GAT229
SIGMA/SML1951 - ≥98% (HPLC)
Synonym: S-
CAS Number: 889860-85-9
Empirical Formula (Hill Notation): C22H18N2O2
Molecular Weight: 342.39
Linear Formula: C22H18N2O2
Product Type: Chemical
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| assay | ≥98% (HPLC) |
| color | white to beige |
| form | powder |
| optical activity | [α]/D -80 to -94°, c = 1 in methanol |
| solubility | DMSO: 20 mg/mL, clear |
| storage temp. | 2-8°C |
| Biochem/physiol Actions: | Gαi/o-biased CB1 cannabinoid postive allosteric modulator (PAM) with no intrinsic activity |
| Biochem/physiol Actions: | GAT229 is the S-(-)-enantiomer of GAT211, a positive allosteric modulator (PAM) of cannabinoid CB1 receptor signaling that was found to amplify the therapeutic effect of endocannabinoids without the negative side effects of psychoactivity or tolerance. GAT229 was found to be a potent, Gαi/o-biased CB1 PAM without intrinsic activity, while the R-(+)-enantiomer, GAT228, was found to be an unbiased CB1 allosteric agonist. In radioligand binding assays, both GAT228 and GAT229 behaved as PAMs of orthosteric ligand binding, with GAT229 exhibiting higher potency and efficacy. Allosteric CB1R activation by GAT211 and its enantiomers could be a better therapeutic strategy for enhancing endogenous cannabinergic activity than targeting endocannabinoid-degrading enzymes with small-molecule inhibitors, with a lower likelihood of tolerance and dependence. |
| RIDADR | NONH for all modes of transport |
| WGK Germany | WGK 3 |
| Flash Point(F) | Not applicable |
| Flash Point(C) | Not applicable |
| Purity | ≥98% (HPLC) |
| Storage Temp. | 2-8°C |
| UNSPSC | 12352200 |