ML-184  (Synonyms: CID2440433)

ML-184 (CID244033) is a selective GPR55 agonist with an EC₅₀ of 250 nM, more than 100-fold selectivity for GPR55 over GPR35, CB1, and CB2. ML-184 induces ERK1/2 phosphorylation and PKCβII translocation to the plasma membrane via activation of GPR55. ML-184 (CID2440433) increases the proliferation of neural stem cells and promotes neuronal differentiation in vitro^[1][2][3].

ML-184 (1 μM; 48 h) increases the proportion of cells in the S phase and promotes cell proliferation in human neural stem cells (hNSCs), an effect that could be blocked by pretreatment with 5 μM ML193^[2].
ML-184 (1 μM; 10 d) significantly increases the mRNA and protein expressions of neuronal markers βIII-tubulin and microtubule-associated protein 2 (MAP2) in hNSCs, without significant effect on the astrocyte marker S100β^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

ML-184 or combined with Sitagliptin (HY-13749) can improve glucose tolerance, insulin sensitivity and insulin secretion response in high-fat-fed (HFF) mice. Islet Ki-67 staining shows that ML-184 increases β-cell proliferation and upregulates pancreatic GPR55, ERK1 and ERK2 gene expression in HFF mice^[3].
ML-184 can increase β-cell area and β-cell mass and reduce α-cell area and mass in high-fat-fed (HFF) mice. ML-184 or combined with Sitagliptin (HY-13749) can significantly increase circulating GIP levels and reduce food intake in mice; it can also increase jejunal GPR55 and JNK1 gene expression levels^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

470.63

C₂₅H₃₄N₄O₃S

794572-10-4

Solid

White to off-white

CC1=CC=CC(N2CCN(CC2)C(C3=CC(S(N(C)C)(=O)=O)=CC=C3N4CCCC4)=O)=C1C

Room temperature in continental US; may vary elsewhere.

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

• [1]. Kotsikorou E, et al. Identification of the GPR55 agonist binding site using a novel set of high-potency GPR55 selective ligands. Biochemistry. 2011 Jun 28;50(25):5633-47.  [Content Brief]

  [2]. Hill JD, et al. Activation of GPR55 increases neural stem cell proliferation and promotes early adult hippocampal neurogenesis. Br J Pharmacol. 2018 Aug;175(16):3407-3421.  [Content Brief]

  [3]. Corbett Reece, et al. Once-daily oral administration of gpr55 agonist ml-184 has direct and indirect benefits on [beta]-cell and gastrointestinal health in obese-diabetic mice. Endocrine Abstracts. Vol. 104. Bioscientifica, 2024.