herbst-Graham RA , Hutton C , Kozina EM , Niphakis MJ , Ngo N , O'Neill GP , Reardon HT , Shaghafi M , Ulanovskaya OA , Raffaele N , Viader A , Weber OD , Jones TK , Grice CA , Wiener JJM , Simonsen KB , Blankman JL , Clapper JR |
| Ref : Cell Chemical Biology , 33 :74 , 2026 |
| Abstract : |
| PubMedSearch : Tufail_2026_Cell.Chem.Biol_33_74 |
| PubMedID: 41544618 |
| Gene_locus related to this paper: human-DAGLA , human-DAGLB |