ML193 free base · Synonyms: CID 1261822

ML-193 is a potent and selective antagonist of GPR55.

For research use only. Not for human or veterinary use.

Target GPR55

Research area Neurological Disease

Purity >98% Stock Inquire

Data Sheet SDS COA

ML193 structure

CAS No.: 713121-80-3

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
250 mg	USD 550.00	BP-00937-250mg	In stock	Get quote
500 mg	USD 860.00	BP-00937-500mg	In stock	Get quote
1 g	USD 1,400.00	BP-00937-1g	In stock	Get quote
2 g	USD 2,200.00	BP-00937-2g	In stock	Get quote
3 g	USD 2,700.00	BP-00937-3g	In stock	Get quote

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Description

ML-193 (CID 1261822) is a potent and selective antagonist of GPR55, with an IC50 of 221 nM. ML-193 shows more than 27-fold selectivity for GPR55 over GPR35, CB1 and CB2. ML-193 can improve the motor and the sensorimotor deficits of Parkinson's disease (PD) rats.

Biological activity

In Vitro ML-193 (0.01-100 μM; pretreated for 15 min) inhibits β-arrestin trafficking induced by L-α-lysophophosphatidylinositol (LPI, 10 μM) and ML186 (1 μM) with IC50s of 0.22 μM and 0.12 μM, respectively. ML-193 (0.01-10 μM; pretreated for 30 min) decreases the LPI-mediated ERK1/2 phosphorylation, with an IC50 of 0.2 μM in U2OS cells. ML-193 (5 μM; pretreated for 30 min) attenuates the GPR55 agonists induced increases in hNSCs proliferation rates. ML-193 (5 μM; 10 d) attenuates the ML184-induced increases in hNSCs differentiation. In Vivo ML193 (1 and 5 μg/rat; intra-striatal at a rate of 1 μL/min) attenuates sensorimotor deficits and slip steps, increases motor coordination in PD rats.

Identifiers

SMILES: CC(C(C)=NO1)=C1NS(C(C=C2)=CC=C2NC(C3=CC(C4=CC=CC=N4)=NC5=C3C=C(C)C=C5C)=O)(=O)=O
InChIKey: HTSLEZOTMYUPLU-UHFFFAOYSA-N

Specifications

MW (average): 527.5940
Formula: C₂₈H₂₅N₅O₄S
CAS No.: 713121-80-3
Physical state: Solid
Color: white to light yellow
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder 4℃ 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO

Documents

References

[1]. Heynen-Genel S, et, al. Screening for Selective Ligands for GPR55-Antagonists. Probe Reports from the NIH Molecular Libraries Program. 2010 Oct 30.

[2]. Kotsikorou E, et, al. Identification of the GPR55 antagonist binding site using a novel set of high-potency GPR55 selective ligands. Biochemistry. 2013 Dec 31;52(52):9456-69.

[3]. Fatemi I, et, al. The effect of intra-striatal administration of GPR55 agonist (LPI) and antagonist (ML193) on sensorimotor and motor functions in a Parkinson's disease rat model. Acta Neuropsychiatr. 2021 Feb;33(1):15-21.

[4]. 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.

Same research area

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